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526560

Sigma-Aldrich

PI 3-Kδ/γ Inhibitor XV, SW-14

The PI 3-Kδ/γ Inhibitor XV, SW-14 controls the biological activity of PI 3-Kδ/γ. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

PI 3-Kδ/γ Inhibitor XV, SW-14, 2-((4-amino-3-(3-fluoro-4-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one, PI 3-K Inhibitor XV

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About This Item

Empirical Formula (Hill Notation):
C28H22FN7O2
Molecular Weight:
507.52
UNSPSC Code:
12352200

Quality Level

Assay

>95% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

General description

A cell permeable, ATP competitive tolyl quinazolinone inhibitor of PI 3-Kδ/γ that displays 70-fold selectivity over PI 3-Kβ and 900-fold selectivity over PI 3-Kα in enzymatic assays with an IC50 = 9 nM for PI3Kδ and 21 nM for PI 3-Kγ and in a cell-based assay with an EC50 = 132 nM for PI 3-Kδ and 4.5 nM for PI 3-K γ. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs stimulated with lipopolysacharide. Additionally, TNFα production decreases dose-dependently in the same cell lines treated with 370 nM to 10 µM of compound. SW14 exhibits a stronger effect compared to that of PI 3-Kδ inhibition (SW30) or pan-PI 3-K inhibition with different anti-inflammatory profile. In contrast to PI 3-Kα/β it also shows very little anti-proliferative effects even at the highest dose tested (10 µM) in HUVEC culture only.

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Williams, O., et al. 2010. Chem Biol.17, 123.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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