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.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-166588 |
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| Réf. fabricant | 30116125 |
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| Nom chimique ou matériau | (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 |
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| CAS | 2669785-77-5 |
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| Quantité | 5 mg |
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| Cible | Active Degraders |
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| Formule moléculaire | C<sub>48</sub>H<sub>63</sub>N<sub>7</sub>O<sub>8</sub>S |
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| Pureté | 0.97 |
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