(Rac)-SAG
(Rac)-SAG is an isoform of SAG (HY-12848). 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 番号: 364590-63-6
- 分子式: C28H28ClN3OS
- 分子量:490.06
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
EC50: 3 nM (Smo)[1]
SAG (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 (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 (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin[2].
SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells[3].
SAG (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 (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 (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.
化学情報
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CAS 番号 364590-63-6
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分子量 490.06
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分子式 C28H28ClN3OS
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SMILES
O=C(C1=C(Cl)C2=CC=CC=C2S1)N(C3CCC(NC)CC3)CC4=CC=CC(C5=CC=NC=C5)=C4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
(Rac)-SAG 関連分類
HY-12848A 関連分類
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