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JPS016

JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC) . JPS016 degrades class I histone deacetylase (HDAC) . JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].

Product Specifications

CAS Number

[2669785-77-5]

UNSPSC

12352005

Target

HDAC; PROTACs

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/jps016.html

Solubility

10 mM in DMSO

Smiles

O=C(N(C[C@@H]1O)[C@@H](C1)C(NCC2=CC=C(C(SC=N3)=C3C)C=C2)=O)[C@H](C(C)(C)C)NC(COCCCCCCCCCOCC(NC(C=C4)=CC=C4C(NC(C=CC=C5)=C5N)=O)=O)=O

Molecular Formula

C48H63N7O8S

Molecular Weight

898.12

References & Citations

[1]Smalley JP, et al. Optimization of Class I Histone Deacetylase PROTACs Reveals that HDAC1/2 Degradation is Critical to Induce Apoptosis and Cell Arrest in Cancer Cells. J Med Chem. 2022;65 (7) :5642-5659.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

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