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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
化学式 | C23H27N5 |
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分子量 | 373.49 | CAS No. | 304909-07-7 | |
Solubility (25°C)* | 体外 | DMSO | 75 mg/mL (200.8 mM) | |
Ethanol | 18 mg/mL (48.19 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. |
製品説明 | SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM. |
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in vitro | SANT-1 inhibits wild type and oncogenic Smo with equal potency. SANT-1 counteracts SAG-induced pathway activation in Shh-LIGHT2 cells. SANT-1 is able to block BODIPY-cyclopamine binding to Smo-expressing cells, but SANT-1 is unable to inhibit completely this association to background levels. This suggests that their interactions with Smo may alter its affinity for cyclopamine rather than compete directly for cyclopamine binding. SANT-1 blocks pathway activation in SmoA1-LIGHT2 cells with potencies similar to those observed in the Shh-LIGHT2 assay. SANT-1 has disparate inhibitory activities in the Shh-LIGHT2 and BODIPY-cyclopamine assays and is unusually potent at blocking SAG-mediated pathway activation.[1] SANT-1 efficiently inhibited cyclopamine- and jervine- induced translocation of Smo to the primary cilium. SANT-1 inhibits PKA stimulation of Smo trafficking to the proximal cilium.[2]
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特徴 | Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists. |
キナーゼアッセイ | Small Molecule Screens for Hh Pathway Modulators | |
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Shh-N (N-terminal fragment of Shh without cholesterol modification)-conditioned medium is obtained from an HEK 293 cell line stably transfected with Shh-N expression and neomycin resistance constructs. The Shh-N-producing HEK 293 cells are grown to 80% confluency in DMEM containing 10% (vol/vol) FBS and 400 μg/ml G418. The medium then is replaced with DMEM containing 2% (vol/vol) FBS, and after 1 day of growth, the medium is collected and filtered through a 0.22-μm membrane. Control medium is obtained from HEK 293 cells. Shh-LIGHT2 cells are then cultured to confluency in 96-well plates and treated with the small molecules (0.714 μg/mL; ≈2 μM compound in each well) in the presence of either Shh-N-conditioned medium or HEK 293 control medium (1:25 dilution into DMEM containing 0.5% bovine calf serum). After incubating the treated cells for 30 h at 37°C, cellular firefly and Renilla luciferase activities are measured. | ||
細胞アッセイ | 細胞株 | Cell-free assays |
濃度 | 20 nM | |
反応時間 | ||
実験の流れ | ||
動物実験 | 動物モデル | Swiss albino male mice |
投薬量 | 3.3 mg/kg | |
投与方法 | i.p. |
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, , Oncotarget, 2017, 8(40): 67891-67903
HOXA3 functions as the on-off switch to regulate the development of hESC-derived third pharyngeal pouch endoderm through EPHB2-mediated Wnt pathway [ Front Immunol, 2023, 14:1258074] | PubMed: 38259452 |
CNPY4 inhibits the Hedgehog pathway by modulating membrane sterol lipids [ Nat Commun, 2022, 13(1):2407] | PubMed: 35504891 |
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
Hedgehog pathway is negatively regulated during the development of Drosophila melanogaster PheRS-m (Drosophila homologs gene of human FARS2) mutants [ Hum Cell, 2022, 10.1007/s13577-022-00796-0] | PubMed: 36205831 |
Microengineered Multi-Organoid System from hiPSCs to Recapitulate Human Liver-Islet Axis in Normal and Type 2 Diabetes [ Adv Sci (Weinh), 2021, e2103495] | PubMed: 34951149 |
Generation of functional human thymic cells from induced pluripotent stem cells [ J Allergy Clin Immunol, 2021, S0091-6749(21)01141-6] | PubMed: 34331993 |
One-Step Generation of Aqueous-Droplet-Filled Hydrogel Fibers as Organoid Carriers Using an All-in-Water Microfluidic System [ ACS Appl Mater Interfaces, 2021, 13(2):3199-3208] | PubMed: 33405509 |
Compound Tongluo Decoction inhibits endoplasmic reticulum stress-induced ferroptosis and promoted angiogenesis by activating the Sonic Hedgehog pathway in cerebral infarction [ J Ethnopharmacol, 2021, S0378-8741(21)00863-1] | PubMed: 34536518 |
FGF2 Inhibits Early Pancreatic Lineage Specification during Differentiation of Human Embryonic Stem Cells [ Cells, 2020, 9(9):E1927] | PubMed: 32825270 |
GATA6-AS1 Regulates GATA6 Expression to Modulate Human Endoderm Differentiation [ Stem Cell Reports, 2020, S2213-6711(20)30291-5] | PubMed: 32795420 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。