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CB-5083

Catalog No. T6796 CAS 1542705-92-9

Synonyms: CB5083, CB 5083

CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor ( IC50=11 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CB-5083, CAS 1542705-92-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 139.00
25 mg	In stock	$ 313.00
50 mg	In stock	$ 493.00
100 mg	In stock	$ 723.00
500 mg	In stock	$ 1,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 100%

Purity: 99.92%

Purity: 95.95%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor ( IC50=11 nM).
Targets&IC50	p97 AAA ATPase:11 nM
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. [1]
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. [1]
Kinase Assay	ATPase assay: Compounds are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 μM. The assay is done in a 384-well plate with each row as a single dilution series with duplicate of each compound concentration point. In 5 μL total volume, 20 nM p97 hexameric enzyme and 20 μM ATP are added to start the reaction. The plate is sealed and incubated at 37 °C for 15 min after mixing thoroughly in an orbital shaker. Compound dilution, ATP and enzymes addition are conducted with automated liquid handling using the Freedom Evo. ADP Glo reagents 1 and 2 are added according to the manufacturer's protocol. The luminescence is measured by Envision plate reader as the end point of the reaction. The IC50 of each compound is derived by fitting the luminescence values to a four-parameter sigmoidal curve.
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)

Synonyms	CB5083, CB 5083
Molecular Weight	413.47
Formula	C24H23N5O2
CAS No.	1542705-92-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 11 mg/mL (26.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 76 mg/mL (183.8 mM)

References and Literature

1. Zhou HJ, et al. J Med Chem. 2015, 58(24), 9480-9497.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Viral Compound Library Orally Active Compound Library Target-Focused Phenotypic Screening Library Mitochondria-Targeted Compound Library NO PAINS Compound Library

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ML241 MNS DBEQ CB-5339 UPCDC30766 ML241 hydrochloride NMS-873 MSC1094308

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CB-5083 1542705-92-9 Ubiquitination p97 Inhibitor inhibit multiple CB5083 VCP solid tumors myeloma CB 5083 AAA ATPase Cdc48 inhibitor

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