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PHA-408

Chemical Structure : PHA-408

CAS No.: 503555-55-3

PHA-408 (PHA-767408;PHA767408;PHA 408)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 560.03
Formula C29H27ClFN7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

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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