General description
A cell permeable, ATP-competitive and selective tolyl quinazolinone inhibitor of PI 3-Kδ (IC50 = 7 nM, 1300 nM, 85000 nM, and 740 nM for PI 3-Kδ PI 3-Kγ PI 3-Kα and PI 3-Kβ, respectively) in an enzymatic assay with an EC50 = 16 nM for PI 3-Kδ and 2.7 µM for PI 3-Kγ in a cell based assay. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs under superantigen stimulated conditions. This compound, at concentrations between 370 nM and 10 µM, leads to a dose-dependent decrease in E-selectin expression. Furthermore, it is not cytotoxic to HUVEC cells.
A cell permeable, ATP-competitive and selective tolyl quinazolinone inhibitor of PI 3-Kδ (IC50 = 7 nM, 1300 nM, 85000 nM, and 740 nM for PI 3-Kδ, PI 3-Kγ PI 3-Kα and PI 3-Kβ, respectively) in an enzymatic assay with an EC50 = 16 nM for PI 3-Kδ and 2.7 µM for PI 3-Kγ in a cell based assay. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs under superantigen stimulated conditions. This compound, at concentrations between 370 nM and 10 µM, leads to a dose-dependent decrease in E-selectin expression. Furthermore, it is not cytotoxic to HUVEC cells.
Warning
Toxicity: Regulatory Review (Z)
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
Molecular Weight: 451.48. Empirical Formula: C25H21N7O2. Quality Level: 100. Assay: >. 95% (HPLC). form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze. color: white. solubility: DMSO: 50 . mg/mL. shipped in: ambient. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.Shipping Information:
Dry Ice Surcharge & Ice Pack Shipments: $40
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- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 526559-5MG
- Temperature Control Device:
- Yes
