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.
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- CAS No.: 3098437-66-9
- Formule: C31H32F2N6O3S
- Masse moléculaire:606.69
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:RPMI-8226 cell subcutaneous xenograft mice[1]
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Dosage:50, 100 mg/kg
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Administration:i.p. every other day, 23 days
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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.
Chemical Information
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CAS No. 3098437-66-9
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Masse moléculaire 606.69
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Formule C31H32F2N6O3S
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SMILES
O=C(OCC#CC1=CC(F)=C(OCC2=NN=C(S[C@H]3C=CCCC3)N2C4=CC=CN=C4)C=C1F)NC(C5)CC65CN(C)C6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)