SAG (Smoothened Agonist)

製品コードS6384 バッチS638401

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C28H28ClN3OS
分子量 490.06 CAS No. 912545-86-9
Solubility (25°C)* 体外 DMSO 98 mg/mL (199.97 mM)
Ethanol 98 mg/mL (199.97 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 SAG (Smoothened Agonist) is a potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.
in vitro

SAG can counteract glucocorticoids (GCs) antagonism of Shh-driven granule neuron precursor (CGNP) proliferation.[2]
in vivo

Systemic administration of Smoothened Agonist (SAG) prevents the neurotoxic effects of glucocorticoids. Smoothened Agonist can cross the blood-brain barrier to activate Shh transcriptional targets in vivo. SAG at the treatment dose effectively prevents GC-induced neonatal cerebellar developmental abnormalities.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Granule neuron precursor (CGNP) primary cells
濃度 15-240 nM
反応時間 24 h
実験の流れ

CGNP are stimulated by various SAG concentrations (15 to 240 nM) compared with ShhN (3 μg/ml) and vehicle after 24 hours in vitro. Quantitative reverse transcription–PCR is performed with SYBR Green master mix in LightCycler 480.
動物実験 動物モデル Ptc+/- mouse medulloblastoma model, Swiss Webster B pups
投薬量 20 mg/kg, 140 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Identification of a distal enhancer regulating hedgehog interacting protein gene in human lung epithelial cells [ EBioMedicine, 2024, 101:105026] PubMed: 38417378
Sonic hedgehog restrains the ubiquitin-dependent degradation of SP1 to inhibit neuronal/glial senescence associated phenotypes in chemotherapy-induced peripheral neuropathy via the TRIM25-CXCL13 axis [ J Adv Res, 2024, S2090-1232(24)00106-1] PubMed: 38479571
Single-cell RNA sequencing reveals the developmental program underlying proximal-distal patterning of the human lung at the embryonic stage [ Cell Res, 2023, 33(6):421-433] PubMed: 37085732
Highly reproducible and cost-effective one-pot organoid differentiation using a novel platform based on PF-127 triggered spheroid assembly [ Biofabrication, 2023, 15(4).] PubMed: 37552975
Triptolide inhibits epithelial ovarian tumor growth by blocking the hedgehog/Gli pathway [ Aging (Albany NY), 2023, 10.18632/aging.205110] PubMed: 37851362
Primary cilia support cartilage regeneration after injury [ Int J Oral Sci, 2023, 15(1):22] PubMed: 37268650
Protocol for the rapid intravenous in ovo injection of developing amniote embryos [ STAR Protoc, 2023, 4(2):102324] PubMed: 37210721
Transcription Factor 4 loss-of-function is associated with deficits in progenitor proliferation and cortical neuron content [ Nat Commun, 2022, 13(1):2387] PubMed: 35501322
The PROTAC selectively degrading Bcl-xL represents a novel Hedgehog pathway inhibitor with capacity of combating resistance to Smoothened inhibitors while sparing bone growth [ Theranostics, 2022, 12(17):7476-7490] PubMed: 36438482
CK2 blockade alleviates liver fibrosis by suppressing activation of hepatic stellate cells via the Hedgehog pathway [ Br J Pharmacol, 2022, 10.1111/bph.15945] PubMed: 36070072

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