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Chemical Structure : PIK-75
CAS No.: 372196-77-5
Catalog No.: PC-43460Not For Human Use, Lab Use Only.
PIK-75 is a potent, isoform-selective p110α inhibitor with IC50 of 0.3 nM, displays >100-fold selectivity over p110β, p110δ and PI3K C2b.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg (Free Sample) | $28 | In stock | |
| 25 mg | $128 | In stock | |
| 50 mg | $198 | In stock | |
| 100 mg | $328 | In stock | |
| 250 mg | Get quote |
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PIK-75 (PIK-75 hydrochloride) is a potent, isoform-selective p110α inhibitor with IC50 of 0.3 nM, displays >100-fold selectivity over p110β, p110δ and PI3K C2b.
PIK-75 blocks the phosphorylation of PKB induced by insulin on both Ser473 and Thr308 in CHO-IR cell (IC50=78 nM), inhibits PI3K activation associated with dramatic suppression of downstream signaling events, including AKT phosphorylation, IKK activation, and NF-kappaB transcription.
PIK-75 potently and dose dependently inhibits in vitro and in vivo production of TNF-alpha and IL-6, diminishes the induced expression of human endothelial cell adhesion molecules (E-selectin, ICAM-1, and VCAM-1), and blocks human monocyte-endothelial cell adhesion.
PIK-75 exhibits significant anti-tumor effectiveness in vivo.
| M.Wt | 488.74 | |
| Formula | C16H15BrClN5O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Benzenesulfonic acid, 2-methyl-5-nitro-, 2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide, hydrochloride (1:1) |
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1. Chaussade C, et al. Biochem J. 2007 Jun 15;404(3):449-58.
2. Dagia NM, et al. Am J Physiol Cell Physiol. 2010 Apr;298(4):C929-41.
3. Zheng Z, et al. Mol Pharmacol. 2011 Oct;80(4):657-64.
4. Hayakawa M, et al. Bioorg Med Chem. 2007 Sep 1;15(17):5837-44.
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