SAG
SAG (CAS 912545-86-9) is a bioactive small molecule agonist, functioning as a potent agonist in Smoothened (SMO) receptors and exhibiting agonist activity in Hedgehog (Hh) signaling pathways. Additionally, it is capable of activating downstream Hedgehog signaling and counteracting pathway inhibition induced by cyclopamine or related antagonists.
In cell-based experimental systems, SAG demonstrates robust activation of the Hedgehog signaling pathway with an EC50 value of ( EC50 value), tested against NIH-3T3 cells and other relevant cell lines. It can also stimulate GLI-mediated transcription and promote downstream target gene expression, leading to phenotypic changes in responsive cellular assays.
In research and drug discovery applications, SAG is widely used as a molecular tool to study Hedgehog pathway activation, investigate developmental biology mechanisms, and evaluate pathway inhibitors in cellular models. The compound is also employed for in vitro and in vivo modulation of SMO receptor activity, providing insight into the functional roles of Hedgehog signaling in various physiological and pathological contexts such as embryonic development, stem cell maintenance, and tumorigenesis.
| Storage | Store at -20°C |
| M.Wt | 490.06 |
| Cas No. | 912545-86-9 |
| Formula | C28H28ClN3OS |
| Synonyms | Smoothened Agonist |
| Solubility | ≥24.5 mg/mL in DMSO; ≥16.33 mg/mL in H2O with gentle warming and ultrasonic; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CN[C@@]1([H])CC[C@@](N(C(C2=C(Cl)C3=CC=CC=C3S2)=O)CC4=CC(C5=CC=NC=C5)=CC=C4)([H])CC1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Shh-LIGHT2 cell line |
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Preparation method |
The solubility of this compound in DMSO is >24.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1~100 μM |
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Applications |
SAG induces Hh pathway activation in a mouse cultured cell with an EC50 of ~3 nM, however, the pathway activity decreases dramatically as SAG concentration surpasses 1 μM. |
| Animal experiment [2]: | |
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Animal models |
P4 wild-type mice |
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Dosage form |
SAG (20 μg/g) with prednisolone (0.67 μg/g), daily, 7 days |
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Application |
SAG at the treatment dose effectively prevented glucocorticoids-induced neonatal cerebellar developmental abnormalities in the mouse. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Chen JK, Taipale J, Young KE et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6. [2] Heine VM, Griveau A, Chapin C et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. Sci Transl Med. 2011 Oct 19;3(105):105ra104. | |
Quality Control & MSDS
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Chemical structure
