2. Epigenetics
    Anti-infection
  3. Epigenetic Reader Domain
    HIV
  4. MS417

MS417  (Synonyms: GTPL7512)

Cat. No.: HY-111139 Purity: 99.87%
COA Handling Instructions

MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).

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

MS417 Chemical Structure

MS417 Chemical Structure

CAS No. : 916489-36-6

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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).

IC50 & Target

IC50: 30 nM (BRD4-BD1), 46 nM (BRD4-BD2), 32.7 μM (CBP BRD)[1]
Kd: 36.1 nM (BRD4-BD1), 25.4 nM (BRD4-BD2)[1]
In Vitro

MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with less selectivity at CBP BrD (IC50, 32.7 μM). MS417 effectively blocks BRD4 binding to NF-κB, almost completely suppresses TNFα-induced NF-κB transcription activation in human embryonic kidney 293T cells at 1 μM and also reduces NF-κB p65 acetylation in the HIV-infected RTECs. MS417 (1 μM) modulation of gene transcription in HIV-infected human primary renal tubular epithelial cells. In addition, MS417 suppresses NF-κB-targeted cytokines and chemokines[1].

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

MS417 (0.08 mg/kg) markedly improves renal function, reduces proteinuria and decreases glomerulosclerosis, tubular injury, and infiltration of inflammatory cells in the kidney of Tg26 mice[1].

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

414.91

Appearance

Solid

Formula

C20H19ClN4O2S
CAS No.
SMILES

O=C(OC)C[[email protected]]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
In Vitro: 

Ethanol : 50 mg/mL (120.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4102 mL 12.0508 mL 24.1016 mL
5 mM 0.4820 mL 2.4102 mL 4.8203 mL
10 mM 0.2410 mL 1.2051 mL 2.4102 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.87%

COA (258 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
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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.

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

MS417916489-36-6GTPL7512MS 417MS-417GTPL 7512GTPL-7512Epigenetic Reader DomainHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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