Description
BRD9539 is a specific inhibitor of euchromatin histone methyltransferase G9a (EHMT2). EHMT2 catalyzes the methylation of lysine 9 on histone H3. BRD9539 inhibits EHMT2 with an IC₅₀ of 6.3 μM. It also inhibits methyl transferase PRC2 with a similar IC₅₀. It is the methyl-ester analogue of BRD4770. It is more potent than BRD4770 in enzyme assays but does not show activity in cell-based assays, probably due to impaired cell permeability compared to that of BRD4770.
BRD9539 is a specific inhibitor of euchromatin histone methyltransferase G9a (EHMT2). EHMT2 catalyzes the methylation of lysine 9 on histone H3. BRD9539 inhibits EHMT2 with an IC₅₀ of 6.3 μM. It also inhibits methyl transferase PRC2 with a similar IC₅₀. It is the methyl-ester analogue of BRD4770. It is more potent than BRD4770 in enzyme assays but does not show activity in cell-based assays, probably due to impaired cell permeability compared to that of BRD4770.
Alternate Name/Synonyms: BRD9539; 2-benzamido-1-(3-phenylpropyl)benzimidazole-5-carboxylic acid
Appearance: Crystalline solid
Formulation:
CAS Number: 1374601-41-8
Structure Available?: True
Peptide sequence:
Salt Form: False
Molecular Formula: C₂₄H₂₁N₃O₃
Molecular Weight: 399.44
Cell-Permeable?: False
Purity: ≥98%
Solubilities: 0.5 mg/ml in in Ethanol, 10 mg/ml in DMSO and DMF in 0
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: A specific inhibitor of euchromatin histone methyltransferase G9a (EHMT2)
MDL Number:
PubChem CID: 73755260
SMILES: C1=CC=C(C=C1)CCCN2C3=C(C=C(C=C3)C(=O)O)N=C2NC(=O)C4=CC=CC=C4
InChi: 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
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |