CHR-6494

SKU: orb1707450

Description

CHR-6494 is a potent and selective haspin kinase inhibitor with an IC50 of 2 nM against histone H3 threonine 3 phosphorylation. This small molecule is a valuable chemical probe for studying mitosis and chromosome dynamics in both cellular and biochemical assays.

Research Area

Cell Biology

Key Properties

• CAS Number: 1333377-65-3
• MW: 292.34
• Purity: 98.78%
• Formula: C₁₆H₁₆N₆
• SMILES: CCCNc(cc1)nn2c1ncc2c(cc3)cc4c3[nH]nc4
• Target: Others,Haspin Kinase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.84 mM);DMSO:50 mg/mL (171.03 mM)

Bioactivity

• Target IC50:
  Haspin:2 nM
• In Vivo:
  CHR-6494 (50 mg/kg, i.p.) inhibits the growth of tumor. It cuases no obvious body weight change in nude mice bearing HCT-116 human colorectal cancer cells .
• In Vitro:
  CHR-6494 does not modify H3S10 and H328 phosphorylation levels and shows no significantly inhibitory effects on other protein kinases. CHR-6494 dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cell (IC50s: 500 nM, 473 nM, 752 nM, and 1059 nM). CHR-6494 (500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1 . CHR-6494 exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM. CHR-6494 (300 nM and 600 nM) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 cells. CHR-6494 in combination with MEK inhibitors synergistically inhibits the viability of melanoma cells, enhances apoptosis in melanoma cells, modulates cell cycle progression independently by arresting melanoma cells at different phases, and suppresses migration of melanoma cells .

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

haspin, CHR 6494, CHR6494, CHR-6494

Compound Identifiers

PubChem CID

70679308