USP25/28-IN-2
USP25/28-IN-2 is a selectivity dual USP25/28 inhibitor with IC50 values of 0.88 and 1.1 μM, respectively. USP25/28-IN-2 modulates USP25 and USP28 activity to affect downstream pathways, modulates c-Myc oncoprotein total levels and half-life, induces apoptosis, reduces cell viability. USP25/28-IN-2 can be used for the research of colorectal carcinoma, colorectal adenocarcinoma.
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- CAS No.: 2165322-95-0
- 화학식: C17H17BrF3NO3
- 분자량:420.23
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
USP25/28-IN-2 (compound AZ2) (0.01-60 μM; 2 h) engages endogenous USP28 in HCT116 cells, with an EC50 of 18.2 μM as measured by Ub-VS probe competition[1].
USP25/28-IN-2 (0.01-60 μM; 2 h) engages endogenous USP25 in HCT116 cells, with an EC50 of 11.5 μM as measured by Ub-VS probe competition[1].
USP25/28-IN-2 (0-100 μM; 3 h) dose-dependently reduces endogenous total c-Myc protein levels in HCT116 cells after 3 h of treatment[1].
USP25/28-IN-2 (0-100 μM; 3 h) dose-dependently induces apoptosis in HCT116 cells, as measured by PARP cleavage[1].
USP25/28-IN-2 (72 h) exerts dose-dependent anti-proliferative effects in multiple cancer cell lines (including HCT116, HT29, and SW480) and tissue-matched normal cell lines, with EC50 values clustered around 20 μM in cancer cells and 28 μM in normal cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 colon carcinoma cells
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Concentration:0; 20; 40; 60; 80; 100 μM
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Incubation Time:3 h
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Result:Dose-dependently reduced endogenous total c-Myc protein levels, with complete reduction observed at the highest concentrations tested.
Left USP28 protein levels unchanged (confirming no general protein degradation).
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Cell Line:HCT116 colon carcinoma cells
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Concentration:0; 20; 40; 60; 80; 100 μM
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Incubation Time:3 h
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Result:Dose-dependently induced PARP cleavage, with cleavage most pronounced following complete down-regulation of c-Myc.
Showed no PARP cleavage at lower concentrations where c-Myc levels were not fully reduced.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Protocol for Pharmacokinetic Study
- Apoptosis Solutions
- CCK-8/WST-8 Cell Proliferation Assay
- MTT Cell Proliferation Assay
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 2165322-95-0
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분자량 420.23
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화학식 C17H17BrF3NO3
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SMILES
FC(F)(F)OC1=CC=CC(=C1)COC2=CC=C(Br)C=C2CNCCO
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
USP25/28-IN-2 Related Classifications
HY-122686 Related Classifications
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