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SAG, Hedgehog Agonist

SAG, Hedgehog Agonist

$129.00
A potent, selective, and cell-permeable small-molecule agonist of the Hedgehog pathway.
Catalog No. Unit Price Qty
M60081-2s 2 mg solid $129.00
M60081-2 10 mM DMSO (0.408 mL) $129.00

Details

Product Information
Molecular Weight: 490.06
Formula: C28H28ClN3OS
Purity: ≥ 98%
CAS#: 364590-63-6
Solubility: DMSO up to 50 mM
Chemical Name: 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

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.


How to Use:

  • In vitro: SAG was used at 200 nM to induce Hh pathway activation.
  • In vivo: n/a

Reference:

  1. 1. 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.
  2. 2. Chen JK, et al. Small molecule modulation of Smoothened activity.(2002) Proc Natl Acad Sci U S A. 99(22):14071-6.
  3. 3. Chen W, et al. Activity-dependent internalization of smoothened mediated by beta-arrestin 2 and GRK2. (2004) Science. 306(5705):2257-60.
  4. 4. Dyer LA, et al. BMP signaling modulates hedgehog-induced secondary heart field proliferation. (2010) Dev Biol. 348(2):167-76.
  5. 5. Heine VM, et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. (2011) Sci Transl Med. 3(105).
  6. 6. Teperino R, et al. Hedgehog partial agonism drives Warburg-like metabolism in muscle and brown fat. (2012) Cell. 151(2):414-26.



Products are for research use only. Not for human use.



Description

Details

Product Information
Molecular Weight: 490.06
Formula: C28H28ClN3OS
Purity: ≥ 98%
CAS#: 364590-63-6
Solubility: DMSO up to 50 mM
Chemical Name: 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

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.


How to Use:

  • In vitro: SAG was used at 200 nM to induce Hh pathway activation.
  • In vivo: n/a

Reference:

  1. 1. 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.
  2. 2. Chen JK, et al. Small molecule modulation of Smoothened activity.(2002) Proc Natl Acad Sci U S A. 99(22):14071-6.
  3. 3. Chen W, et al. Activity-dependent internalization of smoothened mediated by beta-arrestin 2 and GRK2. (2004) Science. 306(5705):2257-60.
  4. 4. Dyer LA, et al. BMP signaling modulates hedgehog-induced secondary heart field proliferation. (2010) Dev Biol. 348(2):167-76.
  5. 5. Heine VM, et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. (2011) Sci Transl Med. 3(105).
  6. 6. Teperino R, et al. Hedgehog partial agonism drives Warburg-like metabolism in muscle and brown fat. (2012) Cell. 151(2):414-26.



Products are for research use only. Not for human use.



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