1. PROTAC Stem Cell/Wnt MAPK/ERK Pathway
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  3. ERK-CLIPTAC

ERK-CLIPTAC is a ERK CLIPTAC (click chemistry-synthesized proteolysis-targeting chimera) degrader. ERK-CLIPTAC forms intracellularly via click chemistry from ERK1/2-IN-14 (HY-175578) and Tz-thalidomide (HY-101460). The formed ERK-CLIPTAC recruits the E3 ubiquitin ligase CRBN to ERK1/2, thereby inducing ubiquitination and subsequent degradation of ERK1/2. Due to its lack of cell permeability, ERK-CLIPTAC cannot induce ERK1/2 degradation in cells. ERK-CLIPTAC can be used in research related to melanoma and colorectal cancer.
(Pink: ERK1 and ERK2 Target protein ligand; Blue: Cereblon ligand (HY-101460); Black: linker).

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

ERK-CLIPTAC

ERK-CLIPTAC Chemical Structure

CAS No. : 2087490-46-6

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Description

ERK-CLIPTAC is a ERK CLIPTAC (click chemistry-synthesized proteolysis-targeting chimera) degrader. ERK-CLIPTAC forms intracellularly via click chemistry from ERK1/2-IN-14 (HY-175578) and Tz-thalidomide (HY-101460). The formed ERK-CLIPTAC recruits the E3 ubiquitin ligase CRBN to ERK1/2, thereby inducing ubiquitination and subsequent degradation of ERK1/2. Due to its lack of cell permeability, ERK-CLIPTAC cannot induce ERK1/2 degradation in cells. ERK-CLIPTAC can be used in research related to melanoma and colorectal cancer[1]. (Pink: ERK1 and ERK2 Target protein ligand; Blue: Cereblon ligand (HY-101460); Black: linker).

IC50 & Target[1]

ERK1

 

ERK2

 

Cereblon

 

In Vitro

ERK-CLIPTAC (0.1-10 μM; 18 h) lacks cell permeability and does not induce ERK1/2 degradation in A375 cells, confirming that functional ERK-CLIPTAC must form intracellularly from its precursors to elicit degradation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A375 cells (BRAFV600E mutant melanoma cells)
Concentration: Preformed ERK-CLIPTAC at 0.1-10 μM
Incubation Time: 18 h
Result: Showed no degradation of ERK1/2 across all tested concentrations of preformed ERK-CLIPTAC.
Molecular Weight

1129.65

Formula

C60H61ClN12O9

CAS No.
SMILES

O=C(NCCC#CC1=NC=CC(NC2=NC=C(C(NC3=C(NC(C=C)=O)C=CC=C3)=N2)Cl)=C1)OC4CCC5=C(C)NN=C(C5CCC4)C6=CC=C(CNC(CCCCCOC7=CC=CC(C(N8C9C(NC(CC9)=O)=O)=O)=C7C8=O)=O)C=C6

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

Purity & Documentation
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    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.

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Product Name:
ERK-CLIPTAC
Cat. No.:
HY-153735
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