GSK126, EZH2 Histone methyltransferase inhibitor (TBI3394)
$126.00 – $585.00
EZH2 Histone methyltransferase inhibitor
SKU | Stock | SIZE (mg) | Price | Quantity | ||
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TBI3394-5MG | Yes | 5 MG | $126.00 | |||
TBI3394-25MG | Yes | 25 MG | $585.00 |
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Description
Product Details
Formal 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
Alternate Names: GSK-2816126
Molecular Formula: C31H38N6O2
Formula Weight: 526.70
CAS Number: 1346574-57-9
Purity: >98%
Formulation: powder
Solubility: Soluble in DMSO (up to 16 mg/ml)
Storage: -20°C
Stability: ≥ 2 years.
Applications
EZH2 Histone methyltransferase inhibitor
Functions
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 methyltransferases. 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 mice. Rescues exhausted CD8+ T cells in HCV infection. Facilitates the transition of embryonic stem cells to feeder-free extended pluripotent stem cells in combination with a cocktail of other agents. Displays neuroprotective effects in ischemic brain injury in a rodent model.
Application Procedures
First dissolved in DMSO (up to 16 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.
Additional information
SIZE (mg) | 25 MG, 5 MG |
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