Home Epigenetics Histone Demethylase inhibitor - JMJD inhibitor CPI-455 HCl For research use only.

CPI-455 HCl

CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

CPI-455 HCl Chemical Structure

CPI-455 HCl Chemical Structure

CAS No. 2095432-28-1

Purity & Quality Control

CPI-455 HCl Related Products

Signaling Pathway

Histone Demethylase Signaling Pathways

Histone Demethylase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 Function assay 1 hr 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, IC50=0.337μM 30745098
Sf9 Function assay 1 hr 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, IC50=0.506μM 30745098
Sf9 Function assay 1 hr 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, IC50=3.01μM 30745098
PC9 Function assay 4 days Inhibition of KDM5A in human PC9 cells assessed as increase in H3K4me3 levels preincubated for 4 days measured up to 24 hrs by ELISA, EC50=5.2μM 27476424
Sf9 Function assay 1 hr 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, IC50=14.3μM 30745098
MDA-MB-231 Growth inhibition assay 50 uM 72 hrs Growth inhibition of human MDA-MB-231 cells at 50 uM after 72 hrs by Alamar blue staining based fluorescence assay 30745098
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Biological Activity

Description CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
Targets
KDM5A [1]
(Cell-free assay)
10 nM
In vitro
In vitro

CPI-455 has improved potency against KDM5A while demonstrating ~200-fold selectivity for KDM5A over KDM4C. CPI-455 inhibits KDM5A, KDM5B and KDM5C to similar extents but showed substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively) and no measurable inhibition of KDM2B, KDM3B or KDM6A. CPI-455-mediated KDM5 inhibition results in a dose-dependent increase in global H3K4me3 in HeLa cells. CPI-455 specifically alters H3K4 methylation in cells and binds at the demethylase active site[1].
Cell Research Cell lines melanoma (M14), breast cancer (SKBR3) and NSCLC (PC9) cell lines
Concentrations 0-25 μM
Incubation Time 14-20 days
Method

All cell lines were treated with DMSO, CPI-4203 or CPI-455 for 5 d with two changes of medium and drug. Thereafter, the cells (PC9, Colo205, Hs888, M14, SKBR3 and EVSA-T) were plated at 2×105 cells in six-well plates in triplicate and treated for an additional 9-15 d, depending on the cell line model. The Incucyte HD imaging system was used to monitor numbers of drug-tolerant cells after cells were stained with Nuclear-ID Red stain.

Chemical Information & Solubility

Molecular Weight 314.77 Formula

C16H15ClN4O
CAS No. 2095432-28-1 SDF Download CPI-455 HCl SDF
Smiles CC(C)C1=C(N=C2C(=CNN2C1=O)C#N)C3=CC=CC=C3.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (200.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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