MM-102

製品コードS7265 バッチS726501

印刷

化学情報

Synonyms

HMTase Inhibitor IX

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₅H₄₉F₂N₇O₄

分子量

669.8

CAS No.

1417329-24-8

Solubility (25°C)*

体外

DMSO

100 mg/mL (149.29 mM)

Water

100 mg/mL (149.29 mM)

Ethanol

100 mg/mL (149.29 mM)

体内（毎回新しく調製した物を用意してください）

	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml
	5% DMSO 1 95% Corn oil	0.83mg/ml

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
in vitro	MM-102, as a MLL1 mimetic, shows high binding affinities to WDR5 with IC50 of 2.9 nM and K_i 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]

製品説明

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

in vitro

MM-102, as a MLL1 mimetic, shows high binding affinities to WDR5 with IC50 of 2.9 nM and K_i 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]

プロトコル(参考用のみ)

キナーゼアッセイ	In Vitro Histone Methyltransferase (HMT) Assay
キナーゼアッセイ	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.
細胞アッセイ	細胞株	MV4;11, KOPN8, and K562 cells
	濃度	~100 μM
	反応時間	7 days
	実験の流れ	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.

参考

[1] Karatas H, et al. J Am Chem Soc. 2013, 135(2), 669-682.

カスタマーフィードバック

: Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 45(4):1529-1540]

: Data from [Data independently produced by , , Mol Cell Biol, 2015, 36(4):615-27]

: Data from [Data independently produced by , , Int J Biol Sci, 2018, 14(9):1122-1132]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Deficiency of lncRNA MERRICAL abrogates macrophage chemotaxis and diabetes-associated atherosclerosis [ Cell Rep, 2024, 43(3):113815]	PubMed: 38428421
H4K20me1 plays a dual role in transcriptional regulation of regeneration and axis patterning in Hydra [ Life Sci Alliance, 2023, 6(5)e202201619]	PubMed: 36944423
Glioblastoma stem cell-specific histamine secretion drives pro-angiogenic tumor microenvironment remodeling [ Cell Stem Cell, 2022, S1934-5909(22)00417-9]	PubMed: 36265493
H3-K27M-mutant nucleosomes interact with MLL1 to shape the glioma epigenetic landscape [ Cell Rep, 2022, 39(7):110836]	PubMed: 35584667
Innate Immune Training of Human Macrophages by Cathelicidin Analogs [ Front Immunol, 2022, 13:777530]	PubMed: 35958593
Targeting matrix metallopeptidase 2 by hydroxyurea selectively kills acute myeloid mixed-lineage leukemia [ Cell Death Discov, 2022, 8(1):180]	PubMed: 35396375
Inhibition of Wdr5 Attenuates Ang-II-Induced Fibroblast-to-Myofibroblast Transition in Cardiac Fibrosis by Regulating Mdm2/P53/P21 Pathway [ Biomolecules, 2022, 12(11)1574]	PubMed: 36358925
Mixed-lineage leukaemia 1 contributes to endometrial stromal cells progesterone responsiveness during decidualization [ J Cell Mol Med, 2020, 10.1111/jcmm.16030]	PubMed: 33201593
Loss of myeloid-specific lamin A/C drives lung metastasis through Gfi-1 and C/EBPε-mediated granulocytic differentiation. [ Mol Carcinog, 2020, 10.1002/mc.23147]	PubMed: 31912614
Chemical Genetics Screen Identifies Epigenetic Mechanisms Involved in Dopaminergic and Noradrenergic Neurogenesis in Zebrafish. [ Front Genet, 2020, 11:80]	PubMed: 32158467

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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