A potent inhibitor of CREBBP/EP300 bromodomains
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SGC-CBP30

Item No. 14469

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)Epigenetic Chemical Probe Guide (PDF)
Technical Information
Formal Name
2-[2-(3-chloro-4-methoxyphenyl)ethyl]-5-(3,5-dimethyl-4-isoxazolyl)-1-[(2S)-2-(4-morpholinyl)propyl]-1H-benzimidazole
CAS Number
1613695-14-9
Molecular Formula
C28H33ClN4O3
Formula Weight
509.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS (pH 7.2) (1:5): 0.1 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/ml
λmax
221, 287 nm
SMILES
COC(C=C1)=C(Cl)C=C1CCC2=NC3=CC(C4=C(C)ON=C4C)=CC=C3N2C[C@H](C)N5CCOCC5
InChi Code
InChI=1S/C28H33ClN4O3/c1-18(32-11-13-35-14-12-32)17-33-25-8-7-22(28-19(2)31-36-20(28)3)16-24(25)30-27(33)10-6-21-5-9-26(34-4)23(29)15-21/h5,7-9,15-16,18H,6,10-14,17H2,1-4H3/t18-/m0/s1
InChi Key
GEPYBHCJBORHCE-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $121

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    10 mg

    $229

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    50 mg

    $894

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    Product Description

    cAMP-responsive element-binding protein binding protein (CREBBP) and E1A-associated protein p300 (EP300) are transcriptional co-activators. Each contains a bromodomain, which recognizes acetylated lysine residues on target proteins. SGC-CBP30 is a potent inhibitor of CREBBP and EP300 bromodomains (IC50s = 21-69 and 38 nM, respectively).1 Developed by the Structural Genomics Consortium (SGC), this compound displays over 40-fold selectivity for CREBBP over BRD4(1) and is functional in cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gallenkamp, D., Gelato, K.A., Haendler, B., et al. Bromodomains and their pharmacological inhibitors. Chem. Med. Chem. 9(3), 438-464 (2014).

    Product Citations

    Kanada, F., Takamura, Y., Miyake, S., et al. Histone acetyltransferase and Polo-like kinase 3 inhibitors prevent rat galactose-induced cataract. Sci. Rep. 9(1), 20085 (2019).