MM-102 (HMTase Inhibitor IX)

製品コードS7265 バッチS726501

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)
		Ethanol	100 mg/mL (149.29 mM)
		Water	50 mg/mL (74.64 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	MM-102（HMTase阻害剤IX）は、細胞を含まないアッセイで0.4 µMのIC50を示す高親和性ペプチドミメティックMLL1阻害剤です。本製品は生理食塩水またはPBS溶液に溶解すると沈殿することがあります。DMSO溶液でストック溶液を調製することをお勧めします。
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, this compound specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. In addition, it effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.

製品説明

MM-102（HMTase阻害剤IX）は、細胞を含まないアッセイで0.4 µMのIC50を示す高親和性ペプチドミメティックMLL1阻害剤です。本製品は生理食塩水またはPBS溶液に溶解すると沈殿することがあります。DMSO溶液でストック溶液を調製することをお勧めします。

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, this compound specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. In addition, it effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.

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. This compound is 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 this compound is 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

https://pubmed.ncbi.nlm.nih.gov/23210835/

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：

Coordinated action of multiple active histone modifications shapes the zygotic genome activation in teleost embryos [ Nat Commun, 2025, 16(1):5222]	PubMed: 40523893
The long non-coding RNA RSDR protects against acute kidney injury in mice by interacting with hnRNPK to regulate DHODH-mediated ferroptosis [ Nat Commun, 2025, 16(1):7483]	PubMed: 40796740
Targeting pancreatic cancer glutamine dependency confers vulnerability to GPX4-dependent ferroptosis [ Cell Rep Med, 2025, 6(2):101928]	PubMed: 39879992
Histone methyltransferase KMT2A promotes pulmonary fibrogenesis via targeting pro-fibrotic factor PU.1 in fibroblasts [ Clin Transl Med, 2025, 15(2):e70217]	PubMed: 39888275
MLL1 downregulation drives hair cell ferroptosis via mitochondrial and endoplasmic reticulum stress mechanisms through PERK-eIF2α-Atf4-Chop and PI3K/Akt-Lrp1 signaling pathway [ Chin Med J (Engl), 2025, 10.1097/CM9.0000000000003633]	PubMed: 40640087
Targeting MLL1/WDR5-Mediated Epigenetic Regulation Mitigates Peritoneal Fibrosis by Reducing p16INK4a [ FASEB J, 2025, 39(8):e70543]	PubMed: 40232893
Fibroblast-specific PRMT5 deficiency suppresses cardiac fibrosis and left ventricular dysfunction in male mice [ Nat Commun, 2024, 15(1):2472]	PubMed: 38503742
Arachidonic acid released by PIK3CA mutant tumor cells triggers malignant transformation of colonic epithelium by inducing chromatin remodeling [ Cell Rep Med, 2024, S2666-3791(24)00179-4]	PubMed: 38614093
MBD2 regulates the progression and chemoresistance of cholangiocarcinoma through interaction with WDR5 [ J Exp Clin Cancer Res, 2024, 43(1):272]	PubMed: 39350229
Deficiency of lncRNA MERRICAL abrogates macrophage chemotaxis and diabetes-associated atherosclerosis [ Cell Rep, 2024, 43(3):113815]	PubMed: 38428421

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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