MM-102

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].

Product Specifications

CAS Number

[1417329-24-8]

Product Name Alternative

HMTase Inhibitor IX

UNSPSC

12352005

Hazard Statement

H302

Target

Apoptosis; Interleukin Related; NF-κB; TNF Receptor; WDR5

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; Immunology/Inflammation; NF-κB

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/MM-102.html

Purity

99.39

Solubility

DMSO : 125 mg/mL (ultrasonic)

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

Molecular Formula

C35H49F2N7O4

Molecular Weight

669.80

Precautions

H302

References & Citations

[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.|[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.|[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.|[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.

Shipping Conditions

Blue Ice

Storage Conditions

-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture and light, under nitrogen)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Citation 01

Acta Pharmacol Sin. 2022 Feb;43 (2) :457-469.|Cell Death Dis. 2022 Sep 6;13 (9) :770.|J Mol Endocrinol. 2021 Jan;66 (1) :45-57.|Proc Natl Acad Sci U S A. 2019 Feb 19;116 (8) :2961-2966.