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Tazemetostat

Inh 1403254-99-8 N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide

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Catalog No. ABIN7233296

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Quick Overview for Tazemetostat (ABIN7233296)

Application

Inhibition (Inh)

Chemical Name

N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)-[1,1'-biphenyl]-3-carboxamide

Purpose

EZH2 inhibitor

Characteristics

Potent and selective SAM-competitive inhibitor of the lysine methyltransferase EZH2 (Ki = 2.5nM wild type human PRC2-containing).1 Displayed strong antiproliferative effects against SMARCB1-deleted malignant rhabdoid tumor (MRT) cell lines in vitro. Antitumor activity was also observed in SMARTCB1 mutant mouse xenografts. Displays potent antitumor activity in various cancer models including non-Hodgkins lymphoma2, pediatric glioma3, small-cell carcinoma of the ovary4, and synovial sarcomas5. Tazemetostat has also been shown to control inflammatory genes by modulating IRF1, IRF8, and STAT1 levels suggesting therapeutic potential for the treatment of neuroinflammatory diseases associated with microglial activation.6

Purity

>98 %

Formula

C34H44N4O4

Solubility

Soluble in DMSO (up to at least 25 mg/ml)
Geldanamycin- FITC
Inh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate

Geldanamycin
Inh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate

Radicicol
Inh 12772-57-5

Geldanamycin- Biotin
Inh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate

Herbimycin A
Inh 70563-58-5 [(2R,3S,5S,6R,7S,8E,10S,11S,12E,14E)-2,5,6,11-tetramethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate

17-GMB-APA-GA
Inh [(3R,5S,6R,7S,10S,11S)-21-[3-[4-(2,5-dioxopyrrol-1-yl)butanoylamino]propylamino]-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate

TEMPO
Inh 2564-83-2 2,2,6,6-Tetramethylpiperidine 1-oxyl, 2,2,6,6-Tetramethyl-1-piperidinyloxy, free radical, (2,2,6,6-Tetramethyl-1-piperidinyl)oxidanyl, 1,1,5,5-tetramethylpentamethylene nitroxide, 2,2,6,6-Tetramethylpiperidine-1-oxyl

Triacsin C
Inh 76896-80-5 (3E)-1-Oxo-3-[(2E,4E,7E)-2,4,7-undecatrien-1-ylidene]triazane

TPCK
Inh 402-71-1 N-(4-Chloro-3-oxo-1-phenyl-2-butanyl)-4-methylbenzenesulfonamide

Staurosporine
Inh 62996-74-1 (2S,3R,4R,6R)-3-Methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one

Application Notes

Optimal working dilution should be determined by the investigator.

Restrictions

For Research Use only
Format

Powder

Storage

-20 °C

Storage Comment

-20°C
Background

EPZ-6438,Transcription,Epigenetics,Proliferation,Protein methyltransferase,Cancer stem cells,Inflammation,Cancer,Posttranslational modification,Neurodegeneration,Chromatin

Molecular Weight

572.8

CAS-No

1403254-99-8