CPI-455 HCl

Catalog No.S8287

CPI-455 HCl Chemical Structure

Molecular Weight(MW): 314.77

CPI-455 is a specific KDM5 inhibitor, 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.

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Biological Activity

Description CPI-455 is a specific KDM5 inhibitor, 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

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].

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL (31.76 mM)
Ethanol 2 mg/mL (6.35 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 314.77
Formula

C16H15ClN4O

CAS No. 1628208-23-0(free base)
Storage powder
Synonyms N/A

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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.

Handling Instructions

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Related Antibodies

Histone Demethylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID