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UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
2 mg | $48 | In Stock | |
5 mg | $79 | In Stock | |
10 mg | $133 | In Stock | |
25 mg | $243 | In Stock | |
50 mg | $397 | In Stock | |
100 mg | $597 | In Stock | |
200 mg | $868 | In Stock | |
1 mL x 10 mM (in DMSO) | $96 | In Stock |
Description | UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM). |
Targets&IC50 | GLP:<2.5 nM, G9a:<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. |
Cell Research | 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. |
Animal Research | 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]. |
Alias | UNC-0642, UNC 0642 |
Molecular Weight | 546.7 |
Formula | C29H44F2N6O2 |
Cas No. | 1481677-78-4 |
Smiles | COc1cc2c(NC3CCN(CC3)C(C)C)nc(nc2cc1OCCCN1CCCC1)N1CCC(F)(F)CC1 |
Relative Density. | 1.23 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (91.46 mM), Sonication and heating are recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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