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Cat. No.: HY-187337

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HaloPROTAC 4

HaloPROTAC 4 is a HaloPROTAC degrader with a pIC₅₀ of 8.1 against human CRBN. HaloPROTAC 4 binds to CRBN to recruit the CUL4^CRBN E3 ubiquitin ligase complex, and covalently binds to HaloTag fusion proteins, thereby inducing proteasome-dependent degradation of HaloTag fusion proteins. HaloPROTAC 4 serves as a protein knockdown tool for chemogenetic-related studies.
(Pink: Cereblon ligand (HY-187338); Blue: E3 ligase ligand; Black: linker).

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Formule: C₄₃H₆₀ClN₅O₇
Masse moléculaire:794.42

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

HaloPROTAC 4 Chemical Structure

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Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
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Activité biologique

Description

HaloPROTAC 4 is a HaloPROTAC degrader with a pIC₅₀ of 8.1 against human CRBN. HaloPROTAC 4 binds to CRBN to recruit the CUL4^CRBN E3 ubiquitin ligase complex, and covalently binds to HaloTag fusion proteins, thereby inducing proteasome-dependent degradation of HaloTag fusion proteins. HaloPROTAC 4 serves as a protein knockdown tool for chemogenetic-related studies^[1]. (Pink: Cereblon ligand (HY-187338); Blue: E3 ligase ligand; Black: linker).

IC₅₀ & Target^[1]

Cereblon

8.1 (pIC₅₀)

Voir tous les produits spécifiques à Isoform PROTACs :

In Vitro

HaloPROTAC 4 (compound 15) binds to purified cereblon protein, with a mean pIC₅₀ of 8.1^[1].
HaloPROTAC 4 induces dose-dependent degradation of FAK-HaloTag-HiBiT in A549 cells, with a pDC₅₀ of 8.57 and a D_max of 59.5% after 24 h of incubation; in addition, the degradation of FAK-HaloTag-HiBiT depends on CRBN binding, HaloTag binding, cullin neddylation and proteasome activity^[1].
HaloPROTAC 4 induces dose-dependent degradation of endogenous MARC1-HaloTag-HiBiT and HiBiT-HaloTag-BRD4 in HEK293 cells, with a maximum degradation rate of approximately 80% after 24 h of incubation; in addition, the degradation of HiBiT-HaloTag-BRD4 shows concentration dependence^[1].

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

Chemical Information

Masse moléculaire 794.42
Formule C₄₃H₆₀ClN₅O₇
SMILES

O=C1NC(CCN1C2=CC=CC3=C2C=CN3C4CCN(CCC5CCN(C(C6=CC=C(OCCOCCOCCOCCCCCCCl)C=C6)=O)CC5)CC4)=O
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

Instruction de manipulation (2659 KB)

Références

[1]. Stevens R, et al. A Systematic Direct-to-Biology Approach Identified Potent Cereblon HaloPROTACs. ACS chemical biology. 2026 Jul 17;21(7):1798-1817. [Content Brief]

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

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HaloPROTAC 4

Voir tous les produits spécifiques à Isoform PROTACs

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

HaloPROTAC 4 Related Classifications

HY-187337 Related Classifications