For research use only.

Catalog No.S8101

18 publications

CB-5083 Chemical Structure

CAS No. 1542705-92-9

CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.

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Selleck's CB-5083 has been cited by 18 publications

3 Customer Reviews

  • LN229 GBM cell lysates were immunoblotted with antibodies recognizing specific focal adhesion proteins. Note the decreased levels of Cas, paxillin, and FAK tyrosine phosphorylation in cells treated with CB-5083. In addition, CB-5083 treatment leads to decreased levels of total PTP-PEST expression, but Vcp protein expression levels are not impacted.

    Cancer Res, 2018, 78(14):3809-3822. CB-5083 purchased from Selleck.

  • Incubation with VCP inhibitors results in activation of Unfolded Protein Response (UPR). SKOV3 cells were incubated with (C) 2.5 μM CB-5083 for 0, 1, 3, 6, 12, 24 and 48 h. Whole cell lysates were subjected to Western blot analysis and probed for UPR-related proteins

    Mol Oncol, 2016, 10(10):1559-1574. CB-5083 purchased from Selleck.

  • Cycloheximide (CHX) chase experiments in the presence of the unrelated competitive p97 inhibitor CB-5083 (5 μm) or DMSO alone. Cells were lysed at indicated time points after CHX addition and lysates subjected to Western blotting. Tubulin was probed as loading control. UT = untreated.

    Mol Cell Proteomics, 2018, 17(7):1295-1307. CB-5083 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
p97 AAA ATPase [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 Mn\VSpVv[3Srb36gZZN{[Xl? MWO2JIg> NY\TSHh2UW6qaXLpeIlwdiCxZjDwPVchSVSSYYPlJIlvKGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJJA3OiCycn;0[YlvKGmwY4XiZZRm\CCob4KgOkBpenNiYomgbY1ufW6xZnz1c5Jme2OnbnPlJIF{e2G7LDDJR|UxRTBwNEmg{txO MkTCNlY2PjV4Nk[=
A549 MlPVR5l1d3SxeHnjbZR6KGG|c3H5 Mk\LO|IhcA>? M1;QbWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JGNmdGy2aYTldk1IdG9iYYPzZZktKEmFNUC9NE43QCEQvF2= MmjpNlY2PjV4Nk[=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
Bip / XBP1s / PERK / pEIF2α / CHOP ; 

PubMed: 26555175     

A549 cells were treated with CB-5083, bortezomib (1 μM), thapsigargin (1 μM) or tunicamycin (2 μg/ml) for 8 hr. Western blot analysis was performed with antibodies against BiP, spliced XBP1 (XBP1s), PERK, phospho-EIF2a, CHOP, cleaved (cl) ATF6 and GAPDH.


PubMed: 31316150     

(A) MCF-7 and (B) MCF-10A cells were each plated for 24 hours and then treated with increasing amounts of CB-5083 (p97i). 24 hours after treatment, cells were collected and fractionated into cytoplasmic, soluble nuclear, and chromatin-bound fractions. Proteins from each fraction were then visualized by Western blot with the indicated antibodies. Actin and Histone H3 serve as loading controls for the indicated fractions. 

p-IRE1α / IRE1α / p-eIF2α / ATF4 ; 

PubMed: 27729194     

SKOV3 cells were incubated with 2.5 μM CB-5083 for 0, 1, 3, 6, 12, 24 and 48 h. Whole cell lysates were subjected to Western blot analysis and probed for UPR-related proteins.

26555175 31316150 27729194
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:[1]
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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:[1]
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  • Cell lines: A549 cells
  • Concentrations: ~40.0 μM
  • Incubation Time: 72 h
  • Method: 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)
Animal Research:[1]
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  • Animal Models: Nu/Nu nude female mice bearing human HCT 116 colon tumor xenografts
  • Dosages: 75 mg/kg, qd
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (198.32 mM)
Water Insoluble
Ethanol '13 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% CMC Na+5% Tween 80
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 413.47


CAS No. 1542705-92-9
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC2=C(C=CC=C2N1C3=NC4=C(COCC4)C(=N3)NCC5=CC=CC=C5)C(=O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02243917 Terminated Drug: CB-5083 Advanced Solid Tumors Cleave Biosciences Inc. October 11 2014 Phase 1
NCT02223598 Terminated Drug: CB-5083|Drug: Dexamethasone Lymphoid Hematological Malignancies|Relapsed and Refractory Multiple Myeloma Cleave Biosciences Inc. August 25 2014 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    I am trying to administrate the compound to mice. Does this compound ever dissolve completely?

  • Answer:

    S8101 CB-5083 can be dissolved in 0.5% CMC Na+5% Tween 80 at 30 mg/ml as a suspension for oral gavage.

ATPase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID