VCP/p97 inhibitor-1
Based on 1 publication(s) in Google Scholar
VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS).
For research use only. We do not sell to patients.
- Purity: 98.64%
- CAS No.: 2630950-38-6
- Formula: C24H26BN5O4S
- Molecular Weight:491.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) VCP/p97 inhibitor-1
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Biological Activity
54.7 nM (VCP/p97)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.8 μM
Compound: 17
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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
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[PMID: 33831696] |
| RPMI-8226 | IC50 |
0.86 μM
Compound: 17
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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
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[PMID: 33831696] |
VCP/p97 inhibitor-1 (compound 17) (3-fold serial dilutions with the highest concentration at 10 μM; 72 hours) has anti-proliferation effect with IC50s of 2.9 and 0.86 μM in A549 and RPMI8226 cells, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, RPMI8226 cells
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Concentration:3-fold serial dilutions with the highest concentration at 10 μM
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Incubation Time:72 hours
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Result:Showed anti-proliferative rates in A549 and RPMI8226 cells (IC50= 2.9 and 0.86 μM, respectively).
Chemical Information
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CAS No. 2630950-38-6
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Appearance Powder
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Molecular Weight 491.37
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Formula C24H26BN5O4S
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Color Off-white to light yellow
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SMILES
O=S(NC1=CC=CC2=C1C=C(C)N2C3=NC(CCC4)=C4C(NCC5=CC(B(O)O)=CC=C5)=N3)(C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 100 mg/mL (203.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.09 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.09 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
[1]. Zhang Y, et al. Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors. Bioorg Med Chem. 2021;38:116114. [Content Brief]
[2]. van den Boom J, et al. VCP/p97-Mediated Unfolding as a Principle in Protein Homeostasis and Signaling. Mol Cell. 2018;69(2):182-194. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0351 mL | 10.1756 mL | 20.3513 mL | 50.8782 mL |
| 5 mM | 0.4070 mL | 2.0351 mL | 4.0703 mL | 10.1756 mL | |
| 10 mM | 0.2035 mL | 1.0176 mL | 2.0351 mL | 5.0878 mL | |
| 15 mM | 0.1357 mL | 0.6784 mL | 1.3568 mL | 3.3919 mL | |
| 20 mM | 0.1018 mL | 0.5088 mL | 1.0176 mL | 2.5439 mL | |
| 25 mM | 0.0814 mL | 0.4070 mL | 0.8141 mL | 2.0351 mL | |
| 30 mM | 0.0678 mL | 0.3392 mL | 0.6784 mL | 1.6959 mL | |
| 40 mM | 0.0509 mL | 0.2544 mL | 0.5088 mL | 1.2720 mL | |
| 50 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0176 mL | |
| 60 mM | 0.0339 mL | 0.1696 mL | 0.3392 mL | 0.8480 mL | |
| 80 mM | 0.0254 mL | 0.1272 mL | 0.2544 mL | 0.6360 mL | |
| 100 mM | 0.0204 mL | 0.1018 mL | 0.2035 mL | 0.5088 mL |
VCP/p97 inhibitor-1 Related Classifications
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