SAG二盐酸盐 T40465

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

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途