VCP/p97 inhibitor-1

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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.

VCP/p97 inhibitor-1 Chemical Structure

CAS No. : 2630950-38-6

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

54.7 nM (VCP/p97)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.8 μM Compound: 17	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]
RPMI-8226	IC₅₀	0.86 μM Compound: 17	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]

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:	A549, RPMI8226 cells
Concentration:	3-fold serial dilutions with the highest concentration at 10 μM
Incubation Time:	72 hours
Result:	Showed anti-proliferative rates in A549 and RPMI8226 cells (IC₅₀= 2.9 and 0.86 μM, respectively).

Molecular Weight

491.37

Formula

C₂₄H₂₆BN₅O₄S

CAS No.

2630950-38-6

SMILES

O=S(NC1=CC=CC2=C1C=C(C)N2C3=NC(CCC4)=C4C(NCC5=CC(B(O)O)=CC=C5)=N3)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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]