Bromodomain IN-2

Names

[ CAS No. ]:
2445335-77-1

[ Name ]:
Bromodomain IN-2

Biological Activity

[Description]:

BD-IN-1 is a pan bromodomain (BD) inhibitor with KD values of 250, 420, 130, 430, 67, 240, 970 nM for BRD4(1), CBP, BRPF1B, BRD7, BRD9, BRDT(1), CECR2 respectively. BD-IN-1 shows antiproliferative activity[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRD4(1):250 nM (Kd)

BRPF1b:130 nM (Kd)

BRD7:430 nM (Kd)

BRD9:67 nM (Kd)

BRDT (1):240 nM (Kd)

CBP:420 nM (Kd)

CECR2:970 nM (Kd)


[In Vitro]

BD-IN-1 (compound 3; 0-100 µM) 具有抗增殖活性，对 SNB-75、UO-31、CAKI-1 细胞和 DU-145、SW-620、NCI-H460 细胞 的 GI50 值分别为 182、479、708 nM 和 13.2、12.0、10.2 µM[1]。

[References]

[1]. Warstat R, et al. A novel pan-selective bromodomain inhibitor for epigenetic drug design. Eur J Med Chem. 2023 Mar 5;249:115139.  

Chemical & Physical Properties

[ Molecular Formula ]:
C16H17ClN2O

[ Molecular Weight ]:
288.77

Related Compounds

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