Chemical Structure : PHA-408
CAS No.: 503555-55-3
货号: PC-61094Not For Human Use, Lab Use Only.
PHA-408 (PHA-767408) is a potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1.
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PHA-408 (PHA-767408) is a potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1.
PHA-408 inhibits LPS-induces TNF-α producton in PBMCs and HWB with IC50 of 20-30 nM, prevents IL-1β-induced IκBα phosphorylation in RASFs while sparing the JNK and p38 MAPK pathways and has no effect on IKK-2 phosphorylation.
PHA-408 demonstrates target-specific anti-inflammatory activities in in vivo model of airway inflammation.
分子量 | 560.03 | |
分子式 | C29H27ClFN7O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
8-[[[5-Chloro-2-(4-methyl-1-piperazinyl)-4-pyridinyl]carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydro-1H-benz[g]indazole-3-carboxamide |
1. Mbalaviele G, et al. J Pharmacol Exp Ther. 2009 Apr;329(1):14-25.
2. Sommers CD, et al. J Pharmacol Exp Ther. 2009 Aug;330(2):377-88.
3. Xie J, et al. Bioorg Med Chem. 2011 Feb 1;19(3):1242-55.
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