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Cat. No.: HY-184291

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VCP/p97 IN-4

VCP/p97 IN-4 is a p97/VCP inhibitor (K_d=14.99 μM) targeting the allosteric site of the D1-D2 domain. VCP/p97 IN-4 inhibits the ATPase activity of VCP/p97 in an ATP concentration-independent manner. VCP/p97 IN-4 induces apoptosis, autophagy, mitochondrial stress and mitochondrial membrane depolarization. VCP/p97 IN-4 inhibits the growth of patient-derived colorectal cancer organoids and exhibits in vivo efficacy in a colorectal cancer xenograft mouse model. VCP/p97 IN-4 can be used for the research of colorectal cancer.

For research use only. We do not sell to patients.

CAS No.: 3114314-82-5
Formula: C₂₈H₂₉F₂N₃
Molecular Weight:445.55

Storage:

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

VCP/p97 IN-4 Chemical Structure

CAS No.: 3114314-82-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
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Biological Activity

Description

In Vitro

Anti-cancerApoptosisAutophagyMitochondrial Oxidative PhosphorylationOthers

Anti-cancer

VCP/p97 IN-4 (0.19-100 μM; 48 h) potently inhibits proliferation of multiple cancer cell lines with IC₅₀ values below 5 μM^[1].
VCP/p97 IN-4 (120 h) completely inhibits the growth of patient-derived colorectal cancer organoids (KOCO-092) with an IC₅₀ of 5.35 μM^[1].

Apoptosis

VCP/p97 IN-4 (10 μM; 24 h) induces apoptosis in HCT-116 human colorectal cancer cells, increasing total apoptosis rates via elevated late apoptotic cell populations^[1].

Apoptosis

Autophagy

VCP/p97 IN-4 (5 μM; 24 h) upregulates autophagy markers (LC3-II, p62) and activates caspase-3-mediated apoptosis in HCT-116 human colorectal cancer cells^[1].

Mitochondrial Oxidative Phosphorylation

VCP/p97 IN-4 (5 μM; 24 h) induces mitochondrial membrane depolarization in HCT-116 human colorectal cancer cells^[1].

Others

VCP/p97 IN-4 (compound 10a) non-competitively inhibits p97/VCP ATPase activity with an IC₅₀ of 1.04 μM, maintaining efficacy independent of ATP concentration^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HCT-116, MC38, SW480, A549, 95D, 4T1, NB4, and Ketr-3
Concentration:

0.19-100 μM
Incubation Time:

48 h
Result:

Potently inhibited proliferation of multiple cancer cell lines with IC₅₀ values below 5 μM.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_last	AUC_{INF_obs}	MRT_{INF_obs}
Mice^[1]	13.4 mg/kg	p.o.	25.0 h	1 h	44.9 ng/mL	780 ng·h/mL	961 ng·h/mL	36.8 h

In Vivo

Anti-cancerInnate Immunity

Anti-cancer

Innate Immunity

VCP/p97 IN-4 (30 μmol/kg; i.p.; daily; 7 consecutive days) achieves 55% tumor growth inhibition in MC38 colorectal cancer xenograft mice, accompanied by measurable liver, thymic, and hematologic toxicity^[1].

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

Animal Model:

C57BL/6N (female, 4-6 weeks old, 20-25 g, subcutaneous inoculation of MC38 colorectal cancer cells)^[1]
Dosage:

30 μmol/kg
Administration:

i.p.; daily; 7 consecutive days
Result:

Achieved 55% tumor growth inhibition rate.
Reduced mean final tumor weight to 0.45 g compared to control's 1.00 g.
Significantly reduced body weight compared to control group.
Significantly increased serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels.
Showed no changes in kidney function markers (creatinine, urea).
Significantly reduced thymus/body weight ratio.
Decreased neutrophil counts.

Related Protocols :

Chemical Information

CAS No. 3114314-82-5
Molecular Weight 445.55
Formula C₂₈H₂₉F₂N₃
SMILES

FC1=CC=C(C=C1)C(C2=CC=C(C=C2)F)CCCNC[C@@H]3CC4=C(NC5=C4C=CC=C5)CN3
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]. Li Y, et al.. A novel non-competitive p97/VCP inhibitor induces apoptosis and autophagy to suppress colorectal cancer growth. European journal of medicinal chemistry. 2026 Oct 05;315:118986. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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