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Purity: ≥98%
GSK343 is a novel, highly potent and selective inhibitor of H3-lysine 27 (H3K27) methyltransferase EZH2 with antineoplastic activity. It inhibits EZH2 with an IC50 of 4 nM in a cell-free assay, and displays >60 fold selectivity for EZH2 over EZH1, and other histone methyltransferases. GSK343 was found to inhibit cell proliferation in some breast and prostate cancer cells. In LNCaP cells, GSK343 suppressed cell growth with IC50 value of 2.9 μM. In human EOC cells, GSK343 notably inhibited cell invasion and induced cell apoptosis. GSK343 was also found to induce LC3-II accumulation and autophagy in A549, MDA-MB-231 and HepG2 cell.
| ln Vitro |
The scaffold line LNCaP was the most susceptible to EZH2 tension among the cell lines in this study, and the growth IC50 value of GSK343 was 2.9 μM >[1]. GSK343 has a positive quenching at position 4 of pyridine, with EZH2 Kiapp=1.2±0.2 nM. GSK343 was discovered to have a half-maximum amplification concentration value of 13 μM in HeLa cells and 15 μM in SiHa cells [2].
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| ln Vivo |
Mice treated with GSK343 (5 mg/kg) showed a substantial reduction of tumor growth when compared to the control group. The group treated with GSK343 experienced a significant reduction in both mean tumor volume and weight. The GSK343-treated group showed a significant reduction in tumor growth as early as 20 days after implantation when compared to the control group; this difference has been consistently reported in additional investigations. Additionally, compared to controls, animals treated with GSK343 in xenograft models exhibited significantly higher levels of E-cadherin messenger RNA but significantly lower levels of vimentin messenger RNA [2].
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| References |
[1]. Sharad K, et al. Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6.
[2]. Ding M, et al. The polycomb group protein enhancer of zeste 2 is a novel therapeutic target for cervical cancer. Clin Exp Pharmacol Physiol. 2015 May;42(5):458-64 |
| Molecular Formula |
C31H39N7O2
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| Molecular Weight |
541.69
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| CAS # |
1346704-33-3
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| Related CAS # |
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| SMILES |
O=C(C1=CC(C2=CC(N3CCN(C)CC3)=NC=C2)=CC4=C1C=NN4C(C)C)NCC5=C(CCC)C=C(C)NC5=O
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| InChi Key |
ULNXAWLQFZMIHX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)
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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.
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| Synonyms |
GSK-343; GSK 343; GSK343
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8461 mL | 9.2304 mL | 18.4607 mL | |
| 5 mM | 0.3692 mL | 1.8461 mL | 3.6921 mL | |
| 10 mM | 0.1846 mL | 0.9230 mL | 1.8461 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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