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MilliporeSigma™ Calbiochem™ Menin-MLL Interaction Inhibitor, MI-2-2

Catalog No. 44482510MG Shop All MilliporeSigma Products
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44-482-510MG 10mg
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Description

A cell-permeable thienopyrimidine compound

A cell-permeable thienopyrimidine compound that competes against MLL (Mixed Lineage Leukemia) for menin binding (IC50 = 46 and 520 nM, respectively, against MBM1 sequence MLL4-15 and MLL4-43 containing both MBM1 & MBM2) by targeting menin MLL-binding pocket with high affinity ( K D = 22nM), effectively disrupting cellular menin and MLL-AF9 fusion interaction (by >90% at 12μM in MLL-AF9-expressing HEK293 cells). Shown to inhibit the oncogenic proliferation of four MLL translocation-harboring human leukemia cell lines (by >95% in 12 d at 6μM), but not non-MLL leukemia Kasumi-1 and HAL-01 lines (≤16% inhibition at 12μM), by downregulating MLL target genes expression via simultaneous hematopoietic differentiation induction and killing of non-differentiated population.
TRUSTED_SUSTAINABILITY

Specifications

Color Off-white
Description 99% by HPLC
Target Proteins Menin
Molecular Formula C17H20F3N5S2·HCl
Solubility DMSO
Content And Storage Hygroscopic, Protect from light
Form Powder
Quantity 10 mg
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