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GSK-126

Inh 1346574-57-9 N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide

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Catalog No. ABIN7233255

Datasheet as PDF

Application

Inhibition (Inh)

Purpose

EZH2 Histone methyltransferase inhibitor

Characteristics

Competitive, selective inhibitor of H3K27 methyltransferase EZH2 (Ki = 0.57 nM), over EZH1 (Ki = 89 nM) and other histone methyltransferases (Ki > 1 μM). GSK-126 caused a dose-dependent decrease in H3K27me3, and blocked invasion of triple-negative breast cancer cells. Conversely, it induced myeloid-derived suppressor cells, blocking antitumor immunity in mice. Decreases myeloma CSCs4, while also inducing differentiation of HepaRG hepatic progenitor cells5. Used to explore the role of epigenetic modification in a mouse model of Parkinson's disease.

Purity

>98 %

Chemical Name

N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide

Formula

C31H38N6O2

Solubility

Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 2 mg/ml).
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- 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

Nicotinamide
Inh 98-92-0 Pyridine-3-carboxylic acid amide

5-Azacytidine
Inh Cell-permeable 320-67-2 4-Amino-1-ß-D-ribofuranosyl-1,3,5-triazin-2(1H)-one

SAHA (Vorinostat)
Inh Cell-permeable 149647-78-9 Suberoylanilide-hydroxamic acid

Phenylbutyrate Na
Inh 1716-12-7 4-Phenylbutyric acid, sodium salt

CI-994
Inh 112522-64-2 4-(Acetylamino)-N-(2-aminophenyl)benzamide

Tranylcypromine hemisulfate (±)
Inh Cell-permeable 13492-01-8 Trans (±)-2-phenylcyclopropanamine, hemisulfate salt

Tenovin-1
Inh 380315-80-0 N-[(4-Acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide

Restrictions

For Research Use only
Format

Powder

Storage

-20 °C
Background

GSK-2816126,Cell migration,Epigenetics,Transcription,Protein methyltransferase,Stem cells,Cancer stem cells,Ubiquitin/Proteasome,Inflammation,Cancer,Neurodegeneration,Posttranslational modification,Pain,Chromatin

Molecular Weight

526.7

CAS-No

1346574-57-9