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Cat. No. Product Name CAS No. Information
PC-63311

BRD0705

2056261-41-5

BRD0705 (BRD-0705) is a potent, paralog-selective GSK3α inhibitor with IC50 of 66 nM, 8-fold selectivity over GSK3β (IC50=515 nM); displays excellent selectivity in a penal of 311 kinases, the CDK family of CDK2, CDK3 and CDK5) are most potently inhibited with IC50 of 6.87, 9.74 and 9.20 uM (87-, 123-, and 116-fold selectivity relative to GSK3α); inhibits GSK3α kinase function, impairs GSK3α Tyr279 phosphorylation in a time- and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation, and does not stabilize β-catenin, induces myeloid differentiation and impairs colony formation in AML cells, with no apparent effect on normal hematopoietic cells; impairs leukemia initiation and prolongs survival in AML mouse models.

PC-63153

1-Azakenpaullone

676596-65-9

1-Azakenpaullone is an analog of kenpaullone and is a potent, selective GSK3β inhibitor with IC50 of 18 nM, weakly inhibits CDK1/cyclin B and CDK5/p25 (IC50=2.0 and 4.2 uM); stimulates the proliferation of human pancreatic islets and drives the differentiation of mouse embryonic stem cells.

PC-45724

Indirubin-3|-monoxime

160807-49-8

A potent GSK3β inhibitor with IC50 of 22 nM; prevents tau phosphorylation both in vitro and in vivo; also inhibits CDKs at higher concentrations, including Cdk1/cyclin B (IC50=180 nM), Cdk2/cyclin A (IC50~500 nM), Cdk2/cyclin E (IC50=250nM), Cdk4/cyclin D1 (IC50=3.3 uM) and Cdk5/p35 (IC50=100 nM); reversibly inhibits the proliferation of many cells types, arresting cycling in the G2/M phase.

PC-63357

MMBO

1005203-15-5 MMBO is a potent, highly selective, brain penetrant, orally active inhibitor of GSK-3 with IC50 of 37 and 53 nM for GSK-3α and GSK-3β, respectively; inhibits tau phosphorylation in primary neural cell culture and also in normal mouse brain, significantly decreases hippocampal tau phosphorylation at GSK-3 sites in transgenic mouse model of AD; suppresses tau pathology as assessed by AT8-immunoreactivity without affecting amyloid β pathology, significantly improves memory and cognitive deficits in AD models.
PC-63312

BRD3731

2056262-08-7 BRD3731 is a potent, selective GSK3β inhibitor with IC50 of 15 nM, 14-fold selectivity for GSK3β over GSK3α (IC50=215 nM); displays excellent selectivity in a penal of 311 kinases, displays reduced potency toward the GSK3β mutant (D133E) with IC50 of 53 nM; induces β-catenin stabilization starting at 20 uM in the HL-60 AML cell line, decreases β-catenin S33/37/T41 phosphorylation and induces β-catenin S675 phosphorylation, resulting in increased β-catenin.
PC-63239

Methyliodobikinin

1186336-04-8 Methyliodobikinin is a potent bikinin-like inhibitor targeting GSK3/Shaggy-like kinase, shows improved cell permeability, highly potent in vivo although it had lower activity in vitro; activates brassinosteroid (BR) signalling and mimic BR action, 3.4 times more active in vivo than bikinin.
PC-43377

CHIR-98014

252935-94-7 CHIR-98014 is a potent, selective glycogen synthase kinase 3 (GSK-3) withIC50 of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; shows less potent activities against 20 other protein kinases including Cdc2 and Erk2; causes GS stimulation in CHO-IR cells and rat hepatocytes, with EC50s of 106 nM and 107 nM, respectively; reduces the viability of ES-CCE cells with IC50 of 1.1 uM, results in a significant activation of the Wnt/beta-catenin pathway in ES-D3 cells combined with CHIR-99021; significantly reduces fasting hyperglycemia within and shows improved glucose disposal in diabetic and insulin-resistant db/db mice.

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