2. Cell Cycle/DNA Damage Apoptosis Autophagy
  3. p97 Caspase p62
  4. VCP/p97 IN-3

VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC50 of 9 nM and the mutant VCP proteins with IC50 of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma.

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

VCP/p97 IN-3 Chemical Structure

VCP/p97 IN-3 Chemical Structure

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VCP/p97 IN-3 Related Antibodies

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Description

VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC50 of 9 nM and the mutant VCP proteins with IC50 of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma[1].

In Vivo

VCP/p97 IN-3 (Compound 38) (50-100 mg/kg, i.p., every other day, 23 days) inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models[1].

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

Animal Model: RPMI-8226 cell subcutaneous xenograft mice[1]
Dosage: 50, 100 mg/kg
Administration: i.p. every other day, 23 days
Result: Increased the ubiquitin of K48 and the level of cleaved caspase-3.
Activated endoplasmic reticulum (ER)-stress and the UPR, as assessed by increases in phosphorylated-eIF2α (p-eIF2α), activation transcription factor 4 (ATF4),74 and glucose-regulated protein (BiP/GRP78).
Activated the DNA damage response as observed from the 2.5-fold increase in phosphorylated Histone 2A (H2A.X).
Reduced p62 levels.
Showed a TGI of 73% on day 23.
Suffered a mean 10% loss in body weight.
Molecular Weight

606.69

Formula

C31H32F2N6O3S
SMILES

O=C(NC1CC2(C1)CN(C)C2)OCC#CC3=CC(F)=CC(OCC4=NN=C(N4C5=CC=CN=C5)S[C@@H]6CCCC=C6)=C3F
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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VCP/p97 IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VCP/p97 IN-3p97Caspasep62VCPCdc48Sequestosome-1SQSTM1RPMI-8226 cellsVCP/p97multiple myelomacaspase-3ER-stressInhibitorinhibitorinhibit

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