NI 42

Names

[ Name ]:
NI 42

Biological Activity

[Description]:

NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/ 940 nM) with excellent selectivity over nonclass IV BRD proteins[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRPF1:7.9 nM (IC50)

BRPF2:48 nM (IC50)

BRPF3:260 nM (IC50)

BRPF1:40 nM (Kd)

BRPF2:210 nM (Kd)

BRPF3:940 nM (Kd)

BRD4 (BD1):4500 nM (IC50)

BRD7:82 nM (IC50)

BRD9:310 nM (IC50)

BRD9:1130 nM (Kd)

[In Vitro]

NI-42 shows IC50s of 82, 310, and 4500 nM for BRD7, BRD9, and BRD4 (BD1), respectively, and has a Kd of 1130 nM for BRD9[1].

[References]

[1]. Igoe N, et al. Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. J Med Chem. 2017 Jan 26;60(2):668-680.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₁₅N₃O₃S

[ Molecular Weight ]:
353.40

NI 42

Names

Biological Activity

Chemical & Physical Properties

Related Compounds