Activators & Inhibitors

hCAIX-IN-11 (Compound 5d) is a selective carbonic anhydrase IX and XII inhibitor. hCAIX-IN-11 shows K i s of 32.7 and 623.5 nM for hCA IX and hCA XII, respectively.

GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective inhibitor of cyclin G associated kinase (GAK) with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride can also bind to RIPK2.

ML261 is a inhibitor of hepatic lipid droplets formation with an IC 50 of 69.7 nM. ML261 has research value in non-alcoholic fatty liver disease (NAFLD) and inflammation.

BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor(IC50= 38.20 μM).

SARS-CoV-2 nsp13-IN-4 (C4 (d)) is a potent and selective small-molecule inhibitor of nsp13 helicase. SARS-CoV-2 nsp13-IN-4 inhibits the ssDNA+ ATPase activity of nsp13 with an IC 50 of 57 μM. SARS-CoV-2 nsp13-IN-4 can provide a broad-spectrum antiviral effect.

SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor (IC 50= 2.3 μM). SIRT5 inhibitor 2 shows inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 has research value in cancer and neurodegenerative diseases.

Antitumor agent-65 (Compound 5) is an analogue/derivative of (-)-cleistenolide. Antitumor agent-65 has potential in cancer research.

DNA-PK-IN-7 is a potent DNA-PK inhibitor (IC50= 1 nM) (WO2021104277A1, compound 5).

ATR-IN-7 is a potent inhibitor of ATR.