CPI-455 hydrochloride
Based on 14 publication(s) in Google Scholar
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.
- Purity: 99.95%
- CAS No.: 2095432-28-1
- Formula: C16H15ClN4O
- Molecular Weight:314.77
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CPI-455 hydrochloride
More- Nat Commun. 2025 Dec 16. [Abstract]
- Cell Mol Biol Lett. 2025 Jan 29;30(1):14. [Abstract]
- Phytomedicine. 2025 Nov 25:148:157385. [Abstract]
- Phytomedicine. 2025 Sep 22:148:157291. [Abstract]
- EBioMedicine. 2024 Jul:105:105177. [Abstract]
- Cell Death Discov. 2025 Jul 29;11(1):351. [Abstract]
- Oncogene. 2021 Apr;40(15):2711-2724. [Abstract]
- Blood Adv. 2021 Sep 14;5(17):3241-3253. [Abstract]
- Inflammation. 2021 Oct;44(5):1803-1814. [Abstract]
- Transl Oncol. 2026 Jul:69:102819. [Abstract]
- Cancers (Basel). 2019 Jan 15;11(1):92. [Abstract]
- Clin Exp Med. 2025 Nov 25;26(1):33. [Abstract]
- ACS Chem Neurosci. 2024 Apr 3;15(7):1570-1580. [Abstract]
- University of Pennsylvania. 2025.
Customer Validation & Images
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Cell Imaging/Staining
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Cell Imaging/Staining
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Others
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WB
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RT-PCR
Biological Activity
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KDM5 |
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.
Chemical Information
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CAS No. 2095432-28-1
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Appearance Solid
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Molecular Weight 314.77
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Formula C16H15ClN4O
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Color White to off-white
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SMILES
N#CC1=C2NC(C3=CC=CC=C3)=C(C(C)C)C(N2N=C1)=O.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Commun
Crosstalk between H3K4me3 and oxidative stress is a potential target for the improvement of ART-derived embryos. [Abstract]2025 Dec 16. PMID: 41402350
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.
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Cell Mol Biol Lett
The histone demethylase KDM5C enhances the sensitivity of acute myeloid leukemia cells to lenalidomide by stabilizing cereblon. [Abstract]2025 Jan 29;30(1):14. PMID: 39881283
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.
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Phytomedicine
Biochanin A alleviates endothelial cell senescence via epigenetic regulation of the HDAC1/H3K4me3/NFKB1 axis. [Abstract]2025 Nov 25:148:157385. PMID: 41086673 -
Phytomedicine
Baicalein specifically suppresses microsatellite instability colorectal cancer by targeting adenosylhomocysteinase to inhibit histone H3 lysine 4 trimethylation-mediated cancer stemness. [Abstract]2025 Sep 22:148:157291. PMID: 41038143 -
EBioMedicine
Enhancer demethylation-regulated gene score identified molecular subtypes, inspiring immunotherapy or CDK4/6 inhibitor therapy in oesophageal squamous cell carcinoma. [Abstract]2024 Jul:105:105177. PMID: 38924839
CPI-455 hydrochloride purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2024 Jul:105:105177. [Abstract]
TP63e and TP63 expression levels in KYSE450 and KYSE180 cells after CPI-455 (10 μM) treatment.
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Cell Death Discov
Mitochondrial dysfunction-mediated metabolic remodeling of TCA cycle promotes Parkinson's disease through inhibition of H3K4me3 demethylation. [Abstract]2025 Jul 29;11(1):351. PMID: 40730642 -
Oncogene
2021 Apr;40(15):2711-2724. PMID: 33712705 -
Blood Adv
KDM5A suppresses PML-RARα target gene expression and APL differentiation through repressing H3K4me2. [Abstract]2021 Sep 14;5(17):3241-3253. PMID: 34448811 -
Inflammation
MLL3 Inhibits Apoptosis of Rheumatoid Arthritis Fibroblast-Like Synoviocytes and Promotes Secretion of Inflammatory Factors by Activating CCL2 and the NF-κB Pathway. [Abstract]2021 Oct;44(5):1803-1814. PMID: 33914205 -
Transl Oncol
A RIPK2 activity signature in prostate cancer: Modulation by RIPK2 inhibition and clinical association. [Abstract]2026 Jul:69:102819. PMID: 42143470 -
Cancers (Basel)
Structure-Based Discovery of a Selective KDM5A Inhibitor that Exhibits Anti-Cancer Activity via Inducing Cell Cycle Arrest and Senescence in Breast Cancer Cell Lines. [Abstract]2019 Jan 15;11(1):92. PMID: 30650517 -
Clin Exp Med
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]2025 Nov 25;26(1):33. PMID: 41286164 -
ACS Chem Neurosci
Histone Lysine Demethylase KDM5 Inhibitor CPI-455 Induces Astrocytogenesis in Neural Stem Cells. [Abstract]2024 Apr 3;15(7):1570-1580. PMID: 38501572 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8. [Content Brief]
[2]. Benjamin R. Leadem. NOVEL HISTONE DEMETHYLASE INHIBITORS SYNERGISTICALLY
[3]. Xiang Yuan, et al. Blockade of Immune-Checkpoint B7-H4 and Lysine Demethylase 5B in Esophageal Squamous Cell Carcinoma Confers Protective Immunity against P. gingivalis Infection. Cancer Immunol Res. 2019 Sep;7(9):1440-1456. [Content Brief]
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 |
CPI-455 hydrochloride Related Classifications
HY-100421A Related Classifications
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