361553

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.

• Synonyme(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
• Formule empirique (notation de Hill): C₁₈H₁₅N₅O₃
• Numéro CAS: 626604-39-5
• Poids moléculaire : 349.34
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: orange-red
• Solubilité: DMSO: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 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)
• Clé InChI: ZDEJZKULWCZIHL-UHFFFAOYSA-N

Description

Description générale

A cell-permeable azaindolylmaleimide compound that acts as a potent, specific, and ATP-competitive inhibitor of GSK-3β (K_i = 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; t_1/2 >100 min).

A cell-permeable, potent, specific, and ATP-competitive inhibitor of GSK-3β (K_i = 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; t_1/2 >100 min).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Gsk-3β

Product competes with ATP.

Reversible: no

Target K_i: 25 nM against GSK-3β

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1