SAG
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SAG is a synthetic chlorobenzothiophene-containing Hh pathway agonist that regulates smo activity. It is a SMO agonist at EC50 of 3 nM and but inhibits hedgehog signaling at >1 μM. [1]
Smoothened (SMO) is a GPCR-like receptor that mediates hedgehog signaling with Patched to regulate gene expression through the Gli transcription factors. It is plays an important role for embryogenesis and adults tissue homeostasis
In a mouse cultured cell assay (Shh-LIGHT2), SAG induces pathway activation (EC50 ≈3 nM). It differs in that pathway activity decreases dramatically as SAG concentration surpasses 1 μM. [1] SAG binds directly to the SMO heptahelical bundle. SAG dose dependently blocks this association and produces apparent dissociation constant (KD) of 59 nM for the SAG/SMO complex. [2]
SAG also antagonizes GC’s antiproliferative effects in CGNP P4 wild-type mice primary cultures. At 15-240 nM, SAG prevents the neurotoxic effects of glucocorticoids without interfering with the beneficial effects of glucocorticoids on lung maturation. [2]
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.
| Storage | Store at -20°C |
| M.Wt | 490.06 |
| Cas No. | 912545-86-9 |
| Formula | C28H28ClN3OS |
| Solubility | ≥24.5mg/mL in DMSO, ≥16.3mg/mL in H2O with ultrasonic and warming |
| 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[[email protected]@]1([H])CC[[email protected]@](N(C(C2=C(Cl)C3=CC=CC=C3S2)=O)CC4=CC(C5=CC=NC=C5)=CC=C4)([H])CC1 |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
| 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
