MI-3 (Menin-MLL Inhibitor)
MI-3 (Menin-MLL Inhibitor) Basic information
- Product Name:
- MI-3 (Menin-MLL Inhibitor)
- Synonyms:
-
- MI-3
- 5-dihydro-5
- 5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(1-methylethyl)
- MI3;MI 3;MENIN-MLL INHIBITOR 3;THIENO[2;3-D]PYRIMIDINE; 4-[4-(4;5-DIHYDRO-5;5-DIMETHYL-2-THIAZOLYL)-1-PIPERAZINYL]-6-(1-METHYLETHYL)
- Menin-MLL inhibitor 3
- Thieno[2,3-d]pyriMidine, 4-[4-(4,5-dihydro-5,5-diMethyl-2-thiazolyl)-1-piperazinyl]-6-(1-Methylethyl)-
- 4-[4-(4,5-Dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(1-methylethyl)thieno[2,3-d]pyrimidine
- MI-3 (Menin-MLL Inhibitor)
- CAS:
- 1271738-59-0
- MF:
- C18H25N5S2
- MW:
- 375.55
- Product Categories:
-
- Inhibitors
- Mol File:
- 1271738-59-0.mol
MI-3 (Menin-MLL Inhibitor) Chemical Properties
- Boiling point:
- 527.9±60.0 °C(Predicted)
- Density
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 8.33 mg/mL (22.18 mM; Need ultrasonic)
- form
- Powder
- pka
- 9.59±0.40(Predicted)
- color
- Light yellow to yellow
MI-3 (Menin-MLL Inhibitor) Usage And Synthesis
Description
MI-3 is an inhibitor of the interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 648 nM). MI-3 binds to menin (Kd = 201 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. It inhibits growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL fusion proteins MLL-AF9 or MLL-ENL (IC50 = 5 μM for both), as well as reduces colony formation and induces differentiation of MLL-AF9-transformed BMCs. MI-3 inhibits growth of human leukemia cell lines containing MLL translocations and decreases the expression of the transcription factors HOXA9, HOXA10, and MEIS1 in THP-1 cells.
Uses
MI-3 (Menin-MLL Inhibitor) reverses oncogenic activity of MLL fusion proteins in leukemia.
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