CB-5083

SKU: orb1300457

Description

CB-5083 is a potent, selective, and orally available inhibitor of the p97 AAA ATPase, with an IC50 of 11 nM. It is widely used in cancer research to study protein homeostasis and has demonstrated antitumor activity in both cellular assays and in vivo xenograft models.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 1542705-92-9
• MW: 413.47
• Purity: >99.99% (May vary between batches)
• Formula: C₂₄H₂₃N₅O₂
• SMILES: Cc1cc2c(cccc2n1-c1nc2CCOCc2c(NCc2ccccc2)n1)C(N)=O
• Target: p97
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:11 mg/mL (26.6 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:6 mg/mL (14.51 mM);DMSO:247.5 mg/mL (598.59 mM)

Bioactivity

• Target IC50:
  p97 AAA ATPase:11 nM
• In Vivo:
  In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition.
• In Vitro:
  In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM.
• Cell Research:
  A549 and other tumor cell lines are cultured according to ATCC guidelines. Cells are cultured in black or white, clear-bottomed, tissue culture-treated 384-well plates. Cells are treated with 10-point dose titration of the compound in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability. Luminescence values are fit to a four-parameter sigmoidal curve to determine IC50 concentrations.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | 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

Cdc48, CB5083, CB-5083, CB 5083, ATPase, AAA, p97, Inhibitor, inhibit, multiple, myeloma, VCP, tumors, solid

Compound Identifiers

PubChem CID

73051434