A selective chemical probe for the bromodomain of BRPF1
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GSK6853

Item No. 20985

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide
CAS Number
1910124-24-1
Molecular Formula
C22H27N5O3
Formula Weight
409.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mLDMSO: 25 mg/mLEthanol: 30 mg/mLEthanol:PBS(pH 7.2) (1:1): 0.5 mg/mL
λmax
239, 318 nm
SMILES
C[C@H](CNCC1)N1C2=C(NC(C3=CC=CC=C3OC)=O)C=C4C(N(C)C(N4C)=O)=C2
InChi Code
InChI=1S/C22H27N5O3/c1-14-13-23-9-10-27(14)17-12-19-18(25(2)22(29)26(19)3)11-16(17)24-21(28)15-7-5-6-8-20(15)30-4/h5-8,11-12,14,23H,9-10,13H2,1-4H3,(H,24,28)/t14-/m1/s1
InChi Key
FQWDVNSBYDXPIO-CQSZACIVSA-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

    $103

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    10 mg

    $186

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    25 mg

    $378

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    Product Description

    GSK6853 is a chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5.1 It exhibits >1,600-fold selectivity for BRPF1 over all other bromodomains in a BROMOscan assay and shows cellular target engagement with a pIC50 value of 7.7 in a NanoBRET assay evaluating the interaction of the NanoLuc-BRPF1 bromodomain with histone H3.3-HaloTag in HEK293 cells.1 See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bamborough, P., Barnett, H.A., Becher, I., et al. GSK6853, a chemical probe for inhibition of the BRPF1 bromodomain. ACS Med. Chem. Lett. 7(6), 552-557 (2016).