AKR1C3-IN-1 is a highly potent inhibitor of aldo-keto reductaseAKR1C3 with an IC50 of 13 nM. It can be used in research targeting both breast and prostate cancer.

TAK-779(Takeda 779), a nonpeptide compound,  is a potent antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5. It also exhibits highly potent and selective inhibition of R5 HIV-1 replication with EC50 and EC90 of 1.2 and 5.7 nM, respectively. It also suppresses the development of the cytokine storm in the murine model of […]

Benzylamiloride hydrochloride (Benzamil hydrochloride) is an inhibitor of Na+/Ca2+ exchanger (NCX) with an IC50 ~100 nM. It reduces hyponatremic brain edema by blocking sodium influx in vivo.

Roflumilast N-oxide is an inhibitor of PDE type 4.

Hispidol is a potent inhibitor of TNF-α–induced monocyte adhesion to colon epithelial cells with an IC50 of 0.50 μM, and effectively suppresses LPS-induced TNF-α gene expression. Its inhibition of TNF-α is linked to reduced AP-1 transcriptional activity, highlighting its potential as a therapeutic candidate for IBD.

Hispidol is a potent inhibitor of TNF-α–induced monocyte adhesion to colon epithelial cells with an IC50 of 0.50 μM, and effectively suppresses LPS-induced TNF-α gene expression. Its inhibition of TNF-α is linked to reduced AP-1 transcriptional activity, highlighting its potential as a therapeutic candidate for IBD.

Compound E (γ-Secretase-IN-1) is a potent inhibitor of γ-secretase, which blocks γ-secretase-mediated cleavage of Notch with an IC50 of 0.32 nM. It also suppresses the production of β-amyloid(40) and β-amyloid(42) with IC50 values of 0.24 nM and 0.37 nM, respectively. It also inhibits Notch signalling, significantly disrupting gonadotropin-dependent follicle growth and halting progression to the […]