Creative Biolabs

SB 216763 [GSK-3 Inhibitor]

[CAT#: MOD2005ZP129]

A highly potent, selective cell permeable GSK-3 inhibitor

Target:
GSK-3

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Description
Efficient, selective, cell-penetrating and ATP-competitive GSK-3 inhibitors have the same effect on GSK-3α as GSK-3β (for GSK-3α, IC50 = 34 nM). It has little activity on the other 24 serine/threonine and tyrosine protein kinases. SB 216763 is The modulator shows activity in vivo. The compound stimulates glycogen synthesis (EC50 = 3.6 µM), acts as a neuroprotective agent and prevents neuronal cell death.It also exhibits anti-inflammatory and cardioprotective effects.

It also widely used in stem cell research, for example:

Maintenance
When cultured with MEF, maintain mESC (mouse embryonic stem cells) in a pluripotent state without LIF
Restore INS-dependent differentiation of C2ind myoblasts

Differentiation
Promote the transformation of human umbilical cord mesenchymal stem cells into neural precursors
Enhance hWJ-MSC cartilage formation and differentiation
Neurogenesis that increases differentiation of human neural progenitor cells
Promote the neural differentiation of CD117 positive hAFS cells into neural progenitor cells

Proliferation
Promote the proliferation of retinal stem cells
Synonyms
SB-216763
Chemical Name
3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
SB-216763 (10-20 µM) induces β-catenin-mediated transcription in HEK293 cells in a dose-dependent manner. SB-216763 (10, 15 and 20 µM) can maintain mESC with pluripotent morphology in long-term culture. SB-216763 (10 µM) can maintain the J1 mESC in a pluripotent state for more than one month [1]. SB-216763 inhibits GSK-3 with an IC50 of 34 nM [2]. SB-216763 is also effective in inhibiting human GSK-3α and GSK-3β [3].
Reference
[1]. Gurrieri, et al. 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. J.Pharmacol.Exp.Ther.2010

[2]. Wang M, et al. The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3).Bioorg Med Chem Lett. 2011 Jan 1;21(1):245-9. Epub 2010 Nov 11.

[3]. Coghlan MP, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803.
Assay Description
SB216763 (20 mg/kg, i.v.) significantly improved the survival rate of BLM-treated mice. Compared with BLM-treated mice, mice randomly receiving BLM plus SB216763 showed a significant reduction. SB216763 (20 mg/kg, i.v.) reduces the degree of alveolitis caused by BLM [1]. SB 216763 (0.2 mg/kg, i.v.) or 17β-E100 or Geni100 can reverse the upper limit effect, because these drugs can significantly reduce the infarct size when the rabbit's heart is subjected to 30 minutes of CAO [2].
References
[1]. Gurrieri, et al. 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. J.Pharmacol.Exp.Ther.2010

[2]. The ceiling effect of pharmacological postconditioning with the phytoestrogen genistein is reversed by the GSK3beta inhibitor SB 216763 [3-(2,4-dichlorophenyl)-4(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione] through mitochondrial ATP-dependent potassium channel opening.
Molecular Weight
371.22
Chemical Formula
C19H12Cl2N2O2
SMILES
CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl
Solubility
Soluble in DMSO (75mM)
IC50
GSK-3α-34.3 nM (IC50); GSK-3β-34.3 nM (IC50)
CAS NO.
280744-09-4
PubChem Substance ID
176158
Purity
>98%
Storage
Room temperature
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -65°C for several months.
Research Use Only
For research use only
Target
GSK-3
Official Name
GSK-3
Full Name
Glycogen synthase kinase 3
Alternative Names
Glycogen Synthase Kinase 3; GSK3; Glycogen Synthase Kinase-3
Gene ID
2932(Human); 56637(Mouse); 84027(Rat)
Uniprot ID
P49841(Human); Q9WV60(Mouse); P18266(Rat)
For Research Use Only. Not For Clinical Use.
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