MS-402| BET BrD inhibitor|CAS 1672684-68-2

Cas No.:	1672684-68-2
Chemical Name:	3-chloro-N-(4-methoxyphenyl)-4-((2-methyl-3-oxocyclopent-1-en-1-yl)amino)benzamide
Synonyms:	MS402;MS 402
SMILES:	O=C(NC1=CC=C(OC)C=C1)C2=CC=C(NC3=C(C)C(CC3)=O)C(Cl)=C2
Formula:	C₂₀H₁₉ClN₂O₃
M.Wt:	370.83
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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.

Description:	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].
Target:	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)
In Vivo:	Reconstitution with naïve 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.
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.

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