Adavivint (SM04690)

Catalog No.S8761

Adavivint (SM04690) Chemical Structure

Molecular Weight(MW): 505.55

SM04690 is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.

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Biological Activity

Description SM04690 is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.
Targets
Wnt [1]
()
In vitro

Bone-marrow-derived hMSCs (CD29+, CD44+ CD166+ CD105+ CD45-), treated with SM04690, show a dose-dependent decrease in the expression of Wnt pathway genes (ASCL1, LEF1, TCF7L2, TCF7, C-262 MYC and AXIN2). M04690 also inhibits the expression of AXIN2, TCF7 and LEF1 in hMSCs and AXIN2 and LGR5 in IEC6 (intestinal stem cells sensitive to Wnt activation) when the Wnt pathway is selectively activated using either Wnt3a or a GSK3β inhibitor, CHIR-99021. SM04690 has minimal effects on the non-canonical Wnt pathway and the BMP pathway. SM04690 protects chondrocytes from catabolic breakdown in vitro[1].

In vivo

Intra-articular injection of SM04690 promotes cartilage growth and improves joint health in a rat model of knee osteoarthritis. It decreases cartilage breakdown in vivo[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: SW480 cells and hMSCs
  • Concentrations: 10, 30 and 100 nM
  • Incubation Time: 48 h
  • Method:

    --


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Sprague-Dawley (SD) rats (12 weeks old, male)
  • Formulation: --
  • Dosages: 0.3μg in 50μl
  • Administration: intra-articular injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 30 mg/mL (59.34 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 505.55
Formula

C29H24FN7O

CAS No. 1467093-03-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Wnt/beta-catenin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID