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EZH2-IN-4

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Catalog No. T39497Cas No. 2088132-99-2
Alias EZH2-IN-4

EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.

EZH2-IN-4

EZH2-IN-4

😃Good
Catalog No. T39497Alias EZH2-IN-4Cas No. 2088132-99-2
EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.
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5 mg$970InquiryInquiry
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Product Introduction

Bioactivity
Description
EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.
Targets&IC50
EZH2 (mutant 5-mer):2.65 nM (IC50), EZH2 (WT 5-mer):0.923 nM (IC50)
In vitro
EZH2-IN-4 (example 38) exhibits potent inhibition in Karpas-422 (EZH2 Y641N) cells with an H3K27me3 IC50 of 0.00973 nM and an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1]. It suppresses the growth of various ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3), with IC50 values r ng ng from 0.02 to 8.6 μM, while show ng no inhibitory effect on SKOV3, HeyA8, and HEC59 cells (IC50 > 20 μM)[1].
In vivo
'EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) shows 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1]. Additionally, administered twice daily at 50 mpk orally (po) with a 5-day pretreatment, followed by at least 23 days of concurrent administration with gemcitabine and cisplatin, it significantly inhibits tumor growth in the A2780 xenograft model[1].'
SynonymsEZH2-IN-4
Chemical Properties
Molecular Weight511.73
FormulaC29H41N3O3S
Cas No.2088132-99-2
Smiles[H][C@@]1(CC[C@@H](CC1)N1CC(C1)OC)[C@@H](C)c1sc2CCCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1C |wU:13.15,1.14,wD:4.7,1.0,(-2.14,-2.64,;-3.68,-2.64,;-2.91,-3.98,;-3.68,-5.31,;-5.22,-5.31,;-5.99,-3.98,;-5.22,-2.64,;-5.99,-6.64,;-5.59,-8.13,;-7.08,-8.53,;-7.48,-7.04,;-7.85,-9.86,;-9.39,-9.86,;-2.91,-1.31,;-3.68,.03,;-1.37,-1.31,;-.46,-.06,;1,-.54,;2.21,.42,;3.71,.08,;4.37,-1.31,;3.71,-2.7,;4.67,-3.9,;6.19,-3.67,;6.75,-2.24,;5.79,-1.03,;8.27,-2.01,;9.23,-3.21,;10.76,-2.98,;8.67,-4.65,;7.15,-4.87,;6.59,-6.31,;2.21,-3.04,;1.86,-4.54,;1,-2.08,;-.46,-2.55,;-.94,-4.02,)|
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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Keywords

EZH-2-IN-4EZH2IN4EZH2 IN 4
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