CB 5083

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Description: Potent p97 ATPase inhibitor
Chemical Name: 1-[7,8-Dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for CB 5083

CB 5083 is a potent p97 inhibitor, inhibiting the D2 ATPase domain (IC50 = 11 nM). CB 5083 shows broad antitumor activity and inhibits tumor growth in vivo. CB 5083 is cytotoxic to A549 cancer cells (IC50 = 680 nM) and reduces cell viablility in a range of colorectal cancer cell lines. Increases CHOP and GRP78 protein levels, upregulates PD-L1 mRNA levels and results in the loss of aggresomes.

Technical Data for CB 5083

M. Wt 413.48
Formula C24H23N5O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1542705-92-9
PubChem ID 73051434
Smiles O=C(N)C1=CC=CC2=C1C=C(N2C=3N=C(NCC=4C=CC=CC4)C5=C(N3)CCOC5)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CB 5083

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 41.35 100
ethanol 41.35 100

Preparing Stock Solutions for CB 5083

The following data is based on the product molecular weight 413.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.42 mL 12.09 mL 24.18 mL
5 mM 0.48 mL 2.42 mL 4.84 mL
10 mM 0.24 mL 1.21 mL 2.42 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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References for CB 5083

References are publications that support the biological activity of the product.

Mukkavalli et al (2021) The p97-UBXN1 complex regulates aggresome formation. J.Cell Sci. 134 PMID: 33712450

Vekaria et al (2016) Targeting p97 to disrupt protein homeostasis in cancer. Front.Oncol. 6 PMID: 27536557

Vekaria et al (2019) Functional cooperativity of p97 and histone deacetylase 6 in mediating DNA repair in mantle cell lymphoma cells. Leukemia 33 1675 PMID: 30664664

Huryn et al (2019) p97: an emerging target for cancer, neurodegenerative diseases, and viral infections. J.Med.Chem. 63 1892 PMID: 31550150

Le Moigne et al (2017) The p97 inhibitor CB-5083 is a unique disrupter of protein homeostasis in models of multiple myeloma. Mol.Cancer Ther. 16 2375 PMID: 28878026

If you know of a relevant reference for CB 5083, please let us know.

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Keywords: CB 5083, CB 5083 supplier, CB5083, p97, atpases, inhibitors, potent, tumor, antitumor, aggresome, valosin, containing, protein, VCP, colorectal, cancer, PD-L1, CRC, ATPase, 7379, Tocris Bioscience

Citations for CB 5083

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Literature in this Area

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Cancer Metabolism Poster

Cancer Metabolism Poster

This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.