SGC-iMLLT 是一种选择性的MLLT1/3-组蛋白相互作用抑制剂,IC50值为 0.26 μM,也是化学探针。它对 MLLT1 YEATS 域 (YD) 和 MLLT3 YD (AF9/YEATS3) 具有高结合力,Kd值分别为 0.129 和 0.077 μM。
产品描述
SGC-iMLLT is a potent and selective MLLT1/3-histone interactions inhibitor(IC50 = 0.26 μM),and is a first-in-class chemical probe displaying cellular target engagement of MLLT1(Kd = 0.129 μM) and MLLT3(Kd = 0.077 μM).
体内活性
After 60 min, SGC-iMLLT shows moderate metabolic resistance with t1/2 of 53 min and 48?% remaining, and the primary process for metabolism is N demethylation.
Cas No.
2255338-25-9
分子式
C22H24N6O
分子量
388.47
储存和溶解度
DMSO:83.33 mg/mL (214.51 mM),Need ultrasonic
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years