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Cat. No.: HY-174984

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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.

CAS No.: 3098437-66-9
Formula: C₃₁H₃₂F₂N₆O₃S
Molecular Weight:606.69

Storage:

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

Data Sheet (270 KB)

VCP/p97 IN-3 Chemical Structure

CAS No.: 3098437-66-9

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Fluorescent Dye

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

Biological Activity
- Description
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Caspase Isoforms :

Parmacokinetics

Species	Dose	Route	CL	V_ss	C_max	AUC_last
Mice^[1]	5 mg/kg	i.v.	4.0 L/h/kg	608 L/kg	/	/
Mice^[1]	50 mg/kg	i.p.	/	/	17.4 μM	42.0 μM·h
Mice^[1]	50 mg/kg	p.o.	/	/	0.7 μM	2.0 μM·h

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.

Chemical Information

CAS No. 3098437-66-9
Molecular Weight 606.69
Formula C₃₁H₃₂F₂N₆O₃S
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
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Green N, et al. Antitumor Efficacy of 1,2,4-Triazole-Based VCP/p97 Allosteric Inhibitors. J Med Chem. 2025 Jul 24;68(14):14465-14494. [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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Biological Activity
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- In Vivo
Chemical Information
Purity & Documentation
References

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VCP/p97 IN-3

All Caspase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

VCP/p97 IN-3 Related Classifications

HY-174984 Related Classifications