Powder: -20°C for 3 years | In solvent: -80°C for 1 year
UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
説明 | UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM). |
ターゲット&IC50 | G9a:<2.5 nM, GLP:<2.5 nM |
In vitro | UNC0642 (Ki: 3.7±1 nM) is competitive with the peptide substrate and non-competitive with the cofactor SAM. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, transporters, GPCRs, and ion channels. UNC0642 exhibits high potency at low cell toxicity, reducing the H3K9me2 mark, and good separation of functional potency in a number of cell lines. |
In vivo | UNC0642 (5 mg/kg, i.p.) results in a plasma Cmax of 947 ng/mL and an AUC of 1265 h·ng/ml. |
細胞研究 | MDA-MB-231, PC3, and U2OS cells are treated with UNC0642 for 48 h. Cell viability assays are performed by incubating cells with 0.1 mg/mL of resazurin for 3 – 4 h. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm. |
動物実験 | Mouse: Standard PK studies are performed using male Swiss albino mice. Plasma and brain concentrations are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following UNC0642 (5 mg/kg, i.p.). The compound concentration at each time point in plasma or brain is the average value from 3 test animals[1]. |
別名 | UNC-0642, UNC 0642 |
分子量 | 546.7 |
分子式 | C29H44F2N6O2 |
CAS No. | 1481677-78-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (91.46 mM), Sonication and heating are recommended.
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
UNC0642 1481677-78-4 Chromatin/Epigenetic Histone Methyltransferase inhibit UNC-0642 Inhibitor UNC 0642 inhibitor