JPS016
Tocris Bioscience, part of Bio-Techne | Catalog # 8083
Selective class I HDAC Degrader (PROTAC®)
Key Product Details
Description
Selective class I HDAC Degrader (PROTAC®)
Product Description
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.PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under license from the University of LeicesterProduct Specifications
Molecular Weight
898.13
Formula
C48H63N7O8S
Storage
Store at -20°C
Purity
≥97% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for JPS016
For research use only
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