Activators & Inhibitors

HDAC-IN-31 is a selective, potent, orally active HDAC inhibitor that acts on HDAC1 (IC50: 84.90 nM), HDAC2 (IC50: 168.0 nM), HDAC3 (IC50: 442.7 nM), HDAC8 (IC50>10000 nM). HDAC-IN-31 has good anti-tumour effects. HDAC-IN-31 has shown potential research value in diffuse large B-cell lymphoma.

MK2-IN-4 is a MAPKAPK2 (MK2) inhibitor (IC50: 45 nM). MK2-IN-4 can be used in cancer, inflammation and immunology studies.

Antioxidant agent-5 (compound D-6) is a potent antioxidant. antioxidant agent-5 inhibits oxLDL-induced increases in ROS levels and NF-κB nuclear translocation. antioxidant agent-5 inhibits oxLDL (oxidized LDL)-induced apoptosis (VECs). Antioxidant agent-5 activates the Nrf2/HO-1 antioxidant pathway and exhibits protective activity against oxLDL-induced endothelial damage.

CDK8-IN-6 (compound 9) is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) (Kd: 13 nM), CDK8-IN-6 showed potential research value in AML cancers.

EGFR-IN-49 is a potent and selective EGFR inhibitor that acts on EGFRT790M (IC50: 65.0 nM) and EGFRT790M/L858R (IC50: 13.6 nM). EGFR-IN-49 induces apoptosis in a dose-dependent manner.

JAK3-IN-12 (compound 15k) is a potent inhibitor of JAK3 (IC50: 9.5 nM) and can be used in the study of rheumatoid arthritis.

HBV-IN-24 (compound (2 S, 6S)-1a) is a potent inhibitor of HBV. HBV-IN-24 is a strong inhibitor of HBV DNA (EC50: 0.6 nM), HBsAg (EC50: 0.6 nM) and HBeAg (EC50: 4.6 nM). antiviral effect and was able to improve neurotoxicity.

ALK5-IN-33 (Compound EX-10) is an orally active, selective inhibitor of ALK-5 (IC50 ≤ 10 nM).

ALK5-IN-34 is a selective, orally active inhibitor of activin receptor-like kinase (ALK), which inhibits the activity of activin receptor-like kinase (IC50 ≤ 10 nM) and also inhibits tumour growth.