(Rac)-SAG 

(Rac)-SAG is an isoform of SAG (HY-12848). 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].

EC50: 3 nM (Smo)^[1]

SAG (0.1 nM-100 μM；30 h) 在 Shh-LIGHT2 细胞中诱导萤火虫荧光素酶表达，EC₅₀ 为 3 nM，然后在更高浓度下抑制表达^[1]。
SAG (1-1000 nM；1 h) 竞争 BODIPY-cyclopamine 与表达 Smo 的 Cos-1 细胞 SAG/Smo 复合物的结合，产生表观解离常数 (K_d) 为 59 nM^[1]。
SAG (100 nM) 抑制 ShhN 诱导的 Robotnikinin 通路激活的抑制作用^[2]。
SAG (250 nM；48 h) 显著增加 MDAMB231 细胞中 SMO mRNA 和蛋白的表达^[3]。
SAG (250 nM；24 和 48 h) 增加 CAXII MDAMB231 细胞在含氧量正常和低氧条件下 24 h 的 mRNA 表达^[3]。
SAG (250 nM；24 h) 增加 MDAMB231 细胞迁移^[3]。

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

在 CD-1 小鼠中，SAG (1.0 mM) 主要在缺损边界诱导更多的成骨，并在八周时间点显著增加 BV/TV^[4]。
SAG (15-20 mg/kg；ip) 在小鼠中以剂量依赖性方式普遍诱导轴前多指畸形^[5]。

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

490.06

C₂₈H₂₈ClN₃OS

364590-63-6

Room temperature in continental US; may vary elsewhere.

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

• [1]. 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]

  [2]. 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]

  [3]. 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]

  [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]