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CPI-455 HCl

Cat. No. M8937
CPI-455 HCl Structure
Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 165 In stock
50mg USD 660 In stock
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Quality Control
Biological Activity

CPI-455 HCl mediated KDM5 inhibition, elevated 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 hydrochloride inhibits KDM5A, KDM5B and KDM5C to similar extents but showed substantially weaker potency toward KDM4C and KDM7B (~200- and 770-fold, respectively).

CPI-455 hydrochloride specifically alters H3K4 methylation in cells and binds at the demethylase active site. Pretreatment of cancer cells with a KDM5-specific inhibitor results in the ablation of a subpopulation of cancer cells that can serve as the founders for therapeutic relapse.

Cell Experiment
Cell lines melanoma (M14), breast cancer (SKBR3) and NSCLC (PC9) cell lines
Preparation 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.
Concentrations 0-25 μM
Incubation time 14-20 days
Animal Experiment
Animal models
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 314.77
Formula C16H14N4O.HCl
CAS Number 1628208-23-0
Purity 99.89%
Solubility DMSO: 10 mg/mL
Storage at -20°C

An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells.
Vinogradova M, et al. Nat Chem Biol. 2016 Jul;12(7):531-8. PMID: 27214401.

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Keywords: CPI-455 HCl supplier, Histone demethylases, inhibitors

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