A potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM)

AS-041164 – 50 mg

Brand:
Cayman
CAS:
6318-41-8
Storage:
-20
UN-No:
Non-Hazardous - /

The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism.{17822} AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM).{17823} When tested at 1.0 μM, it shows little or no activity against 38 other common kinases.{17823} When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.{17823}  

 

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Description

A potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM); shows little or no activity against 38 other common kinases

Formal name: 5-(1,3-benzodioxol-5-ylmethylene)-2,4-thiazolidinedione

Synonyms: 

Molecular weight: 249.2

CAS: 6318-41-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Lipid Biochemistry|Glycerophospholipids|Phosphatidyl Inositol Kinases & Phosphatases

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