CPI-455

Name: CPI-455
Brand: MedChemExpress
SKU: HY-100421
Rating: 5.0 (13 reviews)

Cat. No.: HY-100421 Purity: 98.17%: Data Sheet
COA

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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.

CAS No. : 1628208-23-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of CPI-455:

CPI-455 hydrochloride In-stock
CPI-455 (Standard) Get quote

13 Publications Citing Use of MCE CPI-455

Cell Imaging/Staining

RT-PCR

Others

: 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.

: 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.

: CPI-455 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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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

KDM5

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.

Molecular Weight

278.31

Formula

C₁₆H₁₄N₄O

CAS No.

1628208-23-0

Appearance

Solid

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.95%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (256 KB) HNMR (180 KB) LCMS (117 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]

Complete Stock Solution Preparation Table

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

CPI-455 Related Classifications

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.

Keywords:

CPI-4551628208-23-0CPI455CPI 455Histone DemethylaseInhibitorinhibitorinhibit

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CPI-455

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CPI-455 Related Antibodies

13 Publications Citing Use of MCE CPI-455

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View All Histone Demethylase Isoform Specific Products:

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Purity & Documentation

References

Customer Review

CPI-455 Related Antibodies

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Complete Stock Solution Preparation Table

CPI-455 Related Classifications

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