2. Epigenetics
  3. Histone Methyltransferase
  4. EZH2-IN-4

EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.

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EZH2-IN-4 Chemical Structure

EZH2-IN-4 Chemical Structure

CAS No. : 2088132-99-2

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EZH2-IN-4 Related Antibodies

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View All Histone Methyltransferase Isoform Specific Products:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity[1].

IC50 & Target[1]

WT 5-mer EZH2

0.923 nM (IC50)

mut 5-mer EZH2

2.65 nM (IC50)

In Vitro

EZH2-IN-4 (example 38) shows a cell H3K27me3 IC50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1].
EZH2-IN-4 shows an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1].
EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC50s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC50>20 μM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EZH2-IN-4 Related Antibodies
In Vivo

EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1].
EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

511.72

Formula

C29H41N3O3S
CAS No.
SMILES

CC1=C([C@@H]([C@@]2([H])CC[C@@](N3CC(C3)OC)([H])CC2)C)SC(CCCN4CC5=C(C=C(NC5=O)C)C)=C1C4=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EZH2-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EZH2-IN-42088132-99-2Histone MethyltransferaseH3K27me3Karpas-422Y641NKj?pas-422ovarianCOV-434TOV-21GTOV-112DA2780Caov-3OVCAR3SKOV3HeyA8HEC59Inhibitorinhibitorinhibit

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