528111

PI 3-Kα Inhibitor IV

The PI 3-Kα Inhibitor IV, also referenced under CAS 1188890-32-5, controls the biological activity of PI 3-Kα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : PI 3-Kα Inhibitor IV, 3-(4-Morpholinothieno[3,2-d]pyrimidin-2-yl)phenol, 2HCl, PI 3-K Inhibitor IV
• Formule empirique (notation de Hill): C₁₆H₁₅N₃O₂S · 2HCl
• Numéro CAS: 1188890-32-5
• Poids moléculaire : 386.30
• 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; desiccated (hygroscopic); protect from light
• Couleur: off-white
• Solubilité: DMSO: 10 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C

Description

Description générale

A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-Ks (IC₅₀ = 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC₅₀ ≥ 3.4 µM for Cdk2/E, KDR, PKA, and PKCα). Shown to inhibit cell proliferation (IC₅₀ = 580 nM) and serum-stimulated Akt phosphorylation (IC₅₀<3 µM) in A375 melanoma cells.

A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-kinases (IC₅₀ = 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC₅₀ ≥3.4 µM for Cdk2/E, KDR, PKA, and PKCα). Shown to inhibit cell proliferation (IC₅₀ = 580 nM) and serum-stimulated Akt phosphorylation (IC₅₀<3 µM) in A375 melanoma cells.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
PI 3-Kα

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Hayakawa, M., et al. 2006. Bioorg. Med. Chem.14, 6847.

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
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable