UNC8461
UNC8461 is a PROTAC and is negative control CRBN-recruiting PROTAC analog of UNC8209 (HY-183098). UNC8461 features a methyl group substitution on its CRBN ligand to disrupt CRBN binding. UNC8461 fails to reduce TBK1, AAK1, GAK, and AURKA protein levels in renal cancer cells. UNC8461 does not suppress 3-D soft agar colony formation in renal cancer cells, and exerts modest, partial inhibition on colony formation in some renal cancer cells.
(Pink: TBK1 ligand (HY-183099); Blue: Cereblon ligand (HY-W586822); Black: linker (HY-23105)).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- 화학식: C46H60BrN7O12
- 분자량:982.91
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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Cereblon |
UNC8461 (1 μM; 4-24 h) does not induce degradation of TBK1, AAK1, GAK, or AURKA in UMRC6, A498, UMRC2, or 769-P ccRCC cells[1].
UNC8461 (1 μM; 4-6 weeks) shows only modest, partial inhibition of colony formation in 769-P, A498, UMRC6, UMRC2, 786-O, and Caki-1 ccRCC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:UMRC6, A498, UMRC2, 769-P
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Concentration:1 μM
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Incubation Time:4, 24 h
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Result:Failed to reduce TBK1 protein levels in UMRC6, A498, UMRC2, and 769-P cells at both 4-hour and 24-hour timepoints.
Had no effect on reducing the abundance of AAK1, GAK, or AURKA proteins in UMRC6 and A498 cells after 24-hour incubation.
Chemical Information
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분자량 982.91
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화학식 C46H60BrN7O12
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SMILES
CN(C(C1CCC1)=O)CCCNC2=NC(NC3=CC=C(C=C3)OCCOCCOCCOCCOCCOCCCOC4=CC=CC5=C4C(N(C5=O)C6CCC(N(C)C6=O)=O)=O)=NC=C2Br
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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)