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  3. MS402

MS402 

Cat. No.: HY-120000
Handling Instructions

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.

For research use only. We do not sell to patients.

MS402 Chemical Structure

MS402 Chemical Structure

CAS No. : 1672684-68-2

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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].

IC50 & Target[1]

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.
Molecular Weight

370.83

Formula

C₂₀H₁₉ClN₂O₃

CAS No.

1672684-68-2

SMILES

O=C(NC1=CC=C(OC)C=C1)C2=CC=C(NC3=C(C)C(CC3)=O)C(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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MS402
Cat. No.:
HY-120000
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