MM-102

Modify Date: 2024-01-18 00:45:48

MM-102 Structure
MM-102 structure
Common Name MM-102
CAS Number 1417329-24-8 Molecular Weight 669.80500
Density N/A Boiling Point N/A
Molecular Formula C35H49F2N7O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MM-102


MM-102 is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.IC50 value: 2.4 nMTarget: MLLin vitro: MM-102 inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins. MM-102, with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay with IC50 = 0.4-0.9 μM. MM-102 dose-dependently inhibits cell growth in the MV4;11 and KOPN8 leukemia cell lines, which carry MLL1-AF4 and MLL1-ENL fusion proteins, respectively. MM-102 has IC50 = 25 μM in both cell lines and completely inhibits cell growth in these cell lines at 75 μM. MM-102 effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins and has minimal effect in leukemia cells with wild-type MLL1 protein.[1]

 Names

Name Cyclopentanecarboxam​ide, 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]​-
Synonym More Synonyms

 MM-102 Biological Activity

Description MM-102 is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.IC50 value: 2.4 nMTarget: MLLin vitro: MM-102 inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins. MM-102, with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay with IC50 = 0.4-0.9 μM. MM-102 dose-dependently inhibits cell growth in the MV4;11 and KOPN8 leukemia cell lines, which carry MLL1-AF4 and MLL1-ENL fusion proteins, respectively. MM-102 has IC50 = 25 μM in both cell lines and completely inhibits cell growth in these cell lines at 75 μM. MM-102 effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins and has minimal effect in leukemia cells with wild-type MLL1 protein.[1]
Related Catalog
References

[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.

 Chemical & Physical Properties

Molecular Formula C35H49F2N7O4
Molecular Weight 669.80500
Exact Mass 669.38100
PSA 178.30000
LogP 6.43300
Storage condition -20℃

 Synonyms

MM-102