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GSK126

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

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Quick Overview for GSK126 (ABIN7233255)

Application

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

Purpose

EZH2 Histone methyltransferase inhibitor

Characteristics

A potent, selective, S-adenosyl-methionine-competitive inhibitor of EZH2 methyltransferase, Ki=0.5-3 nM, >150-fold selective for EZH2 over EZH1 and >1000-fold selective over 20 methyltransferases1. Decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 inhibits proliferation of diffuse large B-cell lymphoma (DLBCL) cell lines as well as DLBCL xenografts in mice1. Rescues exhausted CD8+ T cells in HCV infection2. Facilitates the transition of embryonic stem cells to feeder-free extended pluripotent stem cells in combination with a cocktail of other agents3. Displays neuroprotective effects in ischemic brain injury in a rodent model4.

Purity

>98 %

Formula

C31H38N6O2

Solubility

Soluble in DMSO (up to 16 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

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