Activators & Inhibitors

CDK9-IN-14 is a potent, high and low selective CDK9 inhibitor (IC50: 6.92 nM). CDK9-IN-14 is a strong inhibitor of MV-4-11 cells and in vivo tumour models with low toxicity and few side effects.

NR2F6 modulator-1 is a potent modulator of nuclear receptor subfamily 2, group F, member 6 (NR2F6). NR2F6 modulator-1 can be used to study immune regulation and modulation of tumour stem cell activity.

Pparδ agonist 7 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) belongs to the intranuclear receptor transcription factor superfamily and plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Tubulin aggregation-IN-19

Tubulin aggregation-IN-19 (compound 4) is a potent tubulin aggregation inhibitor that has shown potential in breast cancer and drug-resistant colon cancer.

KVI-020 is a selective, orally active blocker of the atrial potassium channel Kv1.5 (IC50: 480 nM). kVI-020 exhibits inhibition of hERG (IC50: 15100 nM). KVI-020 is a potent antiarrhythmic agent and can be used in the study of atrial fibrillation (AF).

Cap-dependent endonuclease-IN-6 (compound 13) is a Cap-dependent endonuclease (CEN) inhibitor that inhibits influenza virus.

HS-276 is a highly selective, orally active inhibitor of TAK1 (Ki: 2.5 nM). HS-276 significantly inhibits TAK1 (IC50: 8.25 nM), CLK2 (IC50: 29 nM), GCK (IC50: 22 nM), ULK2 (IC50: 63 nM), MAP4K5 (IC50. HS-276 can be used to study rheumatoid arthritis (RA).

Antileishmanial agent-10 (Compound 7h) is an antiprotozoal agent.

Antifungal agent 33 (compound 4e) is a potent antifungal agent with significant antifungal activity against Candida albicans (MIC: 16 μg/ml). (IC50: 0.19 μg/ml).