INDY 是 DYRK1A 和 DYRK1B 的 ATP 竞争性抑制剂,IC50 分别为 0.24 μM 和 0.23 μM,对 DYRK1A ATP 口袋的 Ki 为 0.18 μM。
产品描述
INDY is an ATP-competitive inhibitor of Dyrk1A and Dyrk1B with IC50s of 0.24 μM and 0.23 μM and a Ki of 0.18 μM for Dyrk1A ATP pocket, respectively.
体外活性
INDY effectively rescues the repressed NFAT signaling induced by Dyrk1A overexpression. In COS7 cells transfected with either EGFP-Dyrk1A or EGFP-tau, INDY mildly inhibits tau-phosphorylation at the dose of 3 μM, and inhibits nearly completely at the dose of 30 μM[1].
体内活性
In the Xenopus embryo, ProINDY (2.5 μM) recoveres normal development apparently[1].
Cas No.
1169755-45-6
分子式
C12H13NO2S
分子量
235.3
储存和溶解度
DMSO:5 mg/mL (21.25 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years