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Referencia número: HY-183100

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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)).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₄₆H₆₀BrN₇O₁₂
Peso molecular:982.91

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

UNC8461 Chemical Structure

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Descripciòn

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^[1]. (Pink: TBK1 ligand (HY-183099); Blue: Cereblon ligand (HY-W586822); Black: linker (HY-23105)).

IC₅₀ & Target^[1]

Cereblon

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In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

UMRC6, A498, UMRC2, 769-P
Concentration:

1 μM
Incubation Time:

4, 24 h
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

Peso molecular 982.91
Fòrmula C₄₆H₆₀BrN₇O₁₂
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Liao C, et al. Selective degradation of TBK1 uncovers mechanistic insights into blocking ccRCC progression. Cell Chem Biol. 2026;33(4):461-473.e7. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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UNC8461

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas IKK

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

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UNC8461 Related Classifications

HY-183100 Related Classifications