VCP/p97 IN-4
VCP/p97 IN-4 is a p97/VCP inhibitor (Kd=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
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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].
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].
VCP/p97 IN-4 (5 μM; 24 h) induces mitochondrial membrane depolarization in HCT-116 human colorectal cancer cells[1].
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].
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, MC38, SW480, A549, 95D, 4T1, NB4, and Ketr-3
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Concentration:0.19-100 μM
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Incubation Time:48 h
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Result:Potently inhibited proliferation of multiple cancer cell lines with IC50 values below 5 μM.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | AUCINF_obs | MRTINF_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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (female, 4-6 weeks old, 20-25 g, subcutaneous inoculation of MC38 colorectal cancer cells)[1]
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Dosage:30 μmol/kg
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Administration:i.p.; daily; 7 consecutive days
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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.
Chemical Information
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CAS No. 3114314-82-5
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Molecular Weight 445.55
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Formula C28H29F2N3
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SMILES
FC1=CC=C(C=C1)C(C2=CC=C(C=C2)F)CCCNC[C@@H]3CC4=C(NC5=C4C=CC=C5)CN3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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