Molecular structure of GSK343
GSK343 (CAS 1346704-33-3)
See product citations (1)
Alternate Names:
N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide
Application:
GSK343 is an inhibitor of the histone lysine methyltransferase ENX-1
CAS Number:
1346704-33-3
Molecular Weight:
541.69
Molecular Formula:
C31H39N7O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GSK343 is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase ENX-1 (EZH2). GSK343 inhibits ENX-1 enzymatic activity with an IC50 of 4 nM. The compound displays 60 fold selectivity for ENX-1 vs. EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. The IC50 for inhibition of H3K27 methylation is < 200 nM in HCC1806 cells.
GSK343 (CAS 1346704-33-3) References
- Fuse-binding protein 1 is a target of the EZH2 inhibitor GSK343, in osteosarcoma cells. | Xiong, X., et al. 2016. Int J Oncol. 49: 623-8. PMID: 27278257
- [Therapeutic effect of enhancer of Zeste homolog 2 inhibitor GSK343 on periodontitis by regulating macrophage differentiation]. | Zhongchao, W., et al. 2017. Hua Xi Kou Qiang Yi Xue Za Zhi. 35: 264-268. PMID: 28675010
- The EZH2 inhibitor GSK343 suppresses cancer stem-like phenotypes and reverses mesenchymal transition in glioma cells. | Yu, T., et al. 2017. Oncotarget. 8: 98348-98359. PMID: 29228694
- Inhibition of histone methyltransferase EZH2 in Schistosoma mansoni in vitro by GSK343 reduces egg laying and decreases the expression of genes implicated in DNA replication and noncoding RNA metabolism. | Pereira, ASA., et al. 2018. PLoS Negl Trop Dis. 12: e0006873. PMID: 30365505
- GSK343 induces autophagy and downregulates the AKT/mTOR signaling pathway in pancreatic cancer cells. | Xu, H., et al. 2019. Exp Ther Med. 18: 2608-2616. PMID: 31572509
- [Effects of Histone Methyltransferase Inhibitors on the Survival, Apoptosis and Cell Cycle of Raji Cells]. | Xiao, LR., et al. 2019. Sichuan Da Xue Xue Bao Yi Xue Ban. 50: 305-310. PMID: 31631594
- GSK343 induces programmed cell death through the inhibition of EZH2 and FBP1 in osteosarcoma cells. | Xiong, X., et al. 2020. Cancer Biol Ther. 21: 213-222. PMID: 31651209
- p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma. | Yang, PM., et al. 2019. Am J Cancer Res. 9: 2120-2139. PMID: 31720078
- GSK343, an inhibitor of EZH2, mitigates fibrosis and inflammation mediated by HIF-1α in human peritoneal mesothelial cells treated with high glucose. | Wang, Q., et al. 2020. Eur J Pharmacol. 880: 173076. PMID: 32222493
- EZH2 inhibition decreases neuroblastoma proliferation and in vivo tumor growth. | Bownes, LV., et al. 2021. PLoS One. 16: e0246244. PMID: 33690617
- EZH2 inhibitor GSK343 inhibits sepsis-induced intestinal disorders. | Yue, D., et al. 2021. Exp Ther Med. 21: 437. PMID: 33747174
- EZH2 inhibits NK cell-mediated antitumor immunity by suppressing CXCL10 expression in an HDAC10-dependent manner. | Bugide, S., et al. 2021. Proc Natl Acad Sci U S A. 118: PMID: 34301901
- Acquired Resistance to EZH2 Inhibitor GSK343 Promotes the Differentiation of Human DLBCL Cell Lines toward an ABC-Like Phenotype. | Preston, SEJ., et al. 2022. Mol Cancer Ther. 21: 511-521. PMID: 35086959
- Progranulin regulates the development and function of NKT2 cells through EZH2 and PLZF. | Du, Z., et al. 2022. Cell Death Differ. 29: 1901-1912. PMID: 35449211
- GSK343, an Inhibitor of Enhancer of Zeste Homolog 2, Reduces Glioblastoma Progression through Inflammatory Process Modulation: Focus on Canonical and Non-Canonical NF-κB/IκBα Pathways. | Scuderi, SA., et al. 2022. Int J Mol Sci. 23: PMID: 36430394
Inhibitor of:
β-defensin 40, β-defensin 42, β-defensin 43, β-defensin 50, β-defensin 8, 2900008C10Rik, AEBP2, ANKRD24, ASH2L, BPTF, D630045J12Rik, DPY-30, E74 like ETS transcription factor (ELF), EG385328, EG546205, EG546325, EHMT1, ENX-1, EPC2, Evi-1, EZHIP, FAM119A, Gal11, GLT8D3, Histone cluster 1 H2AA, Histone cluster 1 H2AB, Histone cluster 1 H3D, Histone cluster 1 H4M, Histone H2B, HSZFP36, KMT5 (lysine methyltransferase), L3MBTL3, Mael, Med17, Menin, Mettl7a2-Higd1c, MPc2, MSL3L1, MSL3L2, NSD2, Obox3, PCGF6, PHC2, PHC3, PHF1, PHF20, PHF21B, PHF23, PHRF1, Polycomb, PRDM12, PRDM15, PRDM6, PRHOXNB, RING1, Set1A, Sin4p, Sum1, TRIM12, Trimethyl Histone H3, VSTM2A, Zfp931, ZMYND17, ZNF197, ZNF198, ZNF250, ZNF251, ZNF274, ZNF334, ZNF337, ZNF34, ZNF341, ZNF343, ZNF434, ZNF445, ZNF502, ZNF508, ZNF519, ZNF532, ZNF572, ZNF588, ZNF619, ZNF621, ZNF623, ZNF806, and ZNF81.Activator of:
1700011H14Rik, BAF53B, BAZ1A, BC094916, BRD9, BRWD3, CARM1, D4Wsu53e, DDB1, DXBay18, EG236663, EG545802, EG625480, Histone cluster 1 H2BH, Lamin A, MAGE-A4, Mel-18, MTF-2, Nkx-2.2, PRPF31, STH1, and WIZ.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK343, 5 mg | sc-397025 | 5 mg | $151.00 | |||
GSK343, 25 mg | sc-397025A | 25 mg | $461.00 |