UNC1215 is a potent and selective MBT (malignant brain tumor) antagonist, which binds L3MBTL3 with IC50 of 40 nM and Kd of 120 nM, 50-fold selective versus other members of the human MBT family.
Cell Experiment | |
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Cell lines | HEK293T/17 cells |
Preparation method | CellTiter-Glo luminescent cell viability assay |
Concentrations | ~100 μM |
Incubation time | 24 h |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 529.72 |
Formula | C32H43N5O2 |
CAS Number | 1415800-43-9 |
Solubility (25°C) | DMSO ≥ 90 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.
[2] Qianqian Wang, et al. PHF20L1 antagonizes SOX2 proteolysis triggered by the MLL1/WDR5 complexes
[3] Narkhyun Bae, et al. Developing Spindlin1 small-molecule inhibitors by using protein microarrays
[4] Brandi M Baughman, et al. The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer
[5] Lindsey I James, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain
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