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YM458

Catalog No. T74542 CAS 2770108-93-3

YM458, a potent dual inhibitor of EZH2 and BRD4, exhibits IC50 values of 490 nM and 34 nM, respectively. This compound effectively hinders cell proliferation and colony formation, while also inducing cell cycle arrest and apoptosis in solid tumor cells, making it a viable candidate for anticancer research [1].

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YM458, CAS 2770108-93-3

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,520.00
50 mg	8-10 weeks	$ 1,980.00
100 mg	8-10 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	YM458, a potent dual inhibitor of EZH2 and BRD4, exhibits IC50 values of 490 nM and 34 nM, respectively. This compound effectively hinders cell proliferation and colony formation, while also inducing cell cycle arrest and apoptosis in solid tumor cells, making it a viable candidate for anticancer research [1].
Targets&IC50	BRD4:34 nM, EZH2:490 nM
In vitro	YM458 (compound D7) demonstrates antiproliferative effects on AsPC-1 pancreatic cancer cells, inhibiting growth with an IC50 value of 0.69 ± 0.16 μM after 6 days at concentrations ranging from 0 to 30 μM. At a dose of 1 μM over 72 hours, YM458 notably reduces H3K27me3 levels and c-Myc expression in AsPC-1 cells [1]. Furthermore, YM458 exhibits inhibitory activity against various solid tumor cell lines; specifically, it markedly diminishes the proliferation of A549 lung and HCT116 colorectal cancer cells at 1 μM within 4 to 6 days of treatment [1]. Additionally, YM458 at submicromolar ranges (0.05-0.4 μM) over 12 to 20 days dose-dependently impedes colony formation in AsPC-1, HCT116, and A549 cell lines [1].
In vivo	YM458 administered intraperitoneally (IP; 60 mg/kg; every other day, for 38 days) exhibited anticancer activity by inhibiting tumor growth in AsPC-1 and A549 cells, with rates of 38.6% and 62.3%, respectively [1]. In female BALB/c mice, pharmacokinetic parameters revealed after IP administration (80 mg/kg), YM458 had a half-life (t1/2) of 3.81 hours and reached its maximum concentration (Cmax) of 27126.3 ng/mL within 1 hour (Tmax), while oral administration (PO) of the same dosage resulted in a longer half-life (4.16 hours), lower peak concentration (4383.6 ng/mL), and a substantially reduced area under the curve (AUC 0-24) of 13509.1 ng/mL·h. The clearance rate (CL) was 4.88 mL/min/kg with an oral bioavailability (F) of 4.94% [1].

Molecular Weight	957.62
Formula	C53H61ClN8O5S
CAS No.	2770108-93-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide UNC0646 WDR5-0102 GSK2807 Trifluoroacetate PF-06726304 PRMT5-IN-2 WM-586 CARM1-IN-1

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

YM458 2770108-93-3 Chromatin/Epigenetic Histone Methyltransferase inhibitor inhibit

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