PIK-75 is an inhibitor of p110α PI3K that exhibits anticancer and anti-inflammatory activities. In breast cancer cells, PIK-75 inhibits cell motility and adhesion in vitro and in vivo. PIK-75 also enhances glucose-induced insulin secretion. Additionally, PIK-75 inhibits production of TNF-α, IL-6, E-selectin, ICAM-1, and VCAM-1, preventing monocyte-endothelial cell adhesion.
| Cas No. | 372196-77-5 |
|---|---|
| Purity | ≥98% |
| Formula | C16H14BrN5O4S • HCl |
| Formula Wt. | 488.74 |
| IUPAC Name | N-[(E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide;hydrochloride |
| Synonym | PIK-75 HCl |
| Melting Point | 221-223°C |
| Solubility | Soluble in DMSO, DMF |
| Appearance | Yellow Powder |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| Info Sheet | P3540 Info Sheet PDF |
|---|
Buchanan CM, Dickson JM, Lee WJ, et al. Oncogenic mutations of p110α isoform of PI 3-kinase upregulate its protein kinase activity. PLoS One. 2013 Aug 1;8(8):e71337. PMID: 23936502.
Aoyagi K, Ohara-Imaizumi M, Nishiwaki C, et al. Acute inhibition of PI3K-PDK1-Akt pathway potentiates insulin secretion through upregulation of newcomer granule fusions in pancreatic β-cells. PLoS One. 2012;7(10):e47381. PMID: 23077605.
Smirnova T, Zhou ZN, Flinn RJ, et al. Phosphoinositide 3-kinase signaling is critical for ErbB3-driven breast cancer cell motility and metastasis. Oncogene. 2012 Feb 9;31(6):706-15. PMID: 21725367.
Dagia NM, Agarwal G, Kamath DV, et al. A preferential p110alpha/gamma PI3K inhibitor attenuates experimental inflammation by suppressing the production of proinflammatory mediators in a NF-kappaB-dependent manner. Am J Physiol Cell Physiol. 2010 Apr;298(4):C929-41. PMID: 20089935.
