An inhibitor of CBP/EP300 bromodomains
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CPI-637

Item No. 23500

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4R)-1,3,4,5-tetrahydro-4-methyl-6-[1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl]-2H-1,5-benzodiazepin-2-one
CAS Number
1884712-47-3
Molecular Formula
C22H22N6O
Formula Weight
386.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.2 mg/mlDMSO: 0.5 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.1 mg/ml
λmax
201, 229, 320 nm
SMILES
CN1N=C(C2=CN(C)N=C2)C3=C1C=CC(C4=C(N[C@H](C)CC(N5)=O)C5=CC=C4)=C3
InChi Code
InChI=1S/C22H22N6O/c1-13-9-20(29)25-18-6-4-5-16(22(18)24-13)14-7-8-19-17(10-14)21(26-28(19)3)15-11-23-27(2)12-15/h4-8,10-13,24H,9H2,1-3H3,(H,25,29)/t13-/m1/s1
InChi Key
BFTKDWYIRJGJCA-CYBMUJFWSA-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

    $135

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    10 mg

    $186

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    25 mg

    $378

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    Product Description

    CPI-637 is an inhibitor of cyclic-AMP response element binding protein (CBP) and adenoviral E1A binding protein of 300 kDa (EP300), a homologous pair of bromodomain-containing proteins (IC50s = 30 and 51 nM in a time-resolved-FRET (TR-FRET) assay).1 It is selective for CBP and EP300 over the BET family of bromodomains (IC50s = >10 μM), however, CPI-637 is active at bromodomain BRD9 (IC50 = 0.73 μM). CPI-637 also inhibits MYC expression (EC50 = 0.6 μM) in AMO-1 cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Taylor, A.M., Côté, A., Hewitt, M.C., et al. Fragment-based discovery of a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor (CPI-637). ACS Med. Chem. Lett. 7(5), 531-536 (2016).