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Formula | C23H27N5 |
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Molecular Weight | 373.49 | CAS No. | 304909-07-7 | ||||||||
Solubility (25°C)* | In vitro | DMSO | 21 mg/mL (56.22 mM) | ||||||||
Ethanol | 20 mg/mL (53.54 mM) | ||||||||||
Water | Insoluble | ||||||||||
In vivo (Add solvents to the product individually and in order) |
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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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Targets |
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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] When combined HDAC inhibitor SAHA, SANT-1 is able to suppress cellular proliferation and colony formation of Gemcitabine-resistant pancreatic adenocarcinoma cell lines Panc-1 and BxPC-3. [3] |
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Features | Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists. |
Kinase Assay: |
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Animal Study: |
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, , Oncotarget, 2017, 8(40): 67891-67903
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 |
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] | PubMed: 31740922 |
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