| Identification | Back Directory | [Name]
1H-Pyrazole-4-carboxamide, 5-amino-N-[[4-[[(3-cyclohexylpropyl)amino]carbonyl]phenyl]methyl]-1-phenyl- | [CAS]
2413286-32-3 | [Synonyms]
SR-318
1H-Pyrazole-4-carboxamide, 5-amino-N-[[4-[[(3-cyclohexylpropyl)amino]carbonyl]phenyl]methyl]-1-phenyl-
anti-inflammatory,SR 318,TNFR,anti-cancer,p38 MAPK,Inhibitor,inhibit,whole,TNF Receptor,SR-318,SR318,p38α/β,Tumor Necrosis Factor Receptor,blood | [Molecular Formula]
C27H33N5O2 | [MDL Number]
MFCD32693911 | [MOL File]
2413286-32-3.mol | [Molecular Weight]
459.58 |
| Chemical Properties | Back Directory | [Boiling point ]
732.0±60.0 °C(Predicted) | [density ]
1.24±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO:40.0(Max Conc. mg/mL);87.03(Max Conc. mM) | [form ]
A solid | [pka]
13.10±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity[1]. | [Biological Activity]
SR-318 is a potent and selective type-II inhibitor th at targets p38α/β in an inactive DFG-out conformation with good kinome selectivity (p38α/β IC50 = 5/39 nM by radiometric kinase assay). SR-318 selectively inhibits p38α/β by cell-based NanoBRET assay (IC50 = 3.7 nM/p38α10 nM/p38β0.91 μM/ZAK≥3 μM/DDR1DDR2KITMYLK4RSK4) and effectively blocks LPS-induced TNF-α release in human whole blood (IC50 = 283 nM). SR-321 is an inactive structural analog and the recommended negative control compound. | [IC 50]
p38α: 5 nM (IC50); p38β: 32 nM (IC50) | [References]
[1] R?hm S, et al. Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors. J Med Chem. 2019 Dec 12;62(23):10757-10782. DOI:10.1021/acs.jmedchem.9b01227 |
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