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 番号: 1135195-64-0
- 分子式: C18H19N5O
- 分子量:321.38
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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] |
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.
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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.
化学情報
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CAS 番号 1135195-64-0
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分子量 321.38
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分子式 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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別名
VCP/p97-IN-PPA
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ACJI-99C 関連分類
HY-118460 関連分類
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