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F5446 is a selective small molecule SUV39H1 methyltransferase inhibitor. It promotes apoptosis in colorectal cancer cells by inhibiting the deposition of H3K9me3 on the FAS promoter to increase Fas expression, while inhibiting CTL effector gene expression.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | F5446 is a selective small molecule SUV39H1 methyltransferase inhibitor. It promotes apoptosis in colorectal cancer cells by inhibiting the deposition of H3K9me3 on the FAS promoter to increase Fas expression, while inhibiting CTL effector gene expression. |
In vitro | Methods: SW620 and LS411N cells were treated with F5446 (100, 250 nM, 48 h), then fixed, stained with PI, and analyzed for DNA content by flow cytometry. Results: F5446 treatment induced cell cycle arrest at S phase in both SW620 and LS411N cells in a concentration-dependent manner. Methods: SW620, LS411N and CCD841 cells were treated with F5446 (10, 50, 100, 250, 500, 1000 nM) and analyzed for apoptosis. Results: F5446 induced apoptosis in both tumor cell lines in vitro in a concentration-dependent manner. The normal human colon epithelial cell line CCD841 was less sensitive to F5446 in inducing apoptotic cell death than tumor cells. [1] |
In vivo | Methods: F5446 (5, 10 mg/kg, intraperitoneal injection, once every two days, for 26 days) was used to treat SW620 and SW620-5FUR cell-transplanted tumor model mice. Results: F5446 can inhibit tumor growth in vivo in a concentration-dependent manner. [1] |
Alias | F 5446 |
Molecular Weight | 552.94 |
Formula | C26H17ClN2O8S |
Cas No. | 2304465-89-0 |
Smiles | COC(=O)c1cc2-c3c(c[nH]c3C(=O)C(=O)c2n1S(=O)(=O)c1ccc(Cl)cc1)C(=O)OCc1ccccc1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (144.68 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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