SAG (Smoothened Agonist) HCl

Catalog No.S7779 Batch:S777904

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Technical Data

Formula

C28H29Cl2N3OS
Molecular Weight 526.52 CAS No. 2095432-58-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (189.92 mM)
Water 100 mg/mL (189.92 mM)
Ethanol 100 mg/mL (189.92 mM)
* <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.)

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Biological Activity

Description SAG (Smoothened Agonist) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
Targets
Smoothened [1]
(mouse cultured cell assay)
3 nM(EC50)
In vitro

SAG regulates Smo activity by binding directly to the Smo heptahelical bundle. [1]

SAG induces Smo-dependent signaling through Gli in a GRK2-dependent way. [2]

SAG also (1 nM) induces proliferation of neuronal and glial precursors without affecting the differentiation pattern of newly produced cells. [3]
In vivo

In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. [3]

In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities. [4]

Protocol (from reference)

Kinase Assay:

[1]
  • Cell-Based Assays for Hh Pathway Activation

    Assays for Hh pathway activation in Shh-LIGHT2 cells, a clonal NIH 3T3 cell line stably incorporating Gli-dependent firefly luciferase and constitutive Renilla luciferase reporters, are conducted. For studies of SAG (a chlorobenzothiophene-containing Hh pathway agonist) and PA-SAG, Shh-LIGHT2 cells are cultured to confluency in 96-well plates and then treated with various concentrations of these compounds in DMEM containing 0.5% (vol/vol) bovine calf serum.
Cell Assay:

[1]
  • Cell lines

    Shh-LIGHT2 cells

  • Concentrations

    3 nM

  • Incubation Time

    30 h

  • Method

    Cells were treated with various concentrations of SAG in DMEM containing 0.5% (vol/vol) bovine calf serum.
Animal Study:

[3]
  • Animal Models

    Rat

  • Dosages

    2.5 nM

  • Administration

    Intracerebroventricular administration

Customer Product Validation

Data from [Data independently produced by , , J Pain Res, 2018, 11:649-659]

Selleck's SAG (Smoothened Agonist) HCl has been cited by 80 publications

Jag1/2 maintain esophageal homeostasis and suppress foregut tumorigenesis by restricting the basal progenitor cell pool [ Nat Commun, 2024, 15(1):4124] PubMed: 38750026
Jag1/2 maintain esophageal homeostasis and suppress foregut tumorigenesis by restricting the basal progenitor cell pool [ Nat Commun, 2024, 15(1):4124] PubMed: 38750026
High incidence and geographic distribution of cleft palate in Finland are associated with the IRF6 gene [ Nat Commun, 2024, 15(1):9568] PubMed: 39500877
Large-scale single-nuclei profiling identifies role for ATRNL1 in atrial fibrillation [ Nat Commun, 2024, 15(1):10002] PubMed: 39562555
Tissue Mechanics and Hedgehog Signaling Crosstalk as a Key Epithelial-Stromal Interplay in Cancer Development [ Adv Sci (Weinh), 2024, 11(35):e2400063] PubMed: 38976559
Programmed BRD9 Degradation and Hedgehog Signaling Activation via Silk-Based Core-Shell Microneedles Promote Diabetic Wound Healing [ Adv Sci (Weinh), 2024, 11(45):e2404130] PubMed: 39413023
GRK2 kinases in the primary cilium initiate SMOOTHENED-PKA signaling in the Hedgehog cascade [ PLoS Biol, 2024, 22(8):e3002685] PubMed: 39138140
An Epilepsy-Associated CILK1 Variant Compromises KATNIP Regulation and Impairs Primary Cilia and Hedgehog Signaling [ Cells, 2024, 13(15)1258] PubMed: 39120290
Generation of self-renewing neuromesodermal progenitors with neuronal and skeletal muscle bipotential from human embryonic stem cells [ Cell Rep Methods, 2024, 4(11):100897] PubMed: 39515335
An epilepsy-associated CILK1 variant compromises KATNIP regulation and impairs primary cilia and Hedgehog signaling [ bioRxiv, 2024, 2024.05.14.594243] PubMed: 38798407

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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