GSK-3 Inhibitor IX (BIO)

产品描述
GSK-3 inhibitor IX (BIO) is a potent, selective, cell-permeable, ATP-competitive and reversible inhibitor of GSK-3α (glycogen synthase kinase-3α) and GSK-3β (lycogen synthase kinase-3β) (IC50 = 5nM for GSK-3β). [1]GSK3 (glycogen synthase kinase-3) is a serine/threonine protein kinase which contributes to cell survival, diabetes, insulin resistance and Alzheimer's diseases. It is contributed to β-catenin/Wnt signaling pathway.BIO facilitated the proliferation in mammalian cardiomyocytes by increasing the proliferation potential of cardiomyocytes. It induced S phase entry and beta-catenin activity in neonatal cardiomyocyte. [3] BIO also activated Wnt signaling and involved in maintaining pluripotency in human and mouse ESCs (embryonic stem cells). [2] In Cos-1 cells treated with 5 μm BIO for 24 hours, phosphorylation of β-catenin was inhibited on GSK-3 specific sites. In cell line deficient for AhR or ARNT, 10 μm BIO treatment for 24 hours showed its effect is through a direct and AhR- independent pathway.[1]In vivo study showed BIO activated maternal Wnt signaling pathway in Xenopus embryos. It caused a hyper dorso-anteriorization at the expense of trunk and tail in a dose-response manner. It also activated the dorsal genes (siamois and chordin) ectopically. [1]References:[1] Meijer L, Skaltsounis AL, Magiatis P, Polychronopoulos P, Knockaert M, Leost M, Ryan XP, Vonica CA, Brivanlou A, Dajani R, Crovace C, Tarricone C, Musacchio A, Roe SM, Pearl L, Greengard P. GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chem Biol. 2003 Dec;10(12):1255-66.[2] Sato N, Meijer L, Skaltsounis L, Greengard P, Brivanlou AH. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nat Med. 2004 Jan;10(1):55-63.[3] Tseng AS, Engel FB, Keating MT. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem Biol. 2006 Sep;13(9):957-63.

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