2. PROTAC NF-κB Apoptosis
  3. PROTACs IKK Apoptosis
  4. 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)).

For research use only. We do not sell to patients.

UNC8461

UNC8461 Chemical Structure

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UNC8461 Related Antibodies

Top Publications Citing Use of Products

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IKK-α IKK-β IKK IKKε TBK1

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Description

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

 

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.

UNC8461 Related Antibodies

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.
Molecular Weight

982.91

Formula

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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UNC8461 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UNC8461UNC 8461UNC-8461PROTACsIKKApoptosisIκB kinaseI kappa B kinase A498UMRC2GAKTBK1PROTACrenal cancer cellsAURKAUMRC6cereblonAAK1Inhibitorinhibitorinhibit

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