2669785-77-5
Chemical Structure
JPS016
- CAS 番号: 2669785-77-5
- Formula:C48H63N7O8S
- Molecular Weight:898.12
InChIKey: BOXZMOCGSKLDAH-OUZJXKGJSA-N
SMILES: O=C(N(C[C@@H]1O)[C@@H](C1)C(NCC2=CC=C(C(SC=N3)=C3C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCCCCCCCCOCC(NC(C=C4)=CC=C4C(NC(C=CC=C5)=C5N)=O)=O)=O
Biological Activity: JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 reduces the viability of colon cancer cells and induces Apoptosis. JPS016 activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 is applicable to research related to colon cancer and sepsis cardiomyopathy[1][2].
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JPS016 | JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 reduces the viability of colon cancer cells and induces Apoptosis. JPS016 activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 is applicable to research related to colon cancer and sepsis cardiomyopathy. | |||||||||||||||||||||
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- [1]. Smalley JP, et al. Optimization of Class I Histone Deacetylase PROTACs Reveals that HDAC1/2 Degradation is Critical to Induce Apoptosis and Cell Arrest in Cancer Cells. J Med Chem. 2022 Apr 14;65(7):5642-5659. [Content Brief]
- [2]. Li Z, et al. PROTAC-mediated degradation of Class I HDACs by JPS016 alleviates septic cardiomyopathy via mitophagy-driven exopher formation and mitochondrial quality control. Int J Biochem Cell Biol. 2026;192:106910. [Content Brief]
Keywords
