1. Epigenetics
  2. Epigenetic Reader Domain
  3. MS402

MS402 

Cat. No.: HY-120000 Purity: 98.98%
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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10 mM * 1 mL in DMSO USD 100 In-stock
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100 mg USD 750 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

MS402MS 402MS-402Epigenetic Reader DomainInhibitorinhibitorinhibit

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Product Name:
MS402
Cat. No.:
HY-120000
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