1417329-24-8
Chemical Structure
MM-102
Synonym(s): HMTase Inhibitor IX
- CAS No.: 1417329-24-8
- Formula:C35H49F2N7O4
- Molecular Weight:669.80
IUPAC Name: (S)-N-(bis(4-fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentane-1-carboxamide
InChIKey: RZKSQRIPRKWVBU-MHZLTWQESA-N
SMILES: O=C(C1(NC([C@@H](NC(C(NC(C(C)C)=O)(CC)CC)=O)CCCNC(N)=N)=O)CCCC1)NC(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3
Biological Activity: MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos[1][2][3][4][5].
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MM-102 | 99.09% | MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos. | ||||||||||||||||||||
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- [1]. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J Am Chem Soc. 2013, 135(2), 669-682. [Content Brief]
- [2]. Townsend E C. Development of a Novel Inhibitor to the Conserved, Developmental Regulator, WDR5, for Treatment of Acute Leukemia[D]. , 2012.
- [3]. Wang D, et al. MBD2 regulates the progression and chemoresistance of cholangiocarcinoma through interaction with WDR5[J]. Journal of Experimental & Clinical Cancer Research, 2024, 43(1): 272. [Content Brief]
- [4]. Hara D, et al. Inhibition of H3K4 Trimethylation Ameliorates Peritoneal Fibrosis and Senescence: FR-PO456[J]. Journal of the American Society of Nephrology, 2022, 33(11S): 447-448. [Content Brief]
- [5]. Zhang Z, et al. Down-regulation of H3K4me3 by MM-102 facilitates epigenetic reprogramming of porcine somatic cell nuclear transfer embryos[J]. Cellular Physiology and Biochemistry, 2018, 45(4): 1529-1540. [Content Brief]
Keywords
