ZM 39923 HCl 是一种JAK3抑制剂,pIC50值为 7.1。它也抑制组织型转谷氨酞胺酶 (TGM2) 的活性,IC50值为 10 nM。
产品描述
ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.
体外活性
The selectivity of Rotigotine for D3 (pKi 9.2) receptors is higher 10-fold than D2/D4/D5 (pKi 8.5-8.0) and 100-fold than D1 receptors (pKi 7.2). Rotigotine (10 μM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. In functional studies, Rotigotine behaves as a full agonist at all dopamine receptors but notably, the potency for stimulation of D1 receptors is similar to that for D2/D3 receptors (pEC50 respectively: 9.0, 9.4-8.6, 9.7). Rotigotine (0.01 μM) slightly protects dopaminergic neurons against MPP+ toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone.
Cas No.
1021868-92-7
分子式
C23H26ClNO
分子量
367.92
别名
ZM 39923 HCl;JAK3 Inhibitor IV
储存和溶解度
H2O:<1 mgml
Ethanol:8 mg/mL (21.74 mM)
DMSO:28 mg/mL (76.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years