UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.
Nucleic Acids Res. 2022 Aug 12;50(14):7938-7958.
HDAC1 and PRC2 mediate combinatorial control in SPI1/PU.1-dependent gene repression in murine erythroleukaemia
UNC1999 purchased from AbMole
Cell Experiment | |
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Cell lines | DLBCL cell line harboring the EZH2Y641N mutant |
Preparation method | DB cells, a diffuse-large B-cell lymphoma cell line harboring the EZH2 Y641N mutation, are obtained from ATCC and cultured in RPMI 1640 supplemented with 10% fetal bovine serum, antibiotics, and various concentrations of compounds (DMSO control, UNC1999, or UNC2400). The medium which contains the test compound or control is refreshed every 3 days. Using TC20 automated cell counter system to measure the numbers of viable cells from at least three independent experiments . Total histones are prepared from cell nuclei using an acidic extraction protocol. About 1 μg of total histones is separated using 15% SDS-PAGE, transferred to PVDF membranes, and probed with histone antibodies. Antibodies used in this study are those against EZH2, general H3, and H3K27me3 |
Concentrations | ~5 μM |
Incubation time | 8 days |
Animal Experiment | |
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Animal models | Male Swiss albino mice |
Formulation | DMSO |
Dosages | ~150 mg/kg (i.p.), ~50 mg/kg (oral) |
Administration | Intraperitoneal administration or oral administration |
Molecular Weight | 569.74 |
Formula | C33H43N7O2 |
CAS Number | 1431612-23-5 |
Solubility (25°C) | DMSO 80 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Naoya Mimura. Novel epigenetic therapies for multiple myeloma
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