2. Epigenetics
  3. Epigenetic Reader Domain
  4. MS402

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.

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MS402 Chemical Structure

MS402 Chemical Structure

CAS No. : 1672684-68-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

MS402 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MS402

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (269.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6967 mL 13.4833 mL 26.9665 mL
5 mM 0.5393 mL 2.6967 mL 5.3933 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.74 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6967 mL 13.4833 mL 26.9665 mL 67.4163 mL
5 mM 0.5393 mL 2.6967 mL 5.3933 mL 13.4833 mL
10 mM 0.2697 mL 1.3483 mL 2.6967 mL 6.7416 mL
15 mM 0.1798 mL 0.8989 mL 1.7978 mL 4.4944 mL
20 mM 0.1348 mL 0.6742 mL 1.3483 mL 3.3708 mL
25 mM 0.1079 mL 0.5393 mL 1.0787 mL 2.6967 mL
30 mM 0.0899 mL 0.4494 mL 0.8989 mL 2.2472 mL
40 mM 0.0674 mL 0.3371 mL 0.6742 mL 1.6854 mL
50 mM 0.0539 mL 0.2697 mL 0.5393 mL 1.3483 mL
60 mM 0.0449 mL 0.2247 mL 0.4494 mL 1.1236 mL
80 mM 0.0337 mL 0.1685 mL 0.3371 mL 0.8427 mL
100 mM 0.0270 mL 0.1348 mL 0.2697 mL 0.6742 mL
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MS402 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS4021672684-68-2MS 402MS-402Epigenetic Reader DomainInhibitorinhibitorinhibit

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