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.
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- CAS. Nr.: 1135195-64-0
- Formel: C18H19N5O
- Molecular Weight:321.38
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
2.7 μM
Compound: 18; PPA
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Antiproliferative activity against human HCT-116 cells after 48 hrs by celltiter-glo luminescence assay
Antiproliferative activity against human HCT-116 cells after 48 hrs by celltiter-glo luminescence assay
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[PMID: 33476933] |
| HeLa | IC50 |
35 μM
Compound: 18; PPA
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Inhibition of proteasomal turnover of p97-independent ODD-luciferase reporter substrate in human HeLa cells incubated for 120 mins by luciferase reporter gene assay
Inhibition of proteasomal turnover of p97-independent ODD-luciferase reporter substrate in human HeLa cells incubated for 120 mins by luciferase reporter gene assay
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[PMID: 33476933] |
| HeLa | IC50 |
6.1 μM
Compound: 18; PPA
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Antiproliferative activity against human HeLa cells after 48 hrs by celltiter-glo luminescence assay
Antiproliferative activity against human HeLa cells after 48 hrs by celltiter-glo luminescence assay
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[PMID: 33476933] |
| RPMI-8226 | IC50 |
3.4 μM
Compound: 18; PPA
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Antiproliferative activity against human RPMI-8226 cells after 48 hrs by celltiter-glo luminescence assay
Antiproliferative activity against human RPMI-8226 cells after 48 hrs by celltiter-glo luminescence assay
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[PMID: 33476933] |
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. Further protocols information, click here.
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Cell Line:TCRα-GFP-expressing HEK293 cells
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Concentration:10 μM
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Incubation Time:60 min, 120 min
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Result:Blocked degradation of TCRα-GFP, with GFP levels remaining stable after 60 and 120 minutes.
Chemical Information
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CAS. Nr. 1135195-64-0
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Molecular Weight 321.38
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Formel C18H19N5O
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SMILES
O=C(C=C)NC1=NC=NC2=C1C(=NN2C(C)(C)C)C=3C=CC=CC3
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Synonyms
VCP/p97-IN-PPA
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
ACJI-99C Related Classifications
HY-118460 Related Classifications
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