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Description: MLS2052 (also known as BIO, GSK3 Inhibitor IX, 6-Bromoindirubin-3'-oxime) is a novel, potent, cell-permeable bis-indolo and specific inhibitor of GSK-3 (glycogen synthase kinase-3) with potential antitumor activity. It inhibits GSK-3 with an IC50 of 5 nM for GSK-3alpha/beta in a cell-free assay, and exhibits > 16-fold selectivity over CDK5. It showed potent antiproliferative activity in vitro and suppressed melanoma tumor growth in a mouse xenograft model.
References:Chem Biol. 2003 Dec; 10(12):1255-66; Nat Med. 2004 Jan; 10(1):55-63; Cancer Res. 2011 Jun 1; 71(11):3972-9.
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