CDK6 Activator

Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke.

INK4C-IN-2 is a p18^INK4C inhibitor. NK4C-IN-2 promotes hematopoietic stem cells (HSCs) division by inhibiting INK4C and activating CDK4/6, with an ED₅₀ of 5.21 nM. INK4C-IN-2 shows no cytotoxic to normal 32D cells, HSCs, leukemia cell lines and myeloma cell lines.

P18IN003 is a potent p18(INK4C) inhibitor andspecifically block the activity of p18 protein. P18IN003 has the potential to be aneffective chemical agent for therapeutic expansion of HSC.