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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

1 image

Produktnummer ABIN7233255

Kurzübersicht für GSK-126 (ABIN7233255)

Applikation

Inhibition (Inh)

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

Verwendungszweck

EZH2 Histone methyltransferase inhibitor

Produktmerkmale

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.

Reinheit

>98 %

Formel

C31H38N6O2

Löslichkeit

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

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

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

Anacardic Acid
Inh 16611-84-0 2-Hydroxy-6-pentadecylbenzoic acid

EX-527
Inh Cell-permeable 49843-98-3 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-xarboxamide (racemic)

Resveratrol
Act 501-36-0 3,4',5-Trihydroxy-trans-stilbene

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

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

Beschränkungen

Nur für Forschungszwecke einsetzbar
Format

Powder

Lagerung

-20 °C
Hintergrund

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

Molekulargewicht

526.7

CAS-Nummer

1346574-57-9