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Catalog No. Product Name Information product Use Citations sản phẩm Validations
S1653 Tretinoin (NSC 122758)

Tretinoin (NSC 122758, Retinoic acid, All-trans Retinoic Acid, ATRA, vitamin A acid, Vesanoid, Airol, Renova, Atralin, Retin-A, Avita, Stieva-A), which is a ligand for both the retinoic acid receptor (RAR) và the retinoid X receptor (RXR), can induce granulocytic differentiation và apoptosis in acute promyelocytic leukemia (APL) cells.

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E2441 Qingyangshengenin

Qingyanshengenin (NSC 379666), a pregnane glycoside, is a C21 steroidal aglycone isolated from the root of Cynanchumot ophyllum (Asclepiadaceae). Qingyanshengenin has anti-cancer activity.

S3223 L-Quebrachitol

L-Quebrachitol (L-QCT), a natural product isolated from many plants, promotes proliferation và cell DNA synthesis. L-Quebrachitol upregulates bone morphogenetic protein-2 (BMP-2) & runt-related transcription factor-2 (Runx2) và regulatory genes associated with mitogen-activated protein kinase (MAPK) & Wnt/β-catenin signaling pathway, while down-regulating the receptor activator of the nuclear factor-κB(NF-κB) ligand (RANKL) mRNA level.

L2700 Ion Channel Ligand Library

A quality collection of 224 small molecule modulators used for Ion channel research.

S8158 PD-1/PD-L1 Inhibitor 3

PD-1/PD-L1 Inhibitor 3(Programmed Death-1/Programmed Death-Ligand 1 Inhibitor 3)is a Macrocyclic inhibitor of PD-1/PD-L1 interaction with IC50 of 5.6 nM

Biochem Pharmacol, 2022, 197:114940 ChemMedChem, 2022, e202200091 Nat Chem, 2021, 10.1038/s41557-021-00829-5
S6632 Mirogabalin (DS-5565)

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand that has been used in trials studying the treatment of Post-herpetic Neuralgia, Pain Associated With Fibromyalgia, and Diabetic peripheral neuropathic pain.

S6981 Glycerol phenylbutyrate

Glycerol phenylbutyrate (GT4P, HPN-100M, Ravicti) is a nitrogen-binding agent & acts as a sigma-2 (σ2) receptor ligand with a pKi of 8.02. Glycerol phenylbutyrate is a prodrug in which phenylbutyrate (PBA) is released from the glycerol backbone by lipases in the gastrointestinal tract.

S3469 Shield-1

Shield-1 is a specific, cell-permeant và high-affinity ligand of FK506-binding protein-12 (FKBP). Shield-1 reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 stabilizes the entire fusion protein.

Cell Rep, 2022, 38(12):110536
S3617 (20S)-Protopanaxatriol

(20S)-Protopanaxatriol (g-PPT, 20(S)-APPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta và could modulate endothelial cell functions through the glucocorticoid receptor (GR) and estrogen receptor (ER).

S9937 CU-CPD107

CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists và ssRNA ligands. In the presence of R848, CU-CPD107 acts as a TLR8 signaling inhibitor (IC50=13.7 μM). In the presence of ssRNA, CU-CPD107 shows synergistic agonist activities, while CU-CPD107 alone is unable to influence TLR8 signaling.

S6993 (+)-JQ1 carboxylic acid

(+)-JQ1 carboxylic acid ((+)-JQ1-COOH) is a (+)-JQ1 with a carboxylic acid functional group. (+)-JQ1 carboxylic acid ((+)-JQ1-COOH) can be used as a precursor lớn a PROTAC that targets BET bromodomains after conjugation to lớn a linker và E3 ligase ligand.

E0996 3-Aminocoumarin

3-Aminocoumarin (3-Coumarinamine) is ofter used as a ligand for the formation of Cr(III), Ni(II), và Cu(II) complexes.

S6994 TD-165

TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker và an von Hippel-Landau (VHL) binding group.

S6996 LC-2

LC-2 is a first PROTAC capable of degrading endogenous KRASG12C with DC50s between 0.25 μM & 0.76 μM. LC-2 covalently binds KRASG12C with a MRTX849 warhead & recruits the E3 ligase VHL, inducing rapid & sustained KRASG12C degradation leading to lớn suppression of MAPK signaling.

E2673 FGIN 1-27

FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions.

S2754 Xevinapant (AT406)

Xevinapant (AT406, ARRY-334543, Debio1143, SM-406) is a potent Smac mimetic và an antagonist of IAP (inhibitor of apoptosis protein via E3 ubiquitin ligase), binding to lớn XIAP-BIR3, cIAP1-BIR3 và cIAP2-BIR3 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, 50- to 100-fold higher affinities than the Smac AVPI peptide. Phase 1.

Theranostics, 2021, 11(18):9009-9021 Cancers (Basel), 2021, 13(14)3585 Neoplasia, 2021, 23(5):539-550
S0824 BMVC-8C3O

BMVC-8C3O is a DNA G-quadruplexe (G4) ligand that induces topological conversion of non-parallel to lớn parallel forms in human telomeric DNA G4s.

A2015 Avelumab (anti-PD-L1)

Avelumab (anti-PD-L1) (Bavencio, MSB0010718C) is a fully human IgG1 monoclonal antibody that targets the protein programmed death-ligand 1 (PD-L1). Avelumab exhibits potential antibody-dependent cell-mediated cytotoxicity & is used for the treatment of several kinds of carcinoma. MW=143.8 kDa.

A2013 Durvalumab (anti-PD-L1)

Durvalumab (anti-PD-L1) is a selective, high affinity human IgG1 mAb that blocks programmed cell death ligand-1 (PD-L1) binding to PD-1 (IC50=0.1 nM) và CD80 (IC50=0.04 nM). MW=146.3 kDa.

J Med Chem, 2022, 65(5):3879-3893 Mol Pharm, 2022, 10.1021/acs.molpharmaceut.2c00084 J Med Chem, 2021, 64(15):11614-11636
S8105 ZM241385

ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.

Front Cell Dev Biol, 2022, 10:827714 Mol Biol Rep, 2021, 10.1007/s11033-021-07017-1 Cell Mol Immunol, 2020, 10
S0281 U93631

U93631 is a ligand of GABAA receptor of novel chemical structure with IC50 of 100 nM. U93631 induces a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

S1029 Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination & degradation of two lymphoid transcription factors, IKZF1 và IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression và inhibit VEGF expression và induces apoptosis.

Nat Commun, 2022, 13(1):1009 Cell Death Dis, 2022, 13(3):197 Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1851 Oxibendazole

Oxibendazole is a benzimidazole drug that interferes with metabolic pathways, used to lớn protect against roundworms, strongyles, threadworms, pinworms and lungworm infestations in horses and some domestic pets.

Oncol Lett, 2018, 15(2):2218-2226
E0460 ELN441958

ELN-441958 is a potent và neutral antagonist of B1 receptor that inhibits the binding of the B1 agonist ligand <3H>DAKD lớn IMR-90 cells with Ki of 0.26 nM.

E0455 Nimbolide

Nimbolide inhibits auto-ubiquitination of the E3 ligase RNF114 & p21 ubiquitination in vitro. Nimbolide induces apoptosis through inactivation of NF-κB.

S1061 Nutlin-3

Nutlin-3 is a potent & selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.

Nat Biotechnol, 2022, 10.1038/s41587-021-01172-3 J Exp Clin Cancer Res, 2022, 41(1):79 Cell Biosci, 2022, 12(1):20
S3972 Lobeline hydrochloride

Lobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors.

J Cell Mol Med, 2020, 10.1111/jcmm.16029
S5543 1, 10-Phenanthroline monohydrate

1,10-Phenanthroline is a classic chelating bidentate ligand for transition metal ions that has played an important role in the development of coordination chemistry. It is an inhibitor of metallopeptidases.

Int Immunopharmacol, 2022, 106:108578
S9775 SCR130

SCR130 is a novel DNA repair inhibitor with IC50s of 14 μM in Reh cells and 2 μM in Nalm6 cells. SCR130 specifically inhibits DNA Ligase IV‐mediated joining with minimal or no effect on Ligase III và Ligase I mediated joining.

S5004 Pimecrolimus

Pimecrolimus (ASM 981) is an immunophilin ligand, which binds specifically khổng lồ the cytosolic receptor, immunophilin macrophilin-12 (FKBP-12); a calcineurin inhibitor.

Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 34(6):1911-1918
S7963 TIC10 (ONC201)

TIC10 (ONC201) inactivates Akt and ERK to lớn induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.

Mol Cell, 2020, 80(6):1104-1122.e9 ACS Chem Biol, 2019, 14(5):1020-1029 Eur J Pharmacol, 2019, 857:172423
S8842 BAY-218

BAY-218 is a potent & selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands.

EMBO Mol Med, 2022, 14(3):e14552 Acta Biochim Biophys Sin (Shanghai), 2021, gmab017
A2020 Denosumab (anti-RANK ligand)

Denosumab (anti-RANK ligand) (AMG-162, Prolia, Xgeva) is a fully human monoclonal antibody that selectively inhibits primate RANKL. Denosumab inhibits the ability of human RANKL (143–317) khổng lồ stimulate the formation of osteoclasts derived from murine RAW 264.7 cells with an IC50 value of 1.64 nM.

A2022 Cemiplimab (anti-PD-1)

Cemiplimab (anti-PD-1) (Libtayo, REGN-2810, cemiplimab-rwlc) is an intravenous human monoclonal antibody directed against programmed cell death-1 receptor (PD-1) và blocks its interaction with programmed death ligands 1 (PD-L1) và 2 (PD-L2). Cemiplimab blocks T-cell inactivation and enhances the immune system"s anti-tumor response.

S9612 ACBI1

ACBI1 is a potent & cooperative PROTAC degrader of SMARCA2, SMARCA4PBRM1 with DC50 of 6 nM, 11 nM & 32 nM for SMARCA2, SMARCA4 và PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 induces anti-proliferative effects & apoptosis.

S9694 MLi-2

MLi-2 is an orally active và highly selective inhibitor of LRRK2. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro with IC50 of 0.76 nM, a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 with IC50 of 1.4 nM, and a radioligand competition binding assay with IC50 of 3.4 nM.

S4995 Nicotinic acid N-oxide

Nicotinic acid N-oxide (Oxiniacic acid, Nicotinic acid 1-oxide) is nicotinic acid derivative that acts as a ligand & forms lead-carboxylate complexes having phosphorescent properties.

S0767 NL-1

The mitochondrial mitoNEET ligand NL-1 is a mitoNEET inhibitor, which induces a concentration-dependent decrease in cell viability with an IC50 of 47.35 μM & 56.26 μM in REH & REH/Ara-C cells respectively. The docking studies using liver mitochondrial suspensions show the IC50 of NL-1 binding for <3H>-rosiglitazone is 0.9 μM & the Ki for NL-1 site 1 & site 2 was 4.78 & 2.77, respectively.

S9869 NSC622608

NSC622608 is a first small-molecule ligand for V-domain Ig Suppressor of T-cell Activation (VISTA) with an IC50 of 4.8 μM in TR-FRET assay.

S0070 Gefitinib-based PROTAC 3

Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to lớn a VHL ligand via a linker induces degradation of EGFR & mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.

S6966 MT-802

MT-802 is a potent PROTAC that induces Bruton"s tyrosine kinase (BTK) knockdown. MT-802 recruits BTK to the cereblon E3 ubiquitin ligase complex lớn trigger BTK ubiquitination and degradation via the proteasome. MT-802 has potential for treatment of C481S mutant chronic lymphocytic leukemia (CLL).

S6906 Capric acid

Capric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes khổng lồ seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to lớn its specific melting range the hàng hóa may be solid, liquid, a solidified melt or a supercooled melt.

S1069 Luminespib (NVP-AUY922)

Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 và TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein và results in growth inhibition, autophagy & apoptosis. Phase 2.

Biomedicines, 2022, 10(3)624 Cell Death Discov, 2022, 8(1):86 Cell Rep, 2021, 34(11):108870
S9889 dCBP-1

dCBP-1 is a potent & selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression.

S8760 Iberdomide (CC220)

Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities.

ARV-825 is a BRD4 Inhibitor that recruits BRD4 to lớn the E3 ubiquitin ligase cereblon, leading lớn fast, efficient, & prolonged degradation of BRD4 and sustained down-regulation of MYC.

Mol Oncol, 2022, 10.1002/1878-0261.13195 Methods Mol Biol, 2021, 2365:3-20 J Exp Clin Cancer Res, 2019, 38(1):383
S1071 HA14-1

HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.

S4625 Alcaftadine

Alcaftadine (Lastacaft, R89674) is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 & H4 receptors with no affinity for the H3 receptor.

S0322 BC-1215

BC-1215 is an inhibitor of F-box protein 3 (Fbxo3, a ubiquitin E3 ligase component) with IC50 of 0.9 μg/mL and LC50 of 87 μg/ml for IL-1β release. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1-6.

S7742 SCR7

SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ). It increases the efficiency of HDR-mediated genome editing up lớn 19-fold using CRISPR/Cas9 in mammalian cells & mouse embryos.

Protein Cell, 2021, 10.1007/s13238-021-00879-y 10.1126/science.abc5386 Mol Oncol, 2021, 15(12):3490-3512 Pharmacol Res, 2021, S1043-6618(21)00518-1
S9807 EN4

EN4, a covalent ligand that targets cysteine 171 (C171) of MYC, is selective for c-MYC over N-MYC & L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

S5775 SR1078

SR1078, a synthetic ligand for RORα and RORγ, functions as a RORα/γ agonist.

Cell Death Dis, 2021, 12(3):247
E2065 Aconine

Aconine, a derivative of aconitum alkaloids, can inhibit NF- κB activation induced by NF-κ B receptor activator ligand.

S4942 4-Hydroxy-3,5-dimethoxybenzyl alcohol

4-Hydroxy-3,5-dimethoxybenzyl alcohol (Syringic alcohol, Syringyl alcohol) is a kind of phenol with antiviral properties.

S9832 CC-90009

CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 khổng lồ S phase transition 1) for proteasomal degradation.

S7892 Avadomide (CC-122)

Avadomide (CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor & immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN.

Leukemia, 2021, 35(5):1330-1343 Mol Ther Oncolytics, 2020, 18:215-225 Blood Adv, 2019, 3(14):2105-2117
S0095 VL285

VL285 is a potent VHL ligand that degrades HaloTag7 fusion proteins. Cotreatment with excess VL285, the vi xử lý core VHL ligand from which HaloPROTAC3 is derived, is able khổng lồ significantly reduce HaloPROTAC3 mediated activity to 50% degradation.

E3619 Lonicerae Flos Extract

Lonicerae Flos Extract is extracted from Lonicerae flos, the flower bud of Lonicera macranthoides Hand.-Mazz., Lonicera hypoglauca Miq., Lonicera confusa DC., or Lonicera fulvotomentosa Hsu et S. C. Cheng. Lonicerae flos is a traditional Chinese medicine used in the treatment of inflammatory and infectious diseases. Lonicerae flos extract increases survival rates of cecal ligation & puncture (CLP)-induced septic rats.

S0097 (S,R,S)-AHPC (MDK7526)

(S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potential useful for the targeted degradation of the androgen receptor. (S,R,S)-AHPC can be connected to lớn the ligand for protein such as BCR-ABL1 by a linker to size PROTACs such as GMB-475. GMB-475 induces the degradation of BCR-ABL1 with IC50 of 1.11 μM in Ba/F3 cells.

S0102 L 189

L 189 is a novel human DNA ligase inhibitor with IC50 of 5 μM, 9 μM & 5 μM for hLigI, hLigIII và hLigIV, respectively. L 189 inhibits base excision repair (BER) và non-homologous end joining (NHEJ). L 189 specifically sensitizes cancer cells khổng lồ DNA damage.

S7261 Beta-Lapachone

Beta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.

không tính phí Radic Biol Med, 2021, 173:64-69 Front Pharmacol, 2021, 12:766909 Mutagenesis, 2021, geab014
S3502 (S,R,S)-AHPC-PEG4-NH2 hydrochloride

(S,R,S)-AHPC-PEG4-NH2 hydrochloride (VH032-PEG4-NH2 hydrochloride, VHL Ligand-Linker Conjugates 4 hydrochloride, E3 ligase Ligand-Linker Conjugates 7) is a PROTAC E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand & 4-unit PEG linker.

S3786 Glabridin

Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding tên miền of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation và improving learning & memory.

Life Sci, 2021, S0024-3205(20)31752-5
S6224 (R)-Serine

(R)-Serine is the R-enantiomer of serine, which is used in the biosynthesis of proteins. (R)-Serine acts as obligatory coagonist at the glycine site associated with the N-methyl-D-aspartate subtype of glutamate receptors (NMDAR) and has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, & cell migration.

S1567 Pomalidomide (CC-4047)

Pomalidomide (CC-4047) inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase và inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis và cell cycle arrest.

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Nat Commun, 2022, 13(1):1009 Hum Cell, 2022, 10.1007/s13577-022-00671-y Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
S9724 SZL P1-41

SZL P1-41 (compound #25) is a specific inhibitor of S-phase kinase-associated protein 2 (Skp2) that indeed binds to Skp2, prevents Skp2-Skp1 interaction and inhibits Skp2 SCF E3 ligase activity, which consequently suppresses survival of cancer cells & cancer stem cells. SZL P1-41 causes higher apoptosis rates in cancer cells.

S6934 AMG-9810

AMG-9810 is potent, competitive và selective vanilloid receptor 1 (TRPV1) antagonist & inhibits capsaicin activation with IC50 of 24.5 nM & 85.6 nM for human TRPV1 và rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, & endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.

S2314 Kaempferol (NSC 407289)

Kaempferol (NSC 407289, Robigenin), a natural flavonol, functions as an ERRα & ERRγ inverse agonist. It inhibits topoisomerase I catalyzed DNA religation & may also inhibit the activity of fatty acid synthase.

Molecules, 2021, 26(5)1210 Eur J Pharmacol, 2021, 907:174251 Nat Metab, 2021, 10.1038/s42255-021-00479-4
S8449 VH298

VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) và 80 nM in a competitive fluorescence polarization assay. VH-298 can be used in PROTAC technology.

E0102 I-191

I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways và functional responses. I-191 also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88.

S1000 Thalidomide fluoride

Thalidomide fluoride (Cereblon ligand 4, E3 ligase Ligand 4) is the Thalidomide-based Cereblon ligand that is applicable to the recruitment of CRBN protein. Thalidomide fluoride can be connected lớn the ligand for IRAK4 protein by a linker to khung PROTAC IRAK4 degrader-1.

J Med Chem, 2022, 65(1):747-756
S1015 Thalidomide-OH

Thalidomide-OH (Cereblon ligand 2, E3 ligase Ligand 2) is the Thalidomide-based Cereblon ligand that is applicable khổng lồ the recruitment of CRBN protein. Thalidomide-OH can be connected lớn the ligand for protein by a linker to khung PROTACs.

S1016 Lenalidomide-Br

Lenalidomide-Br is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, & is that is applicable lớn the recruitment of CRBN protein. Lenalidomide-Br can be connected khổng lồ the ligand for protein by a linker to khung PROTACs.

Nat Commun, 2022, 13(1):1009 Cell Death Dis, 2022, 13(3):197 Blood Adv, 2022, bloodadvances.2021005772
S9052 Auraptene

Auraptene (7-geranyloxycoumarin) is a natural coumarin derived from citrus plants & possesses valuable pharmacological properties, including anticarcinogenic, anti-inflammatory, antihelicobacter, antigenotoxic, & neuroprotective effects. Auraptene inhibits matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8 & chemokine (C-C motif) ligand-5(CCL5).

S1062 (S,R,S)-AHPC hydrochloride

(S,R,S)-AHPC hydrochloride (VH032-NH2, VHL ligand 1) is the VH032-based VHL ligand that is applicable to the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC hydrochloride can be connected khổng lồ the ligand for protein by a linker to khung PROTACs.

S6926 GNF351

GNF351 is a potent antagonist of aryl hydrocarbon receptor (AHR). GNF351 interacts directly with the AHR ligand binding pocket và competes with a well-characterized photoaffinity AHR ligand for binding to the AHR with IC50 of 62 nM.

Front Pharmacol, 2021, 12:655281
S3557 CMP8

CMP8 is a selective and potent ligand for the estrogen receptor which binds to the mutant estrogen receptor ligand-binding domain (ERLBD) with IC50 of 29 nM, 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα, and hERβ, respectively.

S8432 Troglitazone (CS-045)

Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis và lipid peroxidation in Pfa1 cells.

Qingyangshengenin B, a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic activity.

S1989 GABAA receptor agent 1

GABAA receptor agent 1 is a high affinity ligand for GABAA receptor that exerts potent anticonvulsant activity.

S6020 Potassium thioacetate

Potassium thioacetate is widely used as a sulfur source in the synthesis of sulfur-containing organic compounds. It has been employed for the synthesis of heterocycles, polymers, transition-metal ligands, nanoparticles, bioactive compounds & macromolecular inclusion complexes.

E1144 dBRD9

dBRD9 is a bifunctional molecule that liên kết a small molecule that specifically binds khổng lồ the bromodomain of BRD9 & another ligand that recruits the cereblon E3 ubiquitin ligase, potently and selectively degrades BRD9 with IC50 of 104 nM in MOLM-13 cells.

S3792 Guggulsterone E&Z

Guggulsterone is one of the active constituent of Commiphora mukul. It occurs in two isomeric forms, namely Z-GS and E-GS. Guggulsterone act as antagonist ligands for the bile acid receptor, farnesoid X receptor, and as active ingredients responsible for the hypolipidemic activity.

Biochim Biophys Acta Mol Cell Biol Lipids, 2019, 1864(10):1293-1304 Int J Oncol, 2019, 54(3):879-892
S2592 Emapunil (AC 5216)

Emapunil (AC-5216, 18 kiloDalton Translocator Protein, XBD173) is a novel mitochondrial benzodiazepine receptor/translocator protein (MBR/TSPO) ligand. Emapunil(AC-5216) showes high affinity for MBRs prepared from rat whole brain with Ki of 0.297 nM and IC50 of 3.04 nM and 2.73 nM at rat glioma cells và human glioma cells, respectively.

S2416 Chondroitin sulfate

Chondroitin sulfate (CS) is a major component of the extracellular matrix (ECM) of many connective tissues, including cartilage, bone, skin, ligaments & tendons. It reduces the IL-1β-induced nuclear factor-kB (NF-κB) translocation in chondrocytes in vitro.

Nat Commun, 2020, 11(1):986
S8822 Ligandrol (LGD-4033)

Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) & selectivity.

J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Anal Bioanal Chem, 2021, 10.1007/s00216-021-03740-7
S8888 GMB-475

GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination & subsequent degradation of the oncogenic fusion protein.

E2565 Glabrone

Glabrone, an isoflavone isolated from Glycyrrhiza glabra roots, exhibits anti-influenza & significant PPAR-γ ligand-binding activities.

S8813 LIT-927

LIT-927 is a novel neutraligand of CXCL12 with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma.

J Biomed Mater Res B Appl Biomater, 2022, 10.1002/jbm.b.35021
S8975 Mezigdomide (CC-92480)

Mezigdomide (CC-92480) is a novel protein degrader và a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity.

S9659 UNC6852

UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC & contains an EED226-derived ligand & a ligand for VHL.

E2572 Tetrahydrocolumbamine

Tetrahydrocolumbamine ((-)-Isocorypalmine) is a dopamine receptor ligand isolated from the crude base fraction of Corydalis chaerophylla.

S1172 Serdemetan (JNJ-26854165)

Serdemetan (JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.

S8979 THAL-SNS-032

THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to lớn a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

S2936 BQT

BQT is a bound ligand of 6epv which is the ATAD2 bromodomain in complex with compound 5.

S1177 PD98059

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) & functions as an AHR antagonist.

Neuropathol Appl Neurobiol, 2022, e12795 Front Pharmacol, 2022, 13:817596 FASEB J, 2022, 36(5):e22292
A2000 Cetuximab (anti-EGFR)

Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR lớn block ligand stimulation. MW:145.781 KD.

Cell, 2022, 185(9):1521-1538.e18 Am J Cancer Res, 2022, 12(3):1393-1408 Adv Sci (Weinh), 2021, e2103360 3.">
S2556 Rosiglitazone (BRL 49653)

Rosiglitazone (BRL 49653) is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 & 9 nM for rat, 3T3-L1 & human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. Rosiglitazone modulates TRP channels & induces autophagy. Rosiglitazone prevents ferroptosis.

Redox Biol, 2022, 50:102256 Toxicology, 2022, 465:153048 Hum Cell, 2022, 10.1007/s13577-022-00671-y
E2275 (+)-Nortrachelogenin (Wikstromol)

(+)-Nortrachelogenin, a pharmacologically ligand from from wikstroemia indica, possesses antileukemic activity.

S1986 Meclizine 2HCl

Meclizine (NSC 28728) is a histamine H1 receptor antagonist used lớn treat nausea và motion sickness, has anti-histamine, anti-muscarinic & anti-oxidative phosphorylation properties, also an agonist ligand for mCAR (constitutive androstane receptor) và an inverse agonist for hCAR.

Anticancer Res, 2019, 39(7):3767-3775 Front Pharmacol, 2017, 8:693
S9672 PROTAC SGK3 degrader-1

PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3 (Serum/Glucocorticoid Regulated Kinase Family thành viên 3) for degradation.

A2033 Vibostolimab (anti-TIGIT)

Vibostolimab (anti-TIGIT, MK-7684) is a humanized monoclonal antibody that binds khổng lồ the T-cell immunoreceptor with immunoglobulin & ITIM domains (TIGIT), blocking the interaction between TIGIT and its ligands, CD112 & CD155, thereby activating T lymphocytes which help lớn destroy tumor cells.

S2907 Pirfenidone (S-7701)

Pirfenidone (S-7701, AMR-69) is an inhibitor for TGF-β production & TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, và also has anti-fibrotic và anti-inflammatory properties. Pirfenidone attenuates chemokine (CC motif) ligand-2 (CCL2) and CCL12 production with anti-fibrotic activity. Phase 3.

Cancer Biol Ther, 2022, 23(1):150-162 Sci Rep, 2022, 12(1):7 Integr Biol (Camb), 2022, 14(1):1-12
S9605 Apcin

Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds khổng lồ Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.

Prostate, 2021, 10.1002/pros.24257 Breast Cancer, 2021, 10.1007/s12282-021-01242-z
S5545 DL-Serine

Serine is a non-essential amino acid và a natural ligand và allosteric activator of pyruvate kinase M2.

E2334 Pinoresinol

Pinoresinol is a lignol of plant origin serving for defense in a caterpillar. Pinoresinol drastically sensitizes cancer cells against TNF-related apoptosis-inducing ligand (TRAIL) -induced apoptosis.

S1193 Thalidomide (K17)

Thalidomide (K17) was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.

Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 34(6):1911-1918
S0853 SR-717lithium

SR-717 lithium is a non-nucleotide STING agonist that demonstrates broad interspecies và interallelic specificity with EC50 of 2.1 μM và 2.2 μM in ISG-THP1 (WT) and ISG-THP1 (cGAS KO) cell lines, respectively. SR-717 lithium also induces the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner. SR-717 lithium exhibits antitumor activity.

Signal Transduct Target Ther, 2021, 6(1):382
E0644 X-PHOS

X-PHOS is a palladium complex of phosphine ligand.

S0645 NHPI-PEG4-C2-NHS ester

NHPI-PEG4-C2-NHS ester is used as a linker for antibody-drug conjugates (ADCs).

P1202 TMPyP4 tosylate

TMPyP4 tosylate (TMP 1363), a quadruplex-specific ligand, inhibits the interaction between G-quadruplex (G4)IGF-1 (Insulin-like growth factor type I). TMPyP4 tosylate is also a telomerase inhibitor with antitumor effects.

E0039 A-779

A-779 is a potent và selective antagonist for Angiotensin-(1–7) (Ang-(1-7)) with an IC50 of 0.3 nM in a radioligand binding assay. A-779 shows no significant affinity for AT1 or AT2 receptors at a concentration of 1 μM.

Elife, 2022, 11e72266
A2035 Sintilimab (anti-PD-1)

Sintilimab (anti-PD-1, IBI 308) is a fully human IgG4 monoclonal antibody that binds lớn PD-1 on the surface of T-cells, blocks the PD-1/PD-Ligand 1 (PD-L1) pathway, và reactivates T-cells lớn kill cancer cells.

S6132 All trans-Retinal

All trans-Retinal (Retinaldehyde, vitamin A aldehyde, Retinene), a component of the retinoid cycle, is converted to lớn retinoic acid in vivo by the action of retinal dehydrogenase. Retinoic acid is a ligand for both RAR and RXR. All trans-retinal ias a potent photosensitizer.

S2960 Miridesap

Miridesap (CPHPC, Ro63-8695, GSK2315698) is a ligand for serum amyloid p component (SAP) and intends lớn inhibit and dissociate SAP binding to amyloid fibrils và tangles.

S2643 4-IPP

4-IPP (4-Iodo-6-phenylpyrimidine) is an irreversible inhibitor of macrophage migration inhibitory factor (MIF) & a specific suicide substrate for MIF. 4-IPP can inhibit receptor activator of NF-κB ligand (RANKL)-induced osteoclastogenesis & potentiate osteoblast-mediated mineralization and bone nodule formation in vitro.

Mol Oncol, 2018, 12(8):1398-1409 SNU mở cửa Repository, 2018, None S-Space, 2018, N/A
S8306 Leukadherin-1

Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1(an agonist for the complement receptor 3 (CD11b/CD18)).

J Inflamm Res, 2021, 14:1341-1356 Research Square, 2021, 10.21203/rs.3.rs-870799/v1 bioRxiv, 2020, 10.1101/2020.11.25.398701
S9898 Proxalutamide (GT0918)

Proxalutamide (GT0918) is a second-generation androgen receptor antagonist that binds lớn the ligand-binding tên miền of AR with an IC50 of 32 nM in the AR competive binding assays.

S9146 Anwuligan

Anwuligan (Macelignan), a natural compound isolated from Myristica fragrans Houtt, has antimicrobial & anticariogenic activity against Streptococcus mutans và other streptococcus species. It also shows antioxidant, miễn phí radical scavenging, and neuroprotective activities.

S2678 NSC 207895

NSC 207895 (XI-006) suppresses MDMX with IC50 of 2.5 μM, leading to lớn enhanced p53 stabilization/activation and DNA damage, & also regulates MDM2, an E3 ligase.

Genes Dev, 2020, 34(7-8):526-543 Oncotarget, 2020, 11(46):4224-4242 Sci Rep, 2019, 9(1):1897
S2680 Ibrutinib (PCI-32765)

Ibrutinib (PCI-32765) is a potent và highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent khổng lồ Bmx, CSK, FGR, BRK, HCK, less potent to lớn EGFR, Yes, ErbB2, JAK3, etc. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.

S6794 Thalidomide-O-COOH (Cereblon ligand 3)

Thalidomide-O-COOH (Cereblon ligand 3, E3 ligase Ligand 3), a Thalidomide-based Cereblon (CRBN) ligand, is used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected lớn the ligand for protein by a linker to form PROTACs (Proteolysis Targeting Chimera).

S9848 LM11A-31

LM11A-31 is a small molecule p75NTR Ligand that reverses cholinergic neurite dystrophy in alzheimer's diseasemousemodels with mid- lớn late-stage disease progression.

S4927 Cyclen

Cyclen (1,4,7,10-tetraazacyclododecane) is a macrocycle capable of selectively binding cations that used as a ligand in chemistry for instance with chemicals used in MRI contrast agents.

S4916 Cyanidin Chloride

Cyanidin Chloride, a natural flavonoid abundant in fruits và vegetables, is an agonistic ligand for liver X receptor alpha và beta with EC50 of 3.5 μM and 125.2 μM, respectively.

P1124 Obestatin(rat)

Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction & antioxidant activities.

E0451 Dansylcadaverine(Monodansyl cadaverine)

Dansylcadaverine (Monodansyl cadaverine, MDC) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands.

S5024 Miriplatin

Miriplatin (SM-11355) is a derivative of cisplatin containing myristates as a carrier ligand. It is a novel lipophilic platinum complex developed to treat hepatocellular carcinoma.

A2028 Tiragolumab (anti-TIGIT)

Tiragolumab (anti-TIGIT) (RG6058, MTIG7192A) is a humanized IgG1/kappa monoclonal antibody that binds TIGIT lớn prevent its interaction with its ligand PVR (CD155).