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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H20FN3O2 |
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分子量 | 377.41 | CAS No. | 1129669-05-1 | |
Solubility (25°C)* | 体外 | DMSO | 75 mg/mL (198.72 mM) | |
Ethanol | 10 mg/mL warmed with 50ºC water bath (26.49 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 | IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling. |
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in vitro | In hNPCs, IM-12 inhibits GSK-3β activity with IC50 of 3.8 μM and subsequently increases β-catenin concentration significantly. Through the activation of canonical Wnt signalling pathway, IM-12 promotes the neuronal differentiation of human neural progenitor cells. [1] |
キナーゼアッセイ | GSK-3β activity assay | |
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IC50 of new synthesised compound IM-12 to GSK-3β is determined by a luminometric GSK-3β activity assay. Briefly, compounds are tested in different concentrations diluted in assay buffer containing final concentrations of: 4 mM MOPS pH 7.2; 0.4 mM EDTA; 1 mM EGTA; 2.5 mM β-glycerophosphate; 4 mM MgCl2; 40 μM BSA; 0.05 mM DTT. Four microlitres of diluted compounds are added to 25 μM pGS-2 peptide substrate, 20 ng recombinant GSK-3β and 1 μM ATP to a total assay volume of 40 μl. The enzymatic reaction is stopped after 30 min of incubation at 30 °C by adding 40 μl KinaseGlo. The luminometric signal is allowed to stabilise for 10 min and the measured with a Glomax® 96 Microplate Luminometer. | ||
細胞アッセイ | 細胞株 | ReNcell VM cells |
濃度 | 3 μM | |
反応時間 | 72 hours | |
実験の流れ | To measure viable cells, 50-100 μL of cell suspension is analyzed using CASY technology with the appropriate program. ReNcell VM cells are seeded at a defined cell number and proliferated for 24 h. Then the medium is changed to proliferation medium with added substances at indicated concentrations. The cell number was determined every 24 h. Cells were exposed to the added drugs during the whole experiment, whereas the media is changed every 24 h. |
Data from [Data independently produced by , , Exp Cell Res, 2016, 345(2):206-17.]
Self-renewing human naïve pluripotent stem cells dedifferentiate in 3D culture and form blastoids spontaneously [ Nat Commun, 2024, 15(1):668] | PubMed: 38253551 |
Generation of a humanized mesonephros in pigs from induced pluripotent stem cells via embryo complementation [ Cell Stem Cell, 2023, 30(9):1235-1245.e6] | PubMed: 37683604 |
dCas9 fusion to computer-designed PRC2 inhibitor reveals functional TATA box in distal promoter region [ Cell Rep, 2022, 38(9):110457] | PubMed: 35235780 |
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] | PubMed: 34997030 |
B3GALT5 knockout alters gycosphingolipid profile and facilitates transition to human naïve pluripotency [ Proc Natl Acad Sci U S A, 2020, 117(44):27435-27444] | PubMed: 33087559 |
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] | PubMed: 31740922 |
RHAMM inhibits cell migration via the AKT/GSK3β/Snail axis in luminal A subtype breast cancer [ Anat Rec (Hoboken), 2020, 303(9):2344-2356] | PubMed: 31769593 |
Non-canonical WNT-signaling controls differentiation of lymphatics and extension lymphangiogenesis via RAC and JNK signaling. [ Sci Rep, 2019, 9(1):4739] | PubMed: 30894622 |
Effects of LDOC1 on colorectal cancer cells via downregulation of the Wnt/β-catenin signaling pathway. [ Oncol Rep, 2019, 41(6):3281-3291] | PubMed: 31002361 |
IM-12 activates the Wnt-β-catenin signaling pathway and attenuates rtPA-induced hemorrhagic transformation in rats after acute ischemic stroke. [ Biochem Cell Biol, 2019, 97(6):702-708] | PubMed: 31770017 |
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。
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