1. Epigenetics
  2. Epigenetic Reader Domain
  3. M-525

M-525 

Cat. No.: HY-124069
Handling Instructions

M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity.

For research use only. We do not sell to patients.

M-525 Chemical Structure

M-525 Chemical Structure

CAS No. : 2173582-08-4

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Description

M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity[1].

In Vitro

M-525 achieves an IC50 of 3 nM in the MV4;11 cell line and has an IC50 of 2 µM in the HL-60 cell line. M-525 (3-300 nM; 24 h) is potent and effective in suppressing the expression of MEIS1 and HOX genes in MV4;11 cells carrying the MLL-AF4 fusion and in MOLM-13 cells carrying the MLL-AF9 fusion. It demonstrates high cellular specificity over non-MLL leukemia cells[1].

Molecular Weight

734.92

Formula

C₃₉H₅₁FN₆O₅S

CAS No.

2173582-08-4

SMILES

O=C(OC)N[[email protected]@H]1[[email protected]@H]([[email protected]](C2CCN(CC3CN(C4=CC=C(S(=O)(C5CN(C(/C=C/CN(C)C)=O)C5)=O)C=C4)C3)CC2)(C#N)C6=CC=CC(F)=C6)CCC1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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KeyWords:

M-525 | M525 | M 525 | Epigenetic Reader Domain | Inhibitor | inhibitor | inhibit

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M-525
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HY-124069
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