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> CB-5083 [1542705-92-9]

CB-5083 [1542705-92-9]

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Referencia HY-12861-1mL

embalaje : 10mM/1mL

Marca : MedChemExpress

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Descripciòn

CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM[1].

IC50 & Target

IC50: 11 nM (p97)[1]
Cellular Effect
Cell Line Type Value Description References
A549 IC50
0.49 μM
Compound: 71
Inhibition of p97 ATPase in human A549 cells assessed as reduction in p62 protein incubated for 6 hrs by immunofluorescence assay
Inhibition of p97 ATPase in human A549 cells assessed as reduction in p62 protein incubated for 6 hrs by immunofluorescence assay
[PMID: 26565666]
A549 IC50
0.68 μM
Compound: 71
Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by Celltiter-Glo assay
Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by Celltiter-Glo assay
[PMID: 26565666]
A549 IC50
0.68 μM
Compound: 71
Inhibition of p97 ATPase in human A549 cells assessed as accumulation of K48 poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay
Inhibition of p97 ATPase in human A549 cells assessed as accumulation of K48 poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay
[PMID: 26565666]
A549 IC50
1.03 μM
Compound: 71
Inhibition of p97 ATPase in human A549 cells assessed as accumulation of CHOP poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay
Inhibition of p97 ATPase in human A549 cells assessed as accumulation of CHOP poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay
[PMID: 26565666]
A549 IC50
1.3 μM
Compound: CB-5083
Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay
[PMID: 30606672]
A549 IC50
1.7 μM
Compound: CB-5083
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 33831696]
MIA PaCa-2 EC50
0.146 μM
Compound: 4b
Antiproliferative activity against human MIAPaCa2 cells
Antiproliferative activity against human MIAPaCa2 cells
[PMID: 30830772]
RPMI-8226 IC50
0.8 μM
Compound: CB-5083
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
[PMID: 33831696]
U-87MG ATCC IC50
75.19 nM
Compound: CB5083
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer-glo luminescent assay
[PMID: 36634454]
In Vitro

CB-5083 shows cell killing potency with IC50s of 0.68, 0.68, 1.03, and 0.49 μM for lung carcinoma A549 CTG, A549 K48, A549 CHOP, and A549 p62, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CB-5083 Related Antibodies

Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (241.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4186 mL 12.0928 mL 24.1856 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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