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.

For research use only. We do not sell to patients.

CAS No. : 2095432-28-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of CPI-455 hydrochloride:

Top Publications Citing Use of Products

    CPI-455 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 16.  [Abstract]

    Representative images of blastocysts obtained by in vitro fertilization (IVF) after treatment with different concentrations of CPI-455.

    CPI-455 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 16.  [Abstract]

    ROS staining and quantification were performed on CPI-455 (5 μM) treated/untreated blastocysts from in vitro fertilization (IVF) embryos.

    CPI-455 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 16.  [Abstract]

    During human embryonic development, the proportion of blastocysts on day 5/6 and the proportion of high-quality embryos on day 3 or day 5/6 with/without CPI-455 (5 μM) treatment.

    CPI-455 hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Mol Biol Lett. 2025 Jan 29;30(1):14.  [Abstract]

    HEK293T cells were treated with the KDM5C inhibitors CPI-455 (1 µM) and KDM5-IN-1 (1 µM) for 24 h.

    CPI-455 hydrochloride purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2024 Jul:105:105177.

    TP63e and TP63 expression levels in KYSE450 and KYSE180 cells after CPI-455 (10 μM) treatment.

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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.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 8.33 mg/mL (26.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1769 mL 15.8846 mL 31.7692 mL
    5 mM 0.6354 mL 3.1769 mL 6.3538 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.95%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1769 mL 15.8846 mL 31.7692 mL 79.4231 mL
    5 mM 0.6354 mL 3.1769 mL 6.3538 mL 15.8846 mL
    10 mM 0.3177 mL 1.5885 mL 3.1769 mL 7.9423 mL
    15 mM 0.2118 mL 1.0590 mL 2.1179 mL 5.2949 mL
    20 mM 0.1588 mL 0.7942 mL 1.5885 mL 3.9712 mL
    25 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1769 mL
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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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