Home Epigenetics Histone Methyltransferase inhibitor - MLL inhibitor MM-102

MM-102

Catalog No.S7265 Synonyms: HMTase Inhibitor IX

For research use only.

MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.

MM-102 Chemical Structure

CAS No. 1417329-24-8

Selleck's MM-102 has been cited by 13 publications

Purity & Quality Control

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Biological Activity

Description MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
Targets
MLL1 [1]
(Cell-free assay)
0.4 μM
In vitro

MM-102, as a MLL1 mimetic, shows high binding affinities to WDR5 with IC50 of 2.9 nM and Ki of < 1 nM. In the MLL1-AF9 transduced murine cells, MM-102 specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. In addition, MM-102 effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Rosetta 2 (DE3) pLysS NHvjdmZHfW6ldHnvckBie3OjeR?= Mmn0TY5pcWKrdHnvckBw\iCPTFyxJIJqdmSrbnegeI8hVi22ZYLtbY5idCCKaYOteIFo\2WmIGfSSFUhOjNiZHXs[ZRqd25ibYX0ZY51KCh{NDD0c{A{OzRicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGV{[2incnnjbIliKGOxbHmgVo9{\XS2YTCyJEhFTTNrIIDMfZNUKGOnbHzzJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYmsJGtqKD1iMD6wNFEh|ryPLh?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ3NEi5Nkc,Ojl{NUS4PVI9N2F-
Rosetta 2 (DE3) pLysS MlXWSpVv[3Srb36gZZN{[Xl? MnTZTY5pcWKrdHnvckBw\iCPTFyxJIJqdmSrbnegeI8hVi22ZYLtbY5idCCKaYOteIFo\2WmIGfSSFUhOjNiZHXs[ZRqd25ibYX0ZY51KCh{NDD0c{A{OzRicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGV{[2incnnjbIliKGOxbHmgVo9{\XS2YTCyJEhFTTNrIIDMfZNUKGOnbHzzJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYmsJGlEPTBiPTCwMlAxOjRizszNMi=> MkPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{NUS4PVIoRjJ7MkW0PFkzRC:jPh?=
Rosetta2-(DE3) pLysS M4CxSmZ2dmO2aX;uJIF{e2G7 MWG1JIhzew>? NXjwS3ZSUW6qaXLpeIlwdiCxZjDDMZRmem2rbnHsJFUuTkGPLWfJUkBx\XC2aXTlJIJqdmSrbnegeI8hVi22ZYLtbY5idCCKaYOteIFo\2WmIGfEVlUhMDJ2IITvJFM{PCC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKtLGRGOylicFz5d3Mh[2WubIOgZYZ1\XJiNTDodpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3MDC9JFAvODB{NDFOwG0v NHjYNXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{eyNFU2PSd-Mke3NlA2PTV:L3G+
MV4-11 NF\PWXlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFXhVJM4OiCqcoO= NFjsSWhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOE0yOSClZXzsd{Bp[XKkb4LpcochVUyOLVHGOEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCFQ1u4MYJie2WmIHPvcI9zcW2ndILpZ{Bie3OjeTygTWM2OCB;IEKwMlch|ryPLh?= M1XXd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5N{KwOVU2Lz5{N{eyNFU2PTxxYU6=
MV4-11 NW\HcphOSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3LyPFczKGi{cx?= MmnlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkStNVEh[2WubIOgbIFz[m:{aX7nJG1NVC2DRkSg[pV{cW:wIIDyc5RmcW5iYX\0[ZIhPzJiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSB{MD63JO69VS5? NXXTTlRMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1PVgzOzZpPkK3OVk5OjN4PD;hQi=>
MV4-11 MkWwRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MXu3JIRigXN? M2\CW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0MVEyKGOnbHzzJIhiemKxcnnu[{BOVExvQV[0JIFnfGW{IEeg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KEG|c3H5MEBKSzVyIE2gNlUh|ryPLh?= M3PaSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5N{KwOVU2Lz5{N{eyNFU2PTxxYU6=
MV4-11 M3TBWGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M163dGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0MVEyKGOnbHzzJIhiemKxcnnu[{BOVExvQV[0JIZ2e2mxbjDwdo91\WmwIHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUCgQUAzPSEQvF2u NIfuPVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W5PFI{Pid-Mke1PVgzOzZ:L3G+
K562 MoLZRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MX23NkBpenN? NHrkSJhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgbIFz[m:{aX7nJGJEWi2DQlygZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhS0ONOD3iZZNm\CClb3zvdolu\XS{aXOgZZN{[XluIFnDOVAhRSB|Nz64JO69VS5? NVvwTGRJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke3NlA2PTVpPkK3O|IxPTV3PD;hQi=>
K562 M1jZbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUPmdnp5PyCmYYnz M2DmUWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgO{Bl[Xm|IHL5JG1VWyCjc4PhfUwhUUN3MDC9JFM4NjhizszNMi=> Ml2yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3OUiyN|YoRjJ5NUm4NlM3RC:jPh?=
MV4-11 NEHCXFBHfW6ldHnvckBie3OjeR?= NIPkeoQyOCC3TR?= NIntVG04KGSjeYO= MnL2TY5pcWKrdHnvckBw\iCPTFyxMXdFWjVicILveIVqdi2ycn;0[YlvKGmwdHXyZYN1cW:wIHnuJIh2dWGwIF3WOE0yOSClZXzsd{Bp[XKkb4LpcochVUyOLVHGOEBnfXOrb36gdJJwfGWrbjDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIF3MUFEhcGm|dH;u[UBu\XSqeXz0doFve2[ncnHz[UBi[3Srdnn0fUBjgSCvZXHzeZJqdmdicnXkeYN1cW:wIHnuJGg{UzSvZUKgcIV3\WxiYYSgNVAhfU1iYX\0[ZIhPyCmYYnzJIJ6KFenc4Tldo4h[myxdDDt[ZRp NGHOS|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W5PFI{Pid-Mke1PVgzOzZ:L3G+
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 23210835

Protocol (from reference)

Kinase Assay:

[1]
  • In Vitro Histone Methyltransferase (HMT) Assay:

    The HMT assay is performed in 50 mM HEPES pH 7.8, 100 mM NaCl, 1.0 mM EDTA, and 5% glycerol at 22 °C. Each reaction contains 1.5 μCi of the co-factor, 3H-S-adenosylmethionine. H3 10-residue peptide is used as the substrate at 50 μM. Compounds are added at concentrations ranging from 0.125 to 128 μM and incubated with the pre-assembled WDR5/RbBP5/ASH2L complex at a final concentration of 0.5 μM for each protein for 2–5 min. Reactions are initiated by addition of the MLL1 protein at a final concentration of 0.5 μM and allowed to proceed for 30 min before preparing scintillation counting. To count samples, reactions are spotted on separate squares of P81 filter paper and precipitated by submerging in freshly prepared 50 mM sodium bicarbonate buffer with pH 9.0. After washing and drying, samples are vortexed in Ultima Gold scintillation fluid and counted. As a negative control, assays are performed using 0.5 μM MLL1/WDR5/RbBP5/ASH2L complex assembled with the non-interacting mutant, WDR5D107A.
Cell Research:

[1]
  • Cell lines: MV4;11, KOPN8, and K562 cells
  • Concentrations: ~100 μM
  • Incubation Time: 7 days
  • Method:

    MV4;11, KOPN8, and K562 cells are cultured in RPMI 1640 medium (ATCC) supplemented with 10% fetal bovine serum and 100 U/L penicillin-streptomycin and incubated at 37 °C under 5% CO2. Cells are seeded into 12-well plates for suspension at a density of 5 × 105 per well (1 mL) and treated with either vehicle control (DMSO, 0.2%) or MM-102 for 7 days. The medium is changed every 2 days, and compounds are resupplied. The CellTiter-Glo Luminescent Cell Viability Assay kit is used following the manufacturer’s instruction. First, 100 μL of the assay reagent is added into each well, and the content is mixed for 2 min on an orbital shaker to induce cell lysis. After 10 min incubation at room temperature, the luminescence is read on a microplate reader.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 669.8
Formula

C35H49F2N7O4
CAS No. 1417329-24-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(CC)(C(=O)NC(CCCN=C(N)N)C(=O)NC1(CCCC1)C(=O)NC(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F)NC(=O)C(C)C

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