PROTAC BRD4 Degrader-15

PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1].

Product Specifications

CAS Number

[2417370-67-1]

UNSPSC

12352005

Target

Epigenetic Reader Domain; PROTACs

Type

Reference compound

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-brd4-degrader-15.html

Solubility

10 mM in DMSO

Smiles

O=C1C2=C3C(C4=CC(CS(C)(=O)=O)=C(C(NCCOC5=CC(CCOCC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)=O)=O)=CC(N)=C5)=O)C=C4N(C9=C(C=C(C=N9)F)F)CC3=CN2)=CN1C

Molecular Formula

C57H62F2N10O10S2

Molecular Weight

1149.29

References & Citations

[1]Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64 (5) :2576-2607.