JPS016

Name: JPS016
Brand: Tocris Bioscience
SKU: 8083

Tocris Bioscience, part of Bio-Techne | Catalog # 8083

COA / SDS

Selective class I HDAC Degrader (PROTAC®)

Key Product Details

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% (HPLC)
Molecular Weight:	898.13

View Full Technical Details for JPS016

Technical Data
Citations

Biological Activity for JPS016

JSP016 is a selective Degrader (PROTAC^®) and inhibitor of class I HDACs (DC₅₀ values are 530 nM and 550 nM for HDAC3 and HDAC1; D_max 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.

Licensing Information

Sold under license from the University of Leicester

Technical Data for JPS016

M. Wt	898.13
Formula	C₄₈H₆₃N₇O₈S
Storage	Store at -20°C
Purity	≥97% (HPLC)
CAS Number	2669785-77-5
PubChem ID	163322304
InChi Key	BOXZMOCGSKLDAH-OUZJXKGJSA-N
Smiles	NC(C=CC=C1)=C1NC(C(C=C2)=CC=C2NC(COCCCCCCCCCOCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(NCC4=CC=C(C5=C(C)N=CS5)C=C4)=O)=O)=O)=O)=O

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.

Solubility for JPS016

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	8.98	10

Preparing Stock Solutions for JPS016

The following data is based on the product molecular weight 898.13.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	11.13 mL	55.67 mL	111.34 mL
0.5 mM	2.23 mL	11.13 mL	22.27 mL
1 mM	1.11 mL	5.57 mL	11.13 mL
5 mM	0.22 mL	1.11 mL	2.23 mL

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References for JPS016

References are publications that support the biological activity of the product.

Smalley Optimization of class I hstone deacetylase PROTACs reveals that HDAC1/2 degradation is critical to induce apoptosis and cell arrest in cancer cells. J.Med.Chem. 2022 PMID: 35293758