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 CUL4CRBN 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).
For research use only. We do not sell to patients.
- CAS No.: 3140110-11-5
- Formula: C43H60ClN5O7
- Molecular Weight:794.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
Cereblon 8.1 (pIC50) |
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 Dmax 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. Further protocols information, click here.
Chemical Information
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CAS No. 3140110-11-5
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Molecular Weight 794.42
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Formula C43H60ClN5O7
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SMILES
O=C1NC(CCN1C2=CC=CC3=C2C=CN3C4CCN(CCC5CCN(C(C6=CC=C(OCCOCCOCCOCCCCCCCl)C=C6)=O)CC5)CC4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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RNA interference technology
RNA interference (RNAi) is a cellular mechanism that inhibits gene expression by suppressing gene transcription or activating RNA degradation. This mechanism was discovered in plants in 1998 by Andrew Fire and Craig Mello. Today, this phenomenon can be observed in almost all eukaryotes, including protozoa, flies, nematodes, insects, parasites, and mammals.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HaloPROTAC 4 Related Classifications
HY-187337 Related Classifications
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