| Identification | Back Directory | [Name]
MS-402 | [CAS]
1672684-68-2 | [Synonyms]
MS-402
3-Chloro-N-(4-methoxyphenyl)-4-((2-methyl-3-oxocyclopent-1-en-1-yl)amino)benzamide
Benzamide, 3-chloro-N-(4-methoxyphenyl)-4-[(2-methyl-3-oxo-1-cyclopenten-1-yl)amino]- | [Molecular Formula]
C20H19ClN2O3 | [MDL Number]
MFCD32067932 | [MOL File]
1672684-68-2.mol | [Molecular Weight]
370.83 |
| Chemical Properties | Back Directory | [Boiling point ]
486.9±45.0 °C(Predicted) | [density ]
1.352±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (269.67 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.19±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice[1]. | [in vivo]
Reconstitution with na ve CD4+CD45RBhi cells isolated from spleen and lymph nodes of C57BL/6 mice, Rag1-/- mice begin losing weight after 4 week. MS402 (10 mg/kg; intraperitoneally twice a week for 3 weeks) shows much less weight loss[1]. | Animal Model: | C57BL/6 mice, Rag1-/- mice with T-cell transfer-induced colitis model[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneally twice a week for 3 weeks | | Result: | Showed much less weight loss. |
| [IC 50]
BRD4-BD1: 77 nM (Ki); BRD2-BD1: 83 nM (Ki); BRD3-BD1: 110 nM (Ki); BRD3-BD2: 200 nM (Ki); BRD2-BD2: 240 nM (Ki); BRD4-BD2: 718 nM (Ki) | [References]
[1] Cheung K, et al. BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice. Proc Natl Acad Sci U S A. 2017 Mar 14;114(11):2952-2957. DOI:10.1073/pnas.1615601114 |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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