528106

PI 3-Kγ Inhibitor

The PI 3-Kγ Inhibitor, also referenced under CAS 648450-29-7, controls the biological activity of PI 3-Kγ. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): PI 3-Kγ Inhibitor, 5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione, PI 3-K Inhibitor I
• Empirical Formula (Hill Notation): C₁₂H₇N₃O₂S
• CAS Number: 648450-29-7
• Molecular Weight: 257.27
• MDL number: MFCD11100415
• UNSPSC Code: 12352202
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥90% (HPLC)
• form: solid
• potency: 7.8 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pink
• solubility: DMSO: 2.5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C12H7N3O2S/c16-11-10(18-12(17)15-11)6-7-1-2-8-9(5-7)14-4-3-13-8/h1-6H,(H,15,16,17)/b10-6-
• InChI key: SQWZFLMPDUSYGV-POHAHGRESA-N

Description

General description

A cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (K_i = 7.8 nM; IC₅₀ = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg^+/+ murine monocytes and in a human monocytic cell line THP-1 (IC₅₀ = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.

A cell-permeable, potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (K_i = 7.8 nM; IC₅₀ = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg^+/+ murine monocytes and in a human monocytic cell line THP-1 (IC₅₀ = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Phosphatidylinositol 3-kinase γ (PI 3-Kγ)

Product competes with ATP.

Reversible: no

Target IC₅₀: 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively; 181 nM in selectively blocking MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human mono

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Barber, D.F., et al. 2005. Nat. Med.11, 933.
Camps, M., et al. 2005. Nat. Med.11, 936.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable