MI-538

SKU: orb1308044

Description

MI-538 is a potent small molecule inhibitor that disrupts the menin-MLL fusion protein interaction with an IC50 of 21 nM. It is a valuable research tool for studying oncogenic mechanisms and has demonstrated activity in cellular assays and in vivo models of MLL-rearranged leukemia.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1857417-10-7
• MW: 566.6
• Purity: >99.99% (May vary between batches)
• Formula: C₂₇H₂₅F₃N₈OS
• SMILES: Oc1cc2n(Cc3cn[nH]c3)c(cc2cc1CN1CCC(CC1)Nc1ncnc2sc(CC(F)(F)F)cc12)C#N
• Target: Epigenetic Reader Domain,Histone Methyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:10 mg/mL (17.65 mM);DMSO:95 mg/mL (167.67 mM)

Bioactivity

• Target IC50:
  Menin:6.5 nM(Kd)|Menin-MLL:21 nM
• In Vivo:
  Treatment with MI-538 leads to an approximately 80% reduction in MV4;11 tumor volume, with minimal toxicity, evidenced by less than a 10% decrease in body weight.
• In Vitro:
  Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MI538, MI-538, MI 538, inhibit, Epigenetic Reader Domain, EpigeneticReaderDomain, HistoneMethyltransferase, Histone Methyltransferase, menin, menin and MLL interaction, Menin-MLL, Inhibitor

Compound Identifiers

PubChem CID

117636625