PROTAC USP7 Degrader-1
PROTAC USP7 Degrader-1 is a VHL-recruiting PROTAC and USP7 degrader with binding activity to both USP7 and the VHL E3 ubiquitin ligase. PROTAC USP7 Degrader-1 recruits the VHL E3 ligase to mediate the ubiquitination and subsequent proteolytic degradation of USP7.
(Pink: USP7 ligand (HY-175359); Blue: VHL ligand (HY-112078); Black: linker).
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- 화학식: C64H86N12O8S
- 분자량:1183.51
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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
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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USP7 25 nM (DC50) |
VHL |
PROTAC USP7 Degrader-1 (compound 40) (0.01-10 μM; 5-24 h) potently degrades USP7 in OCI-AML5 cells with a DC50 of 25 nM, induces significant USP7 degradation in HEK293T_GFP-USP7, MM.1S, HL60, and MOLT4 cells, inhibits OCI-AML5 cell growth, and drives selective downregulation of USP7 and its substrates in MM.1S cells[1].
PROTAC USP7 Degrader-1 (compound 40) (1 μM; 0-60 min) exhibits improved metabolic stability in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OCI-AML5, HEK293T_GFP-USP7, MM.1S, HL60, MOLT4
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Concentration:0.01-10 μM; 0.1 μM; 1 μM
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Incubation Time:5 h; 24 h
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Result:Induced 81% USP7 degradation in OCI-AML5 cells at 0.1 μM for 24 h.
Induced 38% USP7 degradation in HEK293T_GFP-USP7 cells at 0.1 μM for 24 h.
Induced 23% cell growth inhibition in OCI-AML5 cells at 0.1 μM for 24 h.
Exhibited a DC50 of 25 nM and a Dₘₐₓ of 95% for USP7 degradation in OCI-AML5 cells after 24 h treatment.
Induced significant USP7 degradation in MM.1S, HL60, and MOLT4 cells at 1 μM for 24 h.
Caused significant downregulation of USP7 and known USP7 substrates including FBXO38, TRIM27, and RNF220 in MM.1S cells at 1 μM for 5 h, with a cleaner degradation fingerprint compared to a reference compound.
Chemical Information
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분자량 1183.51
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화학식 C64H86N12O8S
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SMILES
O=C([C@H]1N(C([C@@H](NC(CCCCCOC2=CC=C(C3=C(C4=NN3C)N=CN(CC5(O)CCN(C(C[C@@H](C)C6=CC=CC=C6)=O)CC5)C4=O)C=C2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C7=CC=C(C8=C(N9CCN(CCN(C)C)CC9)N=CS8)C=C7)C
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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)
PROTAC USP7 Degrader-1 Related Classifications
HY-175358 Related Classifications
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