SAG dihydrochloride 是一种有效的 Smoothened (Smo) 受体激动剂 (EC₅₀=3 nM; K_d=59 nM)。SAG dihydrochloride 可激活 Hedgehog 信号通路并抵消 Cyclopamine (HY-17024) 对 Smo 的抑制作用。

SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC 50 =3 nM; K d =59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.

Solid

EC50: 3 nM (Smo)

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.
SAG (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 (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin.
SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells.
SAG (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; 24 h) increases MDAMB231 cells migration. has not independently confirmed the accuracy of these methods.

SAG (1.0 mM) induces more osteogenesis mainly at the defect borders and a significant increase in BV/TV at the eight week timepoint in CD-1 mice.
SAG (15-20 mg/kg; i.p.) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Chen JK, et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6.
[2]. Stanton BZ, et al. A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol. 2009 Mar;5(3):154-6.
[3]. Guerrini G, et, al. Inhibition of smoothened in b

In Vitro: H₂O : 100 mg/mL (177.63 mM; Need ultrasonic)DMSO : 33.33 mg/mL (59.20 mM; Need ultrasonic)配制储备液