Product Introduction
Bioactivity


英文名: SAG dihydrochloride

描述: SAG dihydrochloride 是一种强效的 Smoothened（Smo）受体激动剂（EC 50 =3 nM；K d =59 nM）。SAG dihydrochloride 可激活刺猬信号通路并抵消环丙胺对 Smo 的抑制。

体外活性: SAG dihydrochloride (1-1000 nM; 1 h) competes for the binding of BODIPY-cyclopamine to Smo-expressing Cos-1 cells, yielding an apparent dissociation constant (Kd) of 59 nM for the SAG/Smo complex. SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM and then inhibits expression at higher concentrations.[1] SAG dihydrochloride (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin.[2] SAG dihydrochloride (250 nM; 24 and 48 h) increases CAXII mRNA expression in MDAMB231 cells at 24h in normoxic and hypoxic conditions in MDAMB231 cells. SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells.[3] SAG (250 nM; 24 h) increases MDAMB231 cells migration.[3]

体内活性: SAG dihydrochloride（15-20 mg/kg；i.p.；小鼠）主要以剂量依赖的方式在小鼠中诱导前轴多指畸形。[4] SAG dihydrochloride（1.0 mM）主要在CD-1小鼠缺陷边缘诱导更多的成骨作用，并且在第八周时显著增加BV/TV。[5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 15 mg/mL (26.64 mM)


关键字: SAG Dihydrochloride | SAG | SAG dihydrochloride

相关产品: MRT-10 | Tolnaftate | RU-SKI 43 | Taladegib | Triparanol | GSA-10 | JK184 | Ciliobrevin A | SMANT hydrochloride | Ciliobrevin D

相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Bioactive Compound Library