1. Epigenetics
  2. Histone Demethylase
  3. CPI-455 hydrochloride

CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

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CPI-455 hydrochloride Chemical Structure

CPI-455 hydrochloride Chemical Structure

CAS No. : 2095432-28-1

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Description

CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].

IC50 & Target

KDM5

 

In Vitro

CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].
CPI-455 hydrochloride, with high measured affinity for the target KDM5 proteins. Within 24 hours, increases in H3K4me3, are observed after exposure to either of the two active compounds, CPI-455 and CPI-766, in a dosedependent manner. IC50 calculation for KDM5 Inhibitor CPI0455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Dual blockade of B7-H4 and KDM5B (CPI-455 hydrochloride, 50/70 mg/kg, ip, daily) in mice elicits protective immunity[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

314.77

Formula

C16H15ClN4O

CAS No.
SMILES

N#CC1=C2NC(C3=CC=CC=C3)=C(C(C)C)C(N2N=C1)=O.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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CPI-455 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CPI-455 hydrochloride
Cat. No.:
HY-100421A
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