| Bioactivity | MI-3 (Menin-MLL inhibitor 3) is a potent and high affinity menin-MLL inhibitor with an IC50 of 648 nM and a Kd of 201 nM[1]. | ||||||||||||
| Target | IC50: 648 nM (menin-MLL); Kd: 201 nM (menin-MLL) | ||||||||||||
| Invitro | MI-3 (12.5-50 μM; HEK293 cells) treatment effectively inhibits the menin-MLL-AF9 interaction in human cells[1].MI-3 (0-1.6 μM; 72 hours; KOPN-8 and MV4;11 cells) treatment shows an effective and dose-dependent growth inhibition in KOPN-8, MV4 and ME-1 cells[1].MI-3 (12.5-50 μM; 48 hours; MV4;11 cells) treatment results in a substantial, and dose-dependent increase in Annexin V and AnnexinV/propidium iodide (PI) cells, demonstrating an increase in the number of cells undergoing apoptosis[1].MI-3 (6.25-25 μM; 6 days; THP-1 cells) treatment results in substantially reduced expression of HOXA9 and MEIS1[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | MI-3 | ||||||||||||
| CAS | 1271738-59-0 | ||||||||||||
| Formula | C18H25N5S2 | ||||||||||||
| Molar Mass | 375.55 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology (2012), 8(3), 277-284. |