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Referencia número: 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).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₄₃H₆₀ClN₅O₇
Peso molecular:794.42

Almacenamiento:

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

HaloPROTAC 4 Chemical Structure

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Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
Chemical Information
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Actividad biológica

Descripciòn

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)

Ver todos los productos específicos de isoformas 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

Peso molecular 794.42
Fòrmula C₄₃H₆₀ClN₅O₇
SMILES

O=C1NC(CCN1C2=CC=CC3=C2C=CN3C4CCN(CCC5CCN(C(C6=CC=C(OCCOCCOCCOCCCCCCCl)C=C6)=O)CC5)CC4)=O
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]. 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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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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HaloPROTAC 4

Ver todos los productos específicos de isoformas PROTACs