| Name | UNC0642 |
| Description | UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM). |
| 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]. |
| 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. |
| 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.
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| Keywords | inhibit | Inhibitor | UNC0642 | Histone Methyltransferase |
| Inhibitors Related | BIX-01294 trihydrochloride | Tazemetostat | Piribedil | XY1 | UNC 0631 | GSK126 | MAK683 | EZM 2302 | EPZ015666 | AMI-1 free acid | MS37452 | MRTX-1719 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Methylation Compound Library | Histone Modification Compound Library | Glycometabolism Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
