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).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C43H60ClN5O7
- 分子量:794.42
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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Cereblon 8.1 (pIC50) |
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.
化学情報
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分子量 794.42
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)