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 decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents. CPI-455 has a high measured affinity for 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 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

78426698