Showing 1105–1120 of 5738 results

SBI-0206965

SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2.

AMI-1

AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.

BQ-123

BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

ONO-4059 Analogue

ONO-4059 analogue is an analogue of ONO-4059, which is a highly potent and selective oral BTK inhibitor with IC50 of 23.9 nM. Phase 1.

NVP-CGM097

NVP-CGM097 is a highly potent and selective MDM2 inhibitor with Ki value of 1.3 nM for hMDM2 in TR-FRET assay. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway.

Disodium (R)-2-Hydroxyglutarate

Disodium (R)-2-Hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 10.87 ± 1.85 mM.

LJI308

LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.

LJH685

LJH685 is a potent pan-RSK inhibitor with IC50 of 6 nM, 5 nM and 4 nM for RSK1, RSK2, and RSK3, respectively.

Oleuropein

Oleuropein is an antioxidant polyphenol isolated from olive leaf. Phase 2.

Oltipraz

Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.

SC79

SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.

8-Bromo-cAMP

8-bromo-cAMP is a cell permeable analog of cAMP that activates cyclic-AMP-dependent protein kinase with a Ka value of 0.05 μM and a PKA activator.

Tenofovir Alafenamide (GS-7340)

Tenofovir Alafenamide (GS-7340) is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and Hepatitis B.

Brilanestrant (GDC-0810, ARN-810)

Brilanestrant (GDC-0810, ARN-810） is a potent ER-α binder (ER-α, IC50 = 6.1 nM ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors.