An inhibitor of the BRPF1 bromodomain
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GSK5959

Item No. 18123

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-dihydro-1,3-dimethyl-2-oxo-6-(1-piperidinyl)-1H-benzimidazol-5-yl]-2-methoxy-benzamide
CAS Number
901245-65-6
Molecular Formula
C22H26N4O3
Formula Weight
394.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS (pH 7.2); (1:7): 0.1 mg/mlDMSO: 1 mg/mlEthanol: 1 mg/ml
λmax
208, 240, 323 nm
SMILES
CN(C1=CC(NC(C2=CC=CC=C2OC)=O)=C(N3CCCCC3)C=C1N4C)C4=O
InChi Code
InChI=1S/C22H26N4O3/c1-24-18-13-16(23-21(27)15-9-5-6-10-20(15)29-3)17(26-11-7-4-8-12-26)14-19(18)25(2)22(24)28/h5-6,9-10,13-14H,4,7-8,11-12H2,1-3H3,(H,23,27)
InChi Key
LTUGYAOMCKNTGG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $203

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    25 mg

    $420

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    Product Description

    GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).1 It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Demont, E.H., Bamborough, P., Chung, C.W., et al. 1,3-Dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain. ACS Med. Chem. Lett. 5, 1190-1195 (2014).