A KDM5 inhibitor
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CPI-455

Item No. 22127

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4,7-dihydro-6-(1-methylethyl)-7-oxo-5-phenyl-pyrazolo[1,5-a]pyrimidine-3-carbonitrile
CAS Number
1628208-23-0
Molecular Formula
C16H14N4O
Formula Weight
278.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:20): 0.05 mg/mlEthanol: 5 mg/ml
λmax
239, 280, 322 nm
SMILES
CC(C)C(C(N1C(N2)=C(C#N)C=N1)=O)=C2C3=CC=CC=C3
InChi Code
InChI=1S/C16H14N4O/c1-10(2)13-14(11-6-4-3-5-7-11)19-15-12(8-17)9-18-20(15)16(13)21/h3-7,9-10,19H,1-2H3
InChi Key
DHXKRMSKXLDZGY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $29

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    5 mg

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    10 mg

    $169

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    25 mg

    $352

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    Cayman Chemical
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    Product Description

    CPI-455 is an inhibitor of the lysine demethylase 5 family (KDM5A-D).1 CPI-455 binds to the demethylase active site and selectively inhibits KDM5A-D (IC50s = 2-10 nM) over KDM2-4, 6, and 7 family members (IC50s = 1 to >25 μM). It increases histone H3K4me2/3 methylation in vitro and decreases the number of drug-tolerant cells in PC9 non-small cell lung, M14 melanoma, and SKBR3 breast cancer cell populations. CPI-455 also reduces growth of glioblastoma cells resistant to temozolomide (TMZ; Item No. 14163) in a dose-dependent manner.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vinogradova, M., Gehling, V.S., Gustafson, A., et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat. Chem. Biol. 12(7), 531-538 (2016).

    2. Banelli, B., Daga, A., Forlani, A., et al. Small molecules targeting histone demethylase genes (KDMs) inhibit growth of temozolomide-resistant glioblastoma cells. Oncotarget 8(21), 34896-34910 (2017).