1. Cell Cycle/DNA Damage
  2. p97
  3. ACJI-99C

ACJI-99C (VCP/p97-IN-PPA) is a selective covalent p97/VCP ATPase inhibitor with an IC50 value of 0.6 μM. ACJI-99C binds with p97 active site residues to block ATPase activity. ACJI-99C irreversibly blocks degradation of p97-dependent protein in cells. ACJI-99C inhibits proliferation of cancer cells, including p97 inhibitor-resistant lines. ACJI-99C can be used for the research of colorectal cancer.

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

ACJI-99C

ACJI-99C Chemical Structure

CAS No. : 1135195-64-0

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Description

ACJI-99C (VCP/p97-IN-PPA) is a selective covalent p97/VCP ATPase inhibitor with an IC50 value of 0.6 μM. ACJI-99C binds with p97 active site residues to block ATPase activity. ACJI-99C irreversibly blocks degradation of p97-dependent protein in cells. ACJI-99C inhibits proliferation of cancer cells, including p97 inhibitor-resistant lines. ACJI-99C can be used for the research of colorectal cancer[1].

In Vitro

ACJI-99C (Compound 18) (60 min) potently and selectively inhibits wild-type human p97 ATPase activity via covalent targeting of Cys522, with an IC50 of 0.62 μM, while showing drastically reduced activity against p97 Cys522 mutants, wild-type yeast Cdc48, hamster NSF, and human 19S ATPase[1].
ACJI-99C (120 min) selectively and irreversibly inhibits p97-dependent protein degradation in HeLa cells, with an IC50 of 1.6 μM for UbG76V-GFP degradation, and 22-fold lower activity against p97-independent ODD-Luc degradation[1].
ACJI-99C (48 h) inhibits proliferation of HCT116, HeLa, and RPMI8226 cancer cell lines with IC50 values ranging from 2.7 μM to 6.1 μM, and retains comparable activity against CB-5083-resistant and NMS-873 (HY-15713)-resistant HCT116 cell lines[1].
ACJI-99C (10 μM; 60-120 min) blocks degradation of the ERAD substrate TCRα-GFP in HEK293 cells after 60 and 120 minutes of incubation[1].
ACJI-99C (15-30 μM; 6 h) alters the abundance of p97-interacting proteins and induces enrichment of p97-related functional pathways in HCT116 cells, with concentration-dependent changes in key proteins like SQSTM1 and GOLGA3[1].
ACJI-99C (5-50 μM; 30 min) does not inhibit human 26S proteasome activity[1].

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

Western Blot Analysis[1]

Cell Line: TCRα-GFP-expressing HEK293 cells
Concentration: 10 μM
Incubation Time: 60 min, 120 min
Result: Blocked degradation of TCRα-GFP, with GFP levels remaining stable after 60 and 120 minutes.
Molecular Weight

321.38

Formula

C18H19N5O

CAS No.
SMILES

O=C(C=C)NC1=NC=NC2=C1C(=NN2C(C)(C)C)C=3C=CC=CC3

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Purity & Documentation
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  • 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.

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ACJI-99C
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HY-118460
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