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SAG dihydrochloride

Catalog No. T40465 CAS 2702366-44-5

SAG dihydrochloride, a powerful agonist of the Smoothened (Smo) receptor (EC 50 = 3 nM; Kd = 59 nM), effectively activates the Hedgehog signaling pathway. It also negates the effects of Cyclopamine inhibition on Smo.

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SAG dihydrochloride, CAS 2702366-44-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 59.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 262.00
50 mg	In stock	$ 396.00
100 mg	In stock	$ 593.00
1 mL * 10 mM (in DMSO)	In stock	$ 239.00

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Purity: 100%

Biological Description

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Description	SAG dihydrochloride, a powerful agonist of the Smoothened (Smo) receptor (EC 50 = 3 nM; Kd = 59 nM), effectively activates the Hedgehog signaling pathway. It also negates the effects of Cyclopamine inhibition on Smo.
Targets&IC50	Smo:3 nM(EC50)
In vitro	SAG dihydrochloride, at concentrations ranging from 1-1000 nM for 1 hour, competes with BODIPY-cyclopamine for binding to Smo-expressing Cos-1 cells, resulting in an apparent Kd of 59 nM for the SAG/Smo complex. At doses between 0.1 nM to 100 μM over 30 hours, it activates firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM, but suppresses expression at higher concentrations. Additionally, 100 nM of SAG dihydrochloride counteracts the inhibitory effect of ShhN-induced pathway activation by Robotnikinin. When applied at 250 nM for 24 and 48 hours, it boosts CAXII mRNA levels at 24 hours under both normoxic and hypoxic conditions, and significantly augments SMO mRNA and protein levels at 48 hours in MDAMB231 cells. Furthermore, a 24-hour exposure to 250 nM of SAG enhances migration in MDAMB231 cells.
In vivo	SAG dihydrochloride (15-20 mg/kg; i.p.; mice) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice.[4] SAG dihydrochloride (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.[5]

Molecular Weight	562.98
Formula	C28H30Cl3N3OS
CAS No.	2702366-44-5

Storage

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

References and Literature

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 breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec; 233(12): 9799-9811. 4. 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. 5. Lee S, et al. Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg. 2017 Feb 13.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

SAG dihydrochloride 2702366-44-5 GPCR/G Protein Stem Cells Hedgehog/Smoothened SAG Dihydrochloride SAG inhibitor inhibit

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