Activators & Inhibitors

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.

Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor. Sovesudil shows IC50 s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil can lower intraocular pressure (IOP) without inducing hyperemia.

BNS-22 is a catalytic inhibitor of DNA topoisomerase II ( TOP2 ). BNS-22 shows the IC 50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and shows anti-proliferative activity.

CDK2-IN-8 is a potent CDK2 inhibitor (IC50= 1.74 μM). CDK2-IN-8 exhibits antiproliferative activity. CDK2-IN-8 can be used for the research of melanoma.

Tubulin polymerization-IN-30 (compound 6e) is a potent inhibitor of Tubulin polymerization. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including HeLa, SGC-7901 and A549 with IC 50 values of 0.403, 2.16 and 2.21 μM.

XP5 is a potent, orally active HDAC6 inhibitor (IC50= 31 nM). XP5 inhibits the proliferation of various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM).

BDZ-g is a potent and selective antagonist of AMPA receptor. BDZ-g can be used for the research of various neurological disorders involving excessive activity of AMPA receptors.