Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 µM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMOs 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/pi-pi interactions with His470, Phe391, Tyr394, stabilizing SMOs inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma[1].
Molecular Weight:
449.37
Formula:
C23H26Cl2N2O3
Target:
Apoptosis,Caspase,Gli,Hedgehog,Smo
Application Notes:
MCE Product type: Reference compound
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