NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC 50 s of BRPF1/2/3=7.9/48/260 nM; K d s of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins.
性状
Solid
IC50 & Target[1][2]
BRPF1 7.9 nM (IC50) BRPF2 48 nM (IC50
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (282.97 mM; Need ultrasonic)配制储备液