CPI-455

SKU: orb1304073

Description

CPI-455

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1628208-23-0
• MW: 278.31
• Purity: 99.03%
• Formula: C₁₆H₁₄N₄O
• SMILES: CC(C)c1c([nH]c2c(cnn2c1=O)C#N)-c1ccccc1
• Target: Histone Demethylase
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:41.67 mg/mL (149.73 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.59 mM)

Bioactivity

• Target IC50:
  KDM5A:10 nM IC50
• In Vitro:
  CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decrease the number of DTPs in multiple cancer cell line models treated with s andard chemotherapy or targeted agent. CPI-455 has a high measured affinity fo the target KDM5 proteins. Within 24 hours, CPI-455 and CPI-766 can dose-dependently increases in H3K4me3, but not H3K4me2. IC50 calculation for KDM5 inhibitor CPI-455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively
• Cell Research:
  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 o 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Histone Demethylase, HistoneDemethylase, KDM5A, CPI 455, CPI455, CPI-455

Compound Identifiers

PubChem CID

78426698