PI 3-K Inhibitor XVIII

A PI 3-K p110β-derived Gβγ-binding peptide (aa 514-537 in p110β C2-helical linker region) is made cell-permeable via N-myristoylation and prevents Gβγ-, but not RTK-, mediated p110β activation both in cell-free immune complex activation assays (complete inhibition by 1 µM peptide) and in cultures (complete inhibition of pAKT T308 by 30 min 30 µM peptide treatment of p110β/p85/Akt/Gβγ-transfected HEK 293E cells) without affecting basal p110β activity, p110β-Rab5 interaction, nor Gαβ-dependent activation of adenylyl cyclase or p101-p110γ dimer. The ATP-competitive p110β inhibitior TGX-221 (Cat. No. 528113) can be used in conjunction for studying Gβγ-dependency of p110β-mediated cellular functions.

An N-myristoylated cell-permeable PI 3-K p110β-derived Gβγ-binding peptide (aa 514-537 in p110β C2-helical linker region) that prevents Gβγ-, but not RTK-, mediated p100β activation both in cell-free assays (1 µM) and in cultures (30 µM in p110β/p85/Akt/Gβγ-transfected HEK 293E cells) without affecting basal p100β activity, p110β-Rab5 interaction, nor Gβγ-dependent activation of adenylyl cyclase or p101-p110γ dimer. The ATP-competitive p110β inhibitior TGX-221 (Cat. No. 528113) can be used in conjunction for studying Gβγ dependency of p110β-mediated cellular functions.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
Gβγ subunit of G-proteins

Supplied as a trifluoroacetate salt.

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

Dbouk, H.A., et al. 2012. Sci. Signal. 5, ra89.

N-Myr-Lys-Ala-Ala-Glu-Ile-Ala-Ser-Ser-Asp-Ser-Ala-Asn-Val-Ser-Ser-Arg-Gly-Gly-Lys-Lys-Phe-Leu-Pro-Val-NH₂

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

Toxicity: Standard Handling (A)