Activators & Inhibitors

AMPK activator 6 (Compound GC) activates the AMPK pathway and reduces lipid content in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase of total cholesterol (TC), low-density lipoprotein-C (LDL-C), triglyceride (TG), and other biochemical indices in blood serum. AMPK activator 6 has research value in non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome .

Lorpucitinib (JNJ-64251330) is an orally available, selective and potent JAK kinase inhibitor for the study of inflammatory and gastrointestinal disorders associated with Janus kinase (JAK) signaling.

D4R antagonist-2 is a potent and selective D4R antagonist (IC50= 6.52 μM). D4R antagonist-2 displays favorable in vitro PK parameters and exhibits good brain penetration. D4R antagonist-2 has the research potential in Parkinson’s disease.

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.