Biological Activity
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 Vitro
No in vitro data are provided in the current product source. Contact us for further information.
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.
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)
References & source
[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.
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.