CB 5083

Name: CB 5083
Brand: Tocris Bioscience
SKU: 7379

Tocris Bioscience, part of Bio-Techne | Catalog # 7379

Citations (3)

COA / SDS

Potent p97 ATPase inhibitor

Key Product Details

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)
Molecular Weight:	413.48

View Full Technical Details for CB 5083

Technical Data
Citations

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
InChi Key	RDALZZCKQFLGJP-UHFFFAOYSA-N
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 for CB 5083

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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.

Le Moigne The p97 inhibitor CB-5083 is a unique disrupter of protein homeostasis in models of multiple myeloma. Mol.Cancer Ther. 2017 PMID: 28878026
Huryn p97: an emerging target for cancer, neurodegenerative diseases, and viral infections. J.Med.Chem. 2019 PMID: 31550150
Vekaria Targeting p97 to disrupt protein homeostasis in cancer. Front.Oncol. 2016 PMID: 27536557
Vekaria Functional cooperativity of p97 and histone deacetylase 6 in mediating DNA repair in mantle cell lymphoma cells. Leukemia 2019 PMID: 30664664
Mukkavalli The p97-UBXN1 complex regulates aggresome formation. J.Cell Sci. 2021 PMID: 33712450