Activators & Inhibitors

NVS-BET-1 is a BET bromodomain inhibitor. NVS-BET-1 can regulate keratinocyte plasticity.

(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent inhibitor of CDK2, JAK2, and FLT3.

Anticancer agent 12 shows cytotoxic activity in malignant cells with no hepatotoxicity.

αβ-Tubulin-IN-1 is a potent and orally active inhibitor of αβ-Tubulin. αβ- Tubulin-IN-1 blocks cell cycle at G2/M phase and induces apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and metastasis. αβ-Tubulin-IN-1 exhibits significant antitumor efficacy.

Influenza A virus-IN-6 (compound 16j) is a potent and selective inhibitor of influenza A virus （IC 50= 3.88 μM, CC50= 36.64 μM). Influenza A virus-IN-6 exhibits anti-IAV activity with low cytotoxicity.

NF-κB-IN-5 (compound 4d) is an orally active NF-κB inhibitor. NF-κB-IN-5 interacts directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines, with IC 50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM for HCT116, U87-MG, HepG2, BGC823, PC9, respectively.

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

MAO-B-IN-7 is a potent and blood-brain barrier permeable MAO-B and AChE inhibitor. MAO-B-IN-7 exhibits IC50 s of 41 nM, 87 nM and 0.3 μM for human AChE, electric eel AChE and MAO-B, respectively. MAO-B-IN-7 effectively alleviates oxidative stress and neuroinflammatory damage.

Antibacterial agent 76 (compound 9) is a potent antibacterial agent.