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JPS016

Catalog #: 8083 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
8083/5
JPS016 | CAS No. 2669785-77-5 | Active Degraders
1 Image
Description: Selective class I HDAC Degrader (PROTAC®)

Chemical Name: (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

Purity: ≥97%

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Biological Activity

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.

Technical Data

M.Wt:
898.13
Formula:
C48H63N7O8S
Solubility:
Soluble to 10 mM in DMSO
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
2669785-77-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under license from the University of Leicester

Product Datasheets

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