AS-605240

SKU: orb1305900

Description

AS-605240 is a potent and selective small molecule inhibitor of phosphoinositide 3-kinase gamma (PI3Kγ), exhibiting an IC50/Ki of 87.8 nM. It is a valuable research tool for studying the role of PI3Kγ in inflammation and immune cell signaling in both cellular and animal models of autoimmune and inflammatory diseases.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 648450-29-7
• MW: 257.27
• Purity: 99.06%
• Formula: C₁₂H₇N₃O₂S
• SMILES: C(C1=CC2=C(C=C1)N=CC=N2)=C3C(=O)NC(=O)S3
• Target: Autophagy,PI3K
• Solubility: DMSO:1 mg/mL (3.89 mM)

Bioactivity

• Target IC50:
  PI3Kα:60 nM|PI3Kβ:270 nM|PI3Kγ:87.8 nM|PI3Kδ:300 nM
• In Vivo:
  In bone marrow-derived monocytes, AS-605240 (1 μM) inhibits PKB phosphorylation induced by MCP-1 or CSF-1. In the synapses of the SC-CA1 region in mice, AS-605240 (100 nM) abrogates NMDAR LTD without affecting mGluR LTD and LTP. Furthermore, AS-605240 exhibits inhibition of PI3Kα/β/δ with IC50 values of 60, 270, and 300 nM, respectively. It also inhibits C5a-regulated PKB phosphorylation with an IC50 of 90 nM.
• In Vitro:
  In the obesity-induced diabetic ob/ob mouse model, AS-605240 at a dosage of 10 mg/kg reduces blood glucose levels, and significantly improves insulin sensitivity and glucose tolerance without affecting body weight, while a higher dosage of 30 mg/kg demonstrates enhanced efficacy with only minor impact on body weight. AS-605240 also reduces the quantity of ATMs and circulating levels of MCP-1. Furthermore, at a dosage of 50 mg/kg, AS-605240 offers protection against symptoms of αCII-induced arthritis and inhibits arthritis inflammation and damage in a collagen-induced arthritis mouse model. Additionally, AS-605240 decreases neutrophil chemotaxis in mice with RANTES-induced peritonitis (ED50: 9.1 mg/kg).
• Cell Research:
  After a 3-hour starvation in serum-free medium, Cells are pretreated with AS-605240 or DMSO for 30 min and stimulated for 5 min with 50 nM of C5a. PKB phosphorylation is monitored using phosphorylated Ser473 Akt-specific antibody and standard ELISA protocols. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AS605240, AS-605240, AS 605240, Autophagy, Inhibitor, inhibit, PI3Kδ, PI3Kγ, PI3Kβ, PI3Kα, PI3K, Phosphoinositide 3-kinase

Compound Identifiers

PubChem CID

24906273