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Tocris Bioscience™ JPS016

Catalog No. 80835
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80-835 5 mg
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Catalog No. 80-835 Supplier Tocris Bioscience™ Supplier No. 8083/5
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Description

Selective class I HDAC Degrader (PROTAC™)

JSP016 is a selective Degrader (PROTAC™) and inhibitor of class I HDACs (DC50 values are 530 nM and 550 nM for HDAC3 and HDAC1; Dmax is 77%, 66% and 45% at HDAC1, 3 and 2; IC50 values are 380 nM, 570 nM and 820 nM at HDAC3, 1 and 2). Comprises a benzamide-based compound joined by a linker to a Von Hippel Lindau (VHL) E3 ligase ligand. JPS016 treatment up- or down-regulates nearly 4000 differentially expressed genes, arrests cells at sub-G1 phase and promotes apoptosis in HCT116 cells.

Specifications

Chemical Name or Material (2S,4R)-1-((S)-2-(2-((9-(2-((4-((2-Aminophenyl)carbamoyl)phenyl)amino)-2-oxoethoxy)nonyl)oxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CAS 2669785-77-5
Quantity 5 mg
Target Active Degraders
Molecular Formula C48H63N7O8S
Purity 0.97
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