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.

• Sinonimo/i: PI 3-Kα Inhibitor IV, 3-(4-Morpholinothieno[3,2-d]pyrimidin-2-yl)phenol, 2HCl, PI 3-K Inhibitor IV
• Formula empirica (notazione di Hill): C₁₆H₁₅N₃O₂S · 2HCl
• Numero CAS: 1188890-32-5
• Peso molecolare: 386.30
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: off-white
• Solubilità: DMSO: 10 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Irritant (B)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable