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Cat. No.: HY-153735

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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).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 2087490-46-6
Formule: C₆₀H₆₁ClN₁₂O₉
Masse moléculaire:1129.65

Stockage:

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

Data Sheet (268 KB)

ERK-CLIPTAC Chemical Structure

CAS No.: 2087490-46-6

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

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

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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.

Chemical Information

CAS No. 2087490-46-6
Masse moléculaire 1129.65
Formule C₆₀H₆₁ClN₁₂O₉
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Lebraud H, et al. Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras. ACS Cent Sci. 2016 Dec 28;2(12):927-934. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

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MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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ERK-CLIPTAC

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