SAG 

SAG (GMP) is SAG (HY-12848) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. SAG is a potent Smoothened (Smo) receptor agonist (EC₅₀=3 nM; K_d=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo^[1][2][3].

SAG (GMP) (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 (GMP) (1-1000 nM; 1 h) competes for the binding of BODIPY-cyclopamine to Smo-expressing Cos-1 cells, yielding an apparent dissociation constant (K_d) of 59 nM for the SAG/Smo complex^[1].
SAG (GMP) (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin^[2].
SAG (GMP) (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells^[3].
SAG (GMP) (250 nM; 24 and 48 h) increases CAXII mRNA expression in MDAMB231 cells at 24h in normoxic and hypoxic conditions in MDAMB231 cells^[3].
SAG (GMP) (250 nM; 24 h) increases MDAMB231 cells migration^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SAG (GMP) (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^[4].
SAG (GMP) (15-20 mg/kg; i.p.) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

490.06

C₂₈H₂₈ClN₃OS

912545-86-9

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [3]. Guerrini G, et, al. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec; 233(12): 9799-9811.  [Content Brief]

  [4]. Lee S, et al. Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg. 2017 Feb 13.  [Content Brief]

  [5]. Fish EW, et al. Preaxial polydactyly following early gestational exposure to the smoothened agonist, SAG, in C57BL/6J mice. Birth Defects Res A Clin Mol Teratol. 2016 Nov 1 .  [Content Brief]