CPI-455

Catalog No.S6389 Batch:S638901

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Technical Data

Formula

C16H14N4O
Molecular Weight 278.31 CAS No. 1628208-23-0
Solubility (25°C)* In vitro Ethanol 5 mg/mL (17.96 mM)
DMSO Insoluble
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes.
Targets
KDM5 [1]
(in enzymatic assays)
10 nM
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]
In vivo

Dual blockade of B7-H4 and KDM5B (CPI-455, 50/70 mg/kg, ip, daily) in mice elicits protective immunity. Treatment with CPI-455 to selectively targets H3K4-specific JmjC demethylases. CPI-455 increases CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Melanoma (M14) cell lines, breast cancer (SKBR3) cell lines, NSCLC (PC9) cell lines

  • Concentrations

    6.25-25 μM

  • Incubation Time

    4 days, 5 days

  • Method

    Cells are plated in 6-well plates and treated with various concentrations of CPI-455 for up to 4 d. Cells are collected at various time points, and global levels of H3K4me3 and total H3 are determined using MSD ELISA.

Selleck's CPI-455 has been cited by 5 publications

Patient derived tumoroids of high grade neuroendocrine neoplasms for more personalized therapies [ NPJ Precis Oncol, 2024, 8(1):59] PubMed: 38429350
Priming therapy by targeting enhancer-initiated pathways in patient-derived pancreatic cancer cells [ EBioMedicine, 2023, 92:104602] PubMed: 37148583
Epigenetically suppressed tumor cell intrinsic STING promotes tumor immune escape [ Biomed Pharmacother, 2023, 157:114033] PubMed: 36436495
Epigenetic alterations of CXCL5 in Cr(VI)-induced carcinogenesis [ Sci Total Environ, 2022, 838(Pt 1):155713] PubMed: 35660107
pncCCND1_B Engages an Inhibitory Protein Network to Downregulate CCND1 Expression upon DNA Damage [ Cancers (Basel), 2022, 14(6)1537] PubMed: 35326688

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.