Antibodies
MM-102
- 貨號 Cat. No.
- S7265
- 規格 Size
- 2mgã€20mg
- 品牌 Brand
- Selleckchem
Description
MM-102
Catalog No.S7265
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM. | |||||
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| Targets | MLL1 | |||||
| IC50 | 0.4 μM [1] | |||||
| 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] | |||||
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Protocol(Only for Reference)
Kinase Assay:
| 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. |
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Cell Assay:
| Cell lines | MV4;11, KOPN8, and K562 cells |
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| 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. |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00985959 | Completed | Multiple Myeloma | Janssen Pharmaceutical K.K. | 2008-07 | Phase 1 |
| NCT01997840 | Not yet recruiting | Multiple Myeloma | Acetylon Pharmaceuticals Incorporated | 2013-11 | Phase 1|Phase 2 |
Chemical Information
| Molecular Weight (MW) | 669.8 |
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| Formula | C35H49F2N7O4 |
| CAS No. | 1417329-24-8 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | HMTase Inhibitor IX |
| Solubility (25°C) * | In vitro | DMSO | 100 mg/mL (149 mM) |
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| Water | 100 mg/mL (149 mM) | ||
| Ethanol | 100 mg/mL (149 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | Cyclopentanecarboxamide, 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]- |
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