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Formula | C29H24FN7O |
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Molecular Weight | 505.55 | CAS No. | 1467093-03-3 | |
Solubility (25°C)* | In vitro | DMSO | 30 mg/mL (59.34 mM) | |
Water | Insoluble | |||
Ethanol | 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Adavivint (SM04690,Lorecivivint) 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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Targets |
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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]. |
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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]. |
Cell Assay: |
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Animal Study: |
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Canonical Wnt Pathway Is Involved in Chemoresistance and Cell Cycle Arrest Induction in Colon Cancer Cell Line Spheroids [ Int J Mol Sci, 2023, 24(6)5252] | PubMed: 36982333 |
"Pharmacological inhibition of CLK2 activates YAP by promoting alternative splicing of AMOTL2" [ bioRxiv, 2023, 2023.04.19.537449] | PubMed: 37131806 |
β-catenin regulates HIV latency and modulates HIV reactivation [ PLoS Pathog, 2022, 18(3):e1010354] | PubMed: 35255110 |
Glycyrrhizic acid alters the hyperoxidative stress-induced differentiation commitment of MSCs by activating the Wnt/β-catenin pathway to prevent SONFH [ Food Funct, 2022, 10.1039/d2fo02337g] | PubMed: 36541285 |
Engineering osteoarthritic cartilage model through differentiating senescent human mesenchymal stem cells for testing disease-modifying drugs [ Sci China Life Sci, 2021, 10.1007/s11427-021-1933-7] | PubMed: 34109475 |
Inhibiting Wnt/beta-catenin in CTNNB1-mutated endometrial cancer [ Mol Carcinog, 2021, 10.1002/mc.23308] | PubMed: 34038589 |
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.