| Identification | Back Directory | [Name]
Benzamide, N-cyclopropyl-4-methyl-3-[3-[[1-methyl-1-[2-[2-(methylamino)ethoxy]phenyl]ethyl]amino]-2-oxo-1(2H)-pyrazinyl]- | [CAS]
1095003-80-7 | [Synonyms]
p38α inhibitor 2
Benzamide, N-cyclopropyl-4-methyl-3-[3-[[1-methyl-1-[2-[2-(methylamino)ethoxy]phenyl]ethyl]amino]-2-oxo-1(2H)-pyrazinyl]- | [Molecular Formula]
C27H33N5O3 | [MOL File]
1095003-80-7.mol | [Molecular Weight]
475.58 |
| Chemical Properties | Back Directory | [density ]
1.23±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (525.67 mM; Need ultrasonic) | [form ]
Solid | [pka]
14.72±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets[1]. | [Biological Activity]
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets[1]. | [IC 50]
p38α MAPK: 9.6 (pIC50) | [References]
[1]. Raubo P, et al. The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors [published online ahead of print, 2020 Jul 15]. Bioorg Med Chem Lett. 2020;30(18):127412. |
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