SAG dihydrochloride

Research use only, not for human use.

SAG dihydrochloride, a powerful agonist of the Smoothened (Smo) receptor (EC 50 = 3 nM; Kd = 59 nM), effectively activates the Hedgehog signaling pathway.

SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of 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.

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.Animal Model:Pregnant C57BL/6J mice Dosage:15, 17, 20 mg/kg Administration:A single i.p.Result:Effective in ca. 80% of the embryos and increased Gli1 and Gli2 mRNA expression in the limb bud, with Gli1 mRNA being the most upregulated at the dose of 20 mg/kg.

——

GPCR/G Protein

Hedgehog (Hh)

Hedgehog/Smoothened

——

——

2702366-44-5

562.98

C28H30Cl3N3OS

>98% (HPLC)

In Vitro:?H2O : 100 mg/mL (177.63 mM; Ultrasonic)DMSO : 33.33 mg/mL (59.20 mM; Ultrasonic )

O=C(C1=C(C2=CC=CC=C2S1)Cl)N([C@@H]3CC[C@H](CC3)NC)CC4=CC(C5=CC=NC=C5)=CC=C4.Cl.Cl

——

(-20℃)

With Ice Pack

≥ 2 years