An inhibitor of EHMT2/G9a and PRC2 in enzyme assays
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BRD9539

Item No. 11788

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(benzoylamino)-1-(3-phenylpropyl)-1H-benzimidazole-5-carboxylic acid
CAS Number
1374601-41-8
Molecular Formula
C24H21N3O3
Formula Weight
399.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.5 mg/ml
λmax
205, 230, 270, 329 nm
SMILES
O=C(C1=CC=CC=C1)NC2=NC3=CC(C(O)=O)=CC=C3N2CCCC4=CC=CC=C4
InChi Code
InChI=1S/C24H21N3O3/c28-22(18-11-5-2-6-12-18)26-24-25-20-16-19(23(29)30)13-14-21(20)27(24)15-7-10-17-8-3-1-4-9-17/h1-6,8-9,11-14,16H,7,10,15H2,(H,29,30)(H,25,26,28)
InChi Key
WPXMEOBILYVKBC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $36

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    1 mg

    $53

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    5 mg

    $108

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    10 mg

    $195

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    Product Description

    BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 µM.1 It inhibits polycomb repressive complex 2 (PRC2) to a similar extent with 54 and 43% activity remaining for G9a and PRC2, respectively, when used at a concentration of 10 µM. It is selective for G9a and PRC2 over SU39H1 and NDMT1 up to a concentration of 40 µM. It is more potent than BRD4770 (Item No. 11787) in enzyme assays but has no activity in cell-based assays when used at concentrations of 5 and 10 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yuan, Y., Wang, Q., Paulk, J., et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem. Biol. 7(7), 1152-1157 (2012).