M-525 ( M525 )

Catalog No. M13475 CAS No. 2173582-08-4

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

M-525
Note

Research use only, not for human use.
Brief Description

M-525 is a first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction with binding IC50 of 3.3 nM in FP assays.
Description

M-525 is a first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction with binding IC50 of 3.3 nM in FP assays; inhibits MV4;11 (MLL fusion) and HL60 (No MLL fusion) cell growth with IC50 of 2.7 and 2,000 nM, respectively; significantly down-regulates the expression of MEIS1, HOXA9 and HOXA11 genes in a dosedependent anner at ow nanomolar concentrations, also effectively suppresses the expression of MEIS1 and HOX genes in the MOLM-13 cell line at 3 nM.
Synonyms

M525
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

——
Indication

——

CAS Number

2173582-08-4
Formula Weight

734.93
Molecular Formula

C39H51FN6O5S
Purity

>98% (HPLC)
Solubility

——
SMILES

O=C(OC)N[C@@H]1[C@@H]([C@](C2=CC=CC(F)=C2)(C3CCN(CC4CN(C5=CC=C(S(=O)(C6CN(C(/C=C/CN(C)C)=O)C6)=O)C=C5)C4)CC3)O)CCC1
Chemical Name

methyl ((1S,2R)-2-((S)-cyano(1-((1-(4-((1-((E)-4-(dimethylamino)but-2-enoyl)azetidin-3-yl)sulfonyl)phenyl)azetidin-3-yl)methyl)piperidin-4-yl)(3-fluorophenyl)methyl)cyclopentyl)carbamate

1. Xu S, et al. Angew Chem Int Ed Engl. 2018 Feb 5;57(6):1601-1605.

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