1. Epigenetics
  2. Histone Methyltransferase
  3. BRD9539

BRD9539 

Cat. No.: HY-15647 Purity: 99.78%
Handling Instructions

BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1.

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

BRD9539 Chemical Structure

BRD9539 Chemical Structure

CAS No. : 1374601-41-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 552 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE BRD9539

    BRD9539 purchased from MCE. Usage Cited in: Theranostics. 2018 Apr 15;8(10):2884-2895.

    Plk1 levels are decreased companied with p53K373me2 decline in HCT116 cells treated with BRD9539.
    • Biological Activity

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    Description

    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1[1].

    IC50 & Target[1]

    G9a

    6.3 μM (IC50)

    PRC2

     

    In Vitro

    BRD9539 decreases ATP levels in a dose-dependent manner in HeLa cells[1].
    BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration. However, BRD9539 has no activity in cell-based assays, presumably due to impaired cell permeability compared to that of BRD4770. In addition, the activities of 16 other chromatin-modifying enzymes and 100 kinases involved in cell-cycle regulation and cancer cell biology are tested for activity in the presence of 5 or 10 μM BRD9539; no activity is seen in any of these assays[1].

    Molecular Weight

    399.44

    Formula

    C₂₄H₂₁N₃O₃

    CAS No.

    1374601-41-8

    SMILES

    O=C(C1=CC=C2C(N=C(NC(C3=CC=CC=C3)=O)N2CCCC4=CC=CC=C4)=C1)O

    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
    Solvent & Solubility
    In Vitro: 

    DMSO : 16.67 mg/mL (41.73 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5035 mL 12.5175 mL 25.0350 mL
    5 mM 0.5007 mL 2.5035 mL 5.0070 mL
    10 mM 0.2504 mL 1.2518 mL 2.5035 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: 1.67 mg/mL (4.18 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: ≥ 1.67 mg/mL (4.18 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    BRD9539BRD 9539BRD-9539Histone MethyltransferaseG9achromatinhistonesEHMT2H3K9senescentPRC2Inhibitorinhibitorinhibit

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    Product name:
    BRD9539
    Cat. No.:
    HY-15647
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