产品描述: | 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 |
靶点: |
EC50: 3 nM (Smo);Hedgehog/Smoothened; Smo |
体内研究: |
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. |
参考文献: |
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. Lee S, et al. Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg. 2017 Feb 13 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 |
溶解性: |
DMSO : ≥ 38 mg/mL (77.54 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.041 ml |
10.203 ml |
20.406 ml |
5 mM |
0.408 ml |
2.041 ml |
4.081 ml |
10 mM |
0.204 ml |
1.02 ml |
2.041 ml |
50 mM |
0.041 ml |
0.204 ml |
0.408 ml |
|
注意: |
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