MM-102 TFA

MM-102 is a Potent WDR5/MLL interaction inhibitor. The MM-102 compound prevents the interaction between mixed lineage leukemia 1 (MLL1) and WD Trp-Asp repeat domain 5 (WDR5) and results in the inhibition of MLL1 H3K4 histone methyltransferase (HMT) activity. Down-Regulation of H3K4me3 by MM-102 Facilitates Epigenetic Reprogramming of Porcine Somatic Cell Nuclear Transfer Embryos

Product information

CAS Number: 1883545-52-5

Molecular Weight: 783.83

Formula: C37H50F5N7O6

Synonym:

MM-102 trifluoroacetic acid

MM-102

MM-102 TFA

MM 102

MM102

Chemical 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 trifluoroacetate

Smiles: CC(C)C(=O)NC(CC)(CC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NC1(CCCC1)C(=O)NC(C1=CC=C(F)C=C1)C1=CC=C(F)C=C1.OC(=O)C(F)(F)F

InChiKey: ZRKTWBXVGMHWHM-YCBFMBTMSA-N

InChi: InChI=1S/C35H49F2N7O4.C2HF3O2/c1-5-34(6-2,43-29(45)22(3)4)31(47)41-27(10-9-21-40-33(38)39)30(46)44-35(19-7-8-20-35)32(48)42-28(23-11-15-25(36)16-12-23)24-13-17-26(37)18-14-24;3-2(4,5)1(6)7/h11-18,22,27-28H,5-10,19-21H2,1-4H3,(H,41,47)(H,42,48)(H,43,45)(H,44,46)(H4,38,39,40);(H,6,7)/t27-;/m0./s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

MM-102 (HMTase Inhibitor IX) 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 (TFA), with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay withIC50=0.4-0.9 μM. MM-102 (HMTase Inhibitor IX) 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 (HMTase Inhibitor IX) has IC50=25 μM in both cell lines and completely inhibits cell growth in these cell lines at 75 μM. MM-102 (HMTase Inhibitor IX) 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.

References:

1. Han X, Xiang J, Li C, Wang J, Wang C, Zhang Y, Li Z, Lu Z, Yue Y, Li X. MLL1 combined with GSK3 and MAP2K inhibition improves the development of in vitro- fertilized embryos. Theriogenology. 2020 Apr 1;146:58-70. doi: 10.1016/j.theriogenology.2020.01.051. Epub 2020 Jan 29. PMID: 32059151.
2. Shimoda H, Doi S, Nakashima A, Sasaki K, Doi T, Masaki T. Inhibition of the H3K4 methyltransferase MLL1/WDR5 complex attenuates renal senescence in ischemia reperfusion mice by reduction of p16INK4a. Kidney Int. 2019 Nov;96(5):1162-1175. doi: 10.1016/j.kint.2019.06.021. Epub 2019 Aug 1. PMID: 31570196.
3. Cai M, Bompada P, Atac D, Laakso M, Groop L, De Marinis Y. Epigenetic regulation of glucose-stimulated osteopontin (OPN) expression in diabetic kidney. Biochem Biophys Res Commun. 2016 Jan 1;469(1):108-113. doi: 10.1016/j.bbrc.2015.11.079. Epub 2015 Nov 22. PMID: 26592666.

Products are for research use only. Not for human use.