Molecular structure of AS-605240, CAS Number: 648450-29-7
AS-605240 (CAS 648450-29-7)
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Alternate Names:
5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione
Application:
AS-605240 is an inhibitor of PI 3-kinase γ
CAS Number:
648450-29-7
Purity:
≥95%
Molecular Weight:
257.27
Molecular Formula:
C12H7N3O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
PI 3-Kgamma Inhibitor is a cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of PI 3-kinase gamma (PI 3-Kgamma) (Ki = 7.8 nM IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-gamma, alpha, beta and delta-isoforms, respectively). PI 3-Kgamma Inhibitor does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 muM. It 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). PI 3-Kgamma Inhibitor has also been shown to exhibit efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.
AS-605240 (CAS 648450-29-7) References
- Effects of PI3Kgamma inhibition using AS-605240 in acute myocardial infarction. | Seropian, IM., et al. 2010. Circ Res. 107: e5; author reply e6-7. PMID: 20651289
- Pharmacologic inhibition of phosphoinositide 3-kinase gamma (PI3Kγ) promotes infarct resorption and prevents adverse cardiac remodeling after myocardial infarction in mice. | Seropian, IM., et al. 2010. J Cardiovasc Pharmacol. 56: 651-8. PMID: 20881611
- PI3K-γ inhibition ameliorates acute lung injury through regulation of IκBα/NF-κB pathway and innate immune responses. | Kim, DI., et al. 2012. J Clin Immunol. 32: 340-51. PMID: 22198681
- Critical role for phosphoinositide 3-kinase gamma in parasite invasion and disease progression of cutaneous leishmaniasis. | Cummings, HE., et al. 2012. Proc Natl Acad Sci U S A. 109: 1251-6. PMID: 22232690
- PI3Kγ activation is required for LPS-induced reactive oxygen species generation in respiratory epithelial cells. | Kim, HJ., et al. 2012. Inflamm Res. 61: 1265-72. PMID: 22825625
- PI3K-γ inhibitors in the therapeutic intervention of diseases caused by obligate intracellular pathogens. | Oghumu, S. and Satoskar, AR. 2013. Commun Integr Biol. 6: e23360. PMID: 23749323
- Possible targets for nonimmunosuppressive therapy of Graves' orbitopathy. | Zhang, L., et al. 2014. J Clin Endocrinol Metab. 99: E1183-90. PMID: 24758182
- Targeting PI3Kγ activity decreases vascular trauma-induced intimal hyperplasia through modulation of the Th1 response. | Smirnova, NF., et al. 2014. J Exp Med. 211: 1779-92. PMID: 25073791
- α-Tocopheryl Phosphate Induces VEGF Expression via CD36/PI3Kγ in THP-1 Monocytes. | Zingg, JM., et al. 2017. J Cell Biochem. 118: 1855-1867. PMID: 28059487
- Comprehensive analysis of T cell leukemia signals reveals heterogeneity in the PI3 kinase-Akt pathway and limitations of PI3 kinase inhibitors as monotherapy. | Ksionda, O., et al. 2018. PLoS One. 13: e0193849. PMID: 29799846
- Screening Novel Drug Candidates for Kidney Renal Clear Cell Carcinoma Treatment: A Study on Differentially Expressed Genes through the Connectivity Map Database. | Gao, B., et al. 2021. Kidney Blood Press Res. 46: 702-713. PMID: 34818247
- BTK and PI3K Inhibitors Reveal Synergistic Inhibitory Anti-Tumoral Effects in Canine Diffuse Large B-Cell Lymphoma Cells. | Kong, W., et al. 2021. Int J Mol Sci. 22: PMID: 34884478
- Phosphoinositide 3 Kinase γ Plays a Critical Role in Acute Kidney Injury. | Jin, X., et al. 2022. Cells. 11: PMID: 35269396
- Inhibition of phosphoinositide‑3 kinases γ/δ ameliorates pulmonary granuloma by rescuing Treg function in a sarcoidosis model. | Zhang, X., et al. 2023. Exp Ther Med. 25: 225. PMID: 37123205
- AS-605240 Blunts Osteoporosis by Inhibition of Bone Resorption. | Sun, J., et al. 2023. Drug Des Devel Ther. 17: 1275-1288. PMID: 37138583
Inhibitor of:
PI 3-kinase p110 alpha, PI 3-kinase p110 beta, PI 3-kinase p110 delta, and PI 3-kinase p110 gamma.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AS-605240, 1 mg | sc-221272 | 1 mg | $23.00 | |||
AS-605240, 5 mg | sc-221272A | 5 mg | $80.00 |