Cat. No.: HY-100421

CPI-455

14 Cited Publications

Customer Review

Based on 14 publication(s) in Google Scholar

CPI-455 is a specific, pan-KDM5 inhibitor with an IC₅₀ of 10 nM for KDM5A. CPI-455 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: 98.17%
CAS No.: 1628208-23-0
Formula: C₁₆H₁₄N₄O
Molecular Weight:278.31

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CPI-455 Chemical Structure

CAS No.: 1628208-23-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

KDM5

All Histone Demethylase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	>50 μM Compound: 3; CPI-455	Growth inhibition of human A549 cells after 72 hrs by Alamar blue staining based fluorescence assay Growth inhibition of human A549 cells after 72 hrs by Alamar blue staining based fluorescence assay	[PMID: 30745098]
DU-145	IC₅₀	35.9 μM Compound: CPI-455	Antiproliferative activity against human DU-145 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36931124]
HepG2	IC₅₀	42.65 μM Compound: CPI-455	Antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36931124]
LNCaP	IC₅₀	29.64 μM Compound: CPI-455	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human LNCaP cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36931124]
MCF7	IC₅₀	35.43 μM Compound: CPI-455	Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36931124]
MGC-803	IC₅₀	33.72 μM Compound: CPI-455	Antitumor activity against human MGC-803 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antitumor activity against human MGC-803 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36931124]
MKN-45	IC₅₀	23.79 μM Compound: CPI-455	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell proliferation measured after 6 days by MTS assay Antiproliferative activity against human MKN-45 cells assessed as reduction in cell proliferation measured after 6 days by MTS assay	[PMID: 32155529]
MKN-45	IC₅₀	30.33 μM Compound: CPI-455	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell proliferation measured after 4 days by MTS assay Antiproliferative activity against human MKN-45 cells assessed as reduction in cell proliferation measured after 4 days by MTS assay	[PMID: 32155529]
PC-3	IC₅₀	26.71 μM Compound: CPI-455	Antitumor activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antitumor activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36931124]
PC-9	EC₅₀	5.2 μM Compound: 18	Antiproliferative activity against human PC-9 cells assessed as reduction in cell viability Antiproliferative activity against human PC-9 cells assessed as reduction in cell viability	[PMID: 34555614]
Sf9	IC₅₀	14300 nM Compound: 3; CPI-455	Inhibition of human C-terminal FLAG-tagged KDM6B (1043 to end residues) expressed in baculovirus infected Sf9 insect cells using H3(21-44)-K27(Me3)-GK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay Inhibition of human C-terminal FLAG-tagged KDM6B (1043 to end residues) expressed in baculovirus infected Sf9 insect cells using H3(21-44)-K27(Me3)-GK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay	[PMID: 30745098]
Sf9	IC₅₀	3010 nM Compound: 3; CPI-455	Inhibition of full-length human N-terminal FLAG/His-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay Inhibition of full-length human N-terminal FLAG/His-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay	[PMID: 30745098]
Sf9	IC₅₀	337 nM Compound: 3; CPI-455	Inhibition of human N-terminal FLAG/His-tagged KDM5B (2 to 751 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay Inhibition of human N-terminal FLAG/His-tagged KDM5B (2 to 751 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay	[PMID: 30745098]
Sf9	IC₅₀	506 nM Compound: 3; CPI-455	Inhibition of human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay Inhibition of human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay	[PMID: 30745098]

In Vitro

CPI-455 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, 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, 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.

Animal Model:

Six-week-old male C57BL/6 mice (One- to 2-mm fragments of P. gingivalis–positive PDXs were implanted subcutaneously into the flank region of humanized mice.)
Dosage:

50 mg/kg or 70 mg/kg (combined with anti–B7-H4).
Administration:

IP, daily, 14-28 days.
Result:

Histopathology analysis revealed no inflammation in either group at 2 weeks in response to the primary infection. However, at 8 weeks after inoculation, mice receiving monotherapy exhibited mild inflammation, whereas the combined treatment presented with heavy to severe inflammation, which persisted at 12 and 16 weeks after challenge.
Treatment with CPI-455 to selectively target H3K4-specific JmjC demethylases increased CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.

Chemical Information

CAS No. 1628208-23-0
Appearance Solid
Molecular Weight 278.31
Formula C₁₆H₁₄N₄O
Color White to off-white
SMILES

N#CC1=C2NC(C3=CC=CC=C3)=C(C(C)C)C(N2N=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

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Journal Impact Factor

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 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 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 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.
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 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.
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 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.
Phytomedicine

Biochanin A alleviates endothelial cell senescence via epigenetic regulation of the HDAC1/H3K4me3/NFKB1 axis. [Abstract]

2025 Oct 13:148:157385. 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
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

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
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
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
Cancers

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
Transl Oncol

A RIPK2 activity signature in prostate cancer: Modulation by RIPK2 inhibition and clinical association. [Abstract]

2026 Jul:69:102819. PMID: 42143470
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
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
University of Pennsylvania

2025.

Solvent & Solubility

In Vitro:

DMSO : 29.17 mg/mL (104.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.5931 mL

17.9656 mL

35.9312 mL

5 mM

0.7186 mL

3.5931 mL

7.1862 mL

10 mM

0.3593 mL

1.7966 mL

3.5931 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5931 mL	17.9656 mL	35.9312 mL	89.8279 mL
	5 mM	0.7186 mL	3.5931 mL	7.1862 mL	17.9656 mL
	10 mM	0.3593 mL	1.7966 mL	3.5931 mL	8.9828 mL
	15 mM	0.2395 mL	1.1977 mL	2.3954 mL	5.9885 mL
	20 mM	0.1797 mL	0.8983 mL	1.7966 mL	4.4914 mL
	25 mM	0.1437 mL	0.7186 mL	1.4372 mL	3.5931 mL
	30 mM	0.1198 mL	0.5989 mL	1.1977 mL	2.9943 mL
	40 mM	0.0898 mL	0.4491 mL	0.8983 mL	2.2457 mL
	50 mM	0.0719 mL	0.3593 mL	0.7186 mL	1.7966 mL
	60 mM	0.0599 mL	0.2994 mL	0.5989 mL	1.4971 mL
	80 mM	0.0449 mL	0.2246 mL	0.4491 mL	1.1228 mL
	100 mM	0.0359 mL	0.1797 mL	0.3593 mL	0.8983 mL

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CPI-455

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Breast Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) CPI-455

All Histone Demethylase Isoforms

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CPI-455

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Breast Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) CPI-455

All Histone Demethylase Isoforms

Biological Activity

Chemical Information

Publications (14)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CPI-455 Related Classifications

HY-100421 Related Classifications