2417370-67-1

2417370-67-1 structure

Name: PROTAC BRD4 Degrader-15
Chemical Name: PROTAC BRD4 Degrader-15
CAS Number: 2417370-67-1
Molecular Formula: C₅₇H₆₂F₂N₁₀O₁₀S₂
Molecular Weight: 1149.29
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2021-09-20 13:11:49
Modify Date: 2024-01-12 12:02:51
PROTAC BRD4 Degrader-15 is a potent BRD4 degrader, 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].

Name	PROTAC BRD4 Degrader-15

Description	PROTAC BRD4 Degrader-15 is a potent BRD4 degrader, 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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> PROTAC >> PROTAC Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain
Target	BRD4 BD1:7.2 nM (IC50) BRD4 BD2:8.1 nM (IC50)
In Vitro	PROTAC BRD4 Degrader-15 (compound 13) (4 h) inhibits suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 15 nM[1]. PROTAC BRD4 Degrader-15 (6 days) inhibits the proliferation of HL-60 and PC3-S1 cells, with an IC50 of 4.2 nM and 91 nM[1].
References	[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.