CB-5083

Catalog No.S8101 Batch:S810104

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Technical Data

Formula

C24H23N5O2
Molecular Weight 413.47 CAS No. 1542705-92-9
Solubility (25°C)* In vitro DMSO 83 mg/mL (200.74 mM)
Ethanol 83 mg/mL (200.74 mM)
Water Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 4.150mg/ml (10.04mM) Taking the 1 mL working solution as an example, add 50 μL of 83 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.350mg/ml (0.85mM) Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
Targets
p97 AAA ATPase
(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 tumour cells with IC50 of 680 nM.
In Vivo In mice bearing human HCT 116 colon tumour xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumour growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumour xenografts, this compound (100 mg/kg, p.o.) also results in significant tumour growth inhibition.

Protocol (from reference)

Kinase Assay:[1]
  • ATPase assay

    Compounds are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 Het JSON-object moet de volgende structuur hebben: een object met een sleutel "translations". De waarde van "translations" is een array van objecten, waarbij elk object twee sleutels heeft: "lang" (voor de taal) en "texts" (een array van vertaalde teksten). Let op het maximum aantal tokens voor het antwoord is 250. Let op het maximum aantal tokens voor het antwoord is 250. Let op het maximum aantal tokens voor het antwoord is 250. 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 De maximale tokenlimiet voor dit antwoord is 250. µL total volume, 20 nM p97 hexameric enzyme and 20 De maximale tokenlimiet voor dit antwoord is 250. 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 Assay:[1]
  • 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 this 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.
Animal Study:[1]
  • Animal Models

    Nu/Nu nude female mice bearing human HCT 116 colon tumor xenografts

  • Dosages

    75 mg/kg, qd

  • Administration

    p.o.

References

  • https://pubmed.ncbi.nlm.nih.gov/26565666/

Customer Product Validation

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.

Data from [ , , Cancer Res, 2018, 78(14):3809-3822 ]

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

Data from [ , , Mol Oncol, 2016, 10(10):1559-1574 ]

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.

Data from [ , , Mol Cell Proteomics, 2018, 17(7):1295-1307 ]

Sellecks CB-5083 Has Been Cited by 63 Publications

Targeting site-specific N-glycosylated B7H3 induces potent antitumor immunity [ Nat Commun, 2025, 16(1):3546] PubMed: 40229277
ATXN3 regulates lysosome regeneration after damage by targeting K48-K63-branched ubiquitin chains [ EMBO J, 2025, 10.1038/s44318-025-00517-x] PubMed: 40730717
Signal peptide-independent secretion of keratin-19 by pancreatic cancer cells [ Proc Natl Acad Sci U S A, 2025, 122(27):e2426218122] PubMed: 40591600
Localized K63 Ubiquitin Signaling Is Regulated by VCP/p97 During Oxidative Stress [ Mol Cell Proteomics, 2025, 24(3):100920] PubMed: 39880084
Pharmacological Modulation of the Unfolded Protein Response as a Therapeutic Approach in Cutaneous T-Cell Lymphoma [ Biomolecules, 2025, 15(1)76] PubMed: 39858470
In vivo manipulation of the protein homeostasis network in rhabdomyosarcoma [ Oncotarget, 2025, 16:681-696] PubMed: 40879698
CB-5083 and luteolin synergistically induce the apoptosis of bladder cancer cells via multiple mechanisms [ Toxicol Appl Pharmacol, 2025, 499:117333] PubMed: 40194745
Vitamin B2 metabolism promotes FSP1 stability to prevent ferroptosis [ bioRxiv, 2025, 2025.08.05.668752] PubMed: 40799549
Signal peptide-independent secretion of keratin-19 by pancreatic cancer cells [ bioRxiv, 2025, 2025.01.18.633717] PubMed: 39896665
TEX264 drives selective autophagy of DNA lesions to promote DNA repair and cell survival [ Cell, 2024, 187(20):5698-5718.e26] PubMed: 39265577

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.