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GSK-3β Inhibitor XI

The GSK-3β Inhibitor XI, also referenced under CAS 626604-39-5, controls the biological activity of GSK-3β. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

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Synonym(s):
GSK-3β Inhibitor XI, 3-(1-(3-Hydroxypropyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-4-pyrazin-2-yl-pyrrole-2,5-dione, 7AIPM
Empirical Formula (Hill Notation):
C18H15N5O3
CAS Number:
Molecular Weight:
349.34

Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange-red

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C18H15N5O3/c24-8-2-7-23-10-12(11-3-1-4-21-16(11)23)14-15(18(26)22-17(14)25)13-9-19-5-6-20-13/h1,3-6,9-10,24H,2,7-8H2,(H,22,25,26)

InChI key

ZDEJZKULWCZIHL-UHFFFAOYSA-N

General description

A cell-permeable azaindolylmaleimide compound that acts as a potent, specific, and ATP-competitive inhibitor of GSK-3β (Ki = 25 nM) and minimally inhibits a panel of 79 commonly studied protein kinases, including several PKC isozymes. Shown to increase intracellular glycogen synthase activity in HEK293 cells with an EC50 of 32 nM and demonstrate metabolic stability in human liver microsomes (HLM; t1/2 >100 min).
A cell-permeable, potent, specific, and ATP-competitive inhibitor of GSK-3β (Ki = 25 nM) that exhibits minimal inhibition against a panel of 79 commonly studied protein kinases, including several PKC isozymes. Shown to increase intracellular glycogen synthase activity in HEK293 cells (EC50 = 32 nM) and demonstrate metabolic stability in human liver microsomes (HLM; t1/2 >100 min).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Gsk-3β
Product competes with ATP.
Reversible: no
Target Ki: 25 nM against GSK-3β

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Justman, Q.A., et al. 2009. Science324, 509.
O′Neill, D.J., et al. 2004. Bioorg. Med. Chem.12, 3167.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1


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