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; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.
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- CAS No.: 912545-86-9
- 화학식: C28H28ClN3OS
- 분자량:490.06
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C3H 10T1/2 | EC50 |
0.13 μM
Compound: SAG
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Agonist activity at Smo in mouse C3H10T1/2 cells assessed as induction of cell differentiation into osteoblast incubated for 6 days by alkaline phosphatase assay
Agonist activity at Smo in mouse C3H10T1/2 cells assessed as induction of cell differentiation into osteoblast incubated for 6 days by alkaline phosphatase assay
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[PMID: 27429255] |
| HUVEC | IC50 |
22 μM
Compound: 10a
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Cytotoxicity against HUVEC after 24 hrs by WST-1 assay
Cytotoxicity against HUVEC after 24 hrs by WST-1 assay
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[PMID: 22985958] |
| Shh Light II | EC50 |
8.8 nM
Compound: 10a
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Activation of Shh pathway in mouse Shh-Light II cells assessed as induction of gli1 expression after 48 hrs by renilla luminescence assay
Activation of Shh pathway in mouse Shh-Light II cells assessed as induction of gli1 expression after 48 hrs by renilla luminescence assay
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[PMID: 22985958] |
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 (Kd) 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) (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.
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Animal Model:Pregnant C57BL/6J mice[5]
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Dosage:15, 17, 20 mg/kg
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Administration:A single i.p.
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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.
Chemical Information
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CAS No. 912545-86-9
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분자량 490.06
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화학식 C28H28ClN3OS
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SMILES
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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SAG (GMP) Related Classifications
HY-12848G Related Classifications
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