Potent, selective, cell permeable and ATP competitive GSK-3 inhibitor which is equally effective at GSK-3α as GSK-3β (IC50 = 34 nM for GSK-3α). Displays little activity at 24 other serine/threonine and tyrosine protein kinases.
SB 216763 is active in vivo.
The compound stimulates glycogen synthesis (EC50 = 3.6 µM), acts as a neuroprotectant and prevents neuronal cell death. It also shows anti-inflammatory and cardioprotective actions.
It is also widely used in stem cell research, for example:
Maintenance
Maintains mESCs (mouse embryonic stem cells) in a pluripotent state in the absence of LIF when cultured with MEFs
Restores INS-dependent differentiation of C2ind myoblasts
Differentiation
Promotes the conversion of human umbilical cord mesenchymal stem cells into neural precursors
Enhances chondrogenic differentiation of hWJ-MSCs
Increases neurogenesis of human neural progenitor cell differentiation
Promotes neural differentiation of CD117-positive hAFS cells towards neural progenitor cells
Proliferation
Promotes the proliferation of retinal stem cells
Solubility & Handling
Storage instructions
Room temperature
Solubility overview
Soluble in DMSO (75mM)
Handling
This compound is light sensitive; we therefore recommend protecting the solid material and solutions from exposure to light.
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References are publications that support the biological activity of the product
Glycogen synthase kinase 3 (GSK3)-inhibitor SB216763 promotes the conversion of human umbilical cord mesenchymal stem cells into neural precursors in adherent culture.
3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.
Gurrieri C et al (2010) J Pharmacol Exp Ther 332(3) : 785-94.
Y-27632 is a selective ROCK inhibitor. Frequently used 3D growth matrix component and for production of organoids. Also used when inducing neurons from fibroblasts. Manufactured to a high degree of optical purity.
Understanding purity and quality - a guide for life scientists
