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MS402 is a novel BD1-selective BET BrD inhibitor, inhibiting primarily Th17 cell differentiation with a little or almost no effect on Th1 or Th2 and Treg cells. MS402 has Ki values 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 preferentially renders Brd4 binding to Th17 signature gene loci over those of housekeeping genes and reduces Brd4 recruitment of p-TEFb to phosphorylate and activate RNA polymerase II for transcription elongation. MS402 prevents and ameliorates T-cell transfer-induced colitis in mice by blocking Th17 cell overdevelopment.
| Cell Experiment | |
|---|---|
| Cell lines | murine primary naive CD4+ T cells |
| Preparation method | To study the role of BET proteins in Th cell differentiation we isolated murine primary naïve CD4+ T cells from mouse spleen and lymph nodes and treated them with IL-12, IL-4 plus α-IL-12, TGF-β plus IL-6, or TGF-β plus IL-2, respectively, to promote Th1, Th2, Th17, or Treg linage-specific differentiation over 3.5 d with or without MS402 added daily to cell culture (Fig. 2A). Strikingly, as shown by flow cytometry analysis, MS402, in a dose-dependent manner, inhibited IL-17 release from 18.6 to 8.0% in the Th17 polarizing condition and to a lesser extent IFN-γ production from 49.7 to 38.6% in the Th1 condition; it had little, if any, effect on IL-4 and Foxp3 expression during Th2 and Treg cell differentiation, respectively (Fig. 2B). MS402 did not affect T-cell proliferation as assessed in a carboxy-fluorescein succinimidyl ester dilution assay (Fig. S2A). |
| Concentrations | 100 nM or 500 nM |
| Incubation time | 3.5 d |
| Animal Experiment | |
|---|---|
| Animal models | Rag1−/− mice |
| Formulation | - |
| Dosages | 10 mg/kg |
| Administration | i.p. injections twice a week for 3 wk |
| Molecular Weight | 370.83 |
| Formula | C20H19ClN2O3 |
| CAS Number | 1672684-68-2 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Epigenetic Reader Domain Products |
|---|
| RVX-208
Apabetalone (RVX-208) is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2. |
| I-BET151
I-BET151 (GSK1210151A) is an inhibitor of the BET family with IC50 of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively. |
| (+)-JQ1
(+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway. |
| I-BET-762
I-BET-762 (GSK525762) is a selective small molecule BET inhibitor. |
| CPI-0610
CPI-0610 is a novel BET protein bromodomain inhibitor. |
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