SAG is a potent, selective, and cell-permeable small-molecule agonist of the Hedgehog pathway. It modulates the coupling of Smo with its downstream effector by interacting with the Smo heptahelical domain (KD = 59 nM). SAG induces Hedgehog pathway activation with an EC50 of ~3 nM in NIH 3T3-derived Shh-LIGHT2 cells and counteracts Cyclopamine-KAAD inhibition of Smo. It was reported that SAG acts as an activator at low concentrations and as an inhibitor at high concentrations (>1 µM). In recent studies, SAG was shown to prevent glucocorticoid-induced neonatal cerebellar injury, and trigger rapid metabolic rewiring via AMPK.
CAS Number: 912545-86-9
Molecular Weight: 490.06
Related CAS Number:
2095432-58-7 (SAG HCl)
2109424-53-3 (SAG(trans-cis) HCl)
Chemical Name: 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
Appearance: Powder Solid
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 50 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Powder: 4oC 1 year
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: DMSO: 4oC 3 month
Drug Formulation: To be determined
HS Tariff Code: 38200
How to use
SAG was used at 200 nM to induce Hh pathway activation.
- Frank-Kamenetsky M, et al. Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists. (2002) Journal of Biology (1): 10.2-10.19.
- Chen JK, et al. Small molecule modulation of Smoothened activity.(2002) Proc Natl Acad Sci U S A. 99(22):14071-6.
- Chen W, et al. Activity-dependent internalization of smoothened mediated by beta-arrestin 2 and GRK2. (2004) Science. 306(5705):2257-60.
- Dyer LA, et al. BMP signaling modulates hedgehog-induced secondary heart field proliferation. (2010) Dev Biol. 348(2):167-76.
- Heine VM, et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. (2011) Sci Transl Med. 3(105).
- eperino R, et al. Hedgehog partial agonism drives Warburg-like metabolism in muscle and brown fat. (2012) Cell. 151(2):414-26.
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