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| Description |
| GSK343 is a potent, selective inhibitor of EZH2 with cellular activity. GSK343 inhibits EZH2 with an IC50 of 4nM and is over 1000-fold selective for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC50 of <200nM as measured by immunofluorescence. GSK343 exhibited limited effects on the growth of EOC cells in conventional two-dimensional (2D) culture. In contrast, GSK343 significantly suppressed the growth of EOC cells cultured in 3D matrigel extracellular matrix (ECM), which more closely mimics the tumor microenvironment in vivo. Notably, GSK343 induces apoptosis of EOC cells in 3D but not 2D culture. In addition, GSK343 significantly inhibited the invasion of EOC cells. |
| Chemical Structure |
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| Chemical Name |
| 1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide |
| SMILES Code |
| O=C(C1=CC(C2=CC(N3CCN(C)CC3)=NC=C2)=CC4=C1C=NN4C(C)C)NCC5=C(CCC)C=C(C)NC5=O |
| Theoretical Analysis |
XingMo Cat#:XM757
Product Name:GSK343
Synonyms:GSK343; GSK-343; GSK 343
CAS#:1346704-33-3
Chemical Formula:C31H39N7O2
Exact Mass:541.31652
Molecular Weight:541.69
Purity:>98%
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| Technical Data |
Purity:
>98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility:
Soluble in DMSO, not in water
Shelf Life:
>2 years if stored properly
Drug Formulation:
This drug may be formulated in DMSO
Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
Harmonized System Code:
293490
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WARNING: This product is for research use only, not for human or veterinary use
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