A WDR5/MLL interaction inhibitor (IC50 = 2.4 nM) that blocks MLL1 methyltransferase activity

MM-102 – 5 mg

Brand:
Cayman
CAS:
1417329-24-8
Storage:
-20
UN-No:
Non-Hazardous - /

WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.{22296} It serves as a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3 at lysine 4 to upregulate transcription.{20287} MM-102 is a potent WDR5/MLL interaction inhibitor (IC50 = 2.4 nM).{28950} It has been shown to block MLL1 methyltransferase activity, reducing the expression of HoxA9 and Meis-1 genes, which are both critical MLL1 target genes in MLL1 fusion protein-mediated leukemogenesis.{28950} MM-102 can also inhibit cell growth and induce apoptosis in leukemia cells harboring MLL1 fusion proteins.{28950}  

 

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Description

A WDR5/MLL interaction inhibitor (IC50 = 2.4 nM) that blocks MLL1 methyltransferase activity, reducing the expression of HoxA9 and Meis-1 genes, which are both critical MLL1 target genes in MLL1 fusion protein-mediated leukemogenesis; inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins

Formal name: 1-[[(2S)-5-[(aminoiminomethyl)amino]-2-[[2-ethyl-2-[(2-methyl-1-oxopropyl)amino]-1-oxobutyl]amino]-1-oxopentyl]amino]-N-[bis(4-fluorophenyl)methyl]-cyclopentanecarboxamide

Synonyms: 

Molecular weight: 669.8

CAS: 1417329-24-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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