Description Features In vitro
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GSK 343

Description Features In vitro
GSK 343 Structure
GSK 343
  • CAS No.1346704-33-3
  • Chemical Name:GSK 343
  • CBNumber:CB52666625
  • Molecular Formula:C31H39N7O2
  • Formula Weight:541.69
  • MOL File:1346704-33-3.mol
GSK 343 Property
  • Boiling point 797.4±60.0 °C(Predicted)
  • Density 1.26±0.1 g/cm3(Predicted)
  • storage temp. 2-8°C
  • solubility DMSO: soluble15mg/mL, clear
  • form powder
  • pka 11.84±0.10(Predicted)
  • color , white to beige to brown
  • InChIKey ULNXAWLQFZMIHX-UHFFFAOYSA-N
  • UNSPSC Code 41106514
  • NACRES NA.77
Safety
  • Hazard Codes  :Xn
  • Risk Statements  :22
  • WGK Germany  :3
  • NFPA 704:
    0
    2 0
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302
  • Precautionary statements P301+P312+P330
GSK 343 Price More Price(2)
  • Brand: Sigma-Aldrich(India)
  • Product number: SML0766
  • Product name : GSK343
  • Purity: ≥98% (HPLC)
  • Packaging: 5MG
  • Price: ₹14267.35
  • Updated: 2022/06/14
  • Buy: Buy
  • Brand: Sigma-Aldrich(India)
  • Product number: SML0766
  • Product name : GSK343
  • Purity: ≥98% (HPLC)
  • Packaging: 25MG
  • Price: ₹58054.48
  • Updated: 2022/06/14
  • Buy: Buy

GSK 343 Chemical Properties,Usage,Production

  • Description GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.
  • Features A chemical probe for the SGC epigenetics initiative. Potential use in a variety of solid tumors.
  • In vitro GSK343 inhibits trimethylation of H3K27 (H3K27me3) with IC50 of 174 nM in HCC1806 breast cancer cells. GSK343 potently inhibits cell proliferation in breast cancer cells and prostate cancer cells, and the prostate cancer cell line LNCaP is the most sensitive to GSK343, with IC50 of 2.9 μM. GSK343 significantly suppresses the growth of EOC cells cultured in 3D matrigel extracellular matrix (ECM), which mimics the tumor microenvironment in vivo. In addition, GSK343 also induces apoptosis of EOC cells in 3D and significantly inhibits the invasion of EOC cells.
  • Uses GSK343 has been used:
    • as an inhibitor of?enhancer of zeste homolog 2 (EZH2) to assess the impact of chromatin condensation on?cell migration
    • as histone methyl transferase inhibitor, to suppress the Polyandrocarpa misakiensis, mitochondrial non-coding-region (NCR) PmNCR?reporter gene expression, facilitated?by TC14-3
    • as a supplement in the growth medium to inhibit the generation of H3K27me3 or to inhibit RNA polymerase II
    • as EZH2 inhibitor to treat castration-resistant neuroendocrine prostate cancer (CRPC-NE)

  • Definition ChEBI: GSK343 is a member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM). It has a role as an EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor, an apoptosis inducer and an antineoplastic agent. It is a N-alkylpiperazine, a secondary carboxamide, an aminopyridine, a pyridone, a N-arylpiperazine and a member of indazoles.
  • Biological Activity gsk343 is a selective and sam-competitive inhibitor of the histone lysine methyltransferase ezh2 with ic50 value of 4 nm [1].ezh2 (enhancer of zestehomolog 2) is a catalytic subunit of the protein complex (polycomb repressive complex 2, prc2). it catalyzes the methylation of h3k27 through transferring the methyl group of sam to h3k27. the trimethylation of h3k27 subsequently results in the transcription suppression of target genes such as runx3, foxc1 and brca1. the overexpression and mutation of ezh2 have been found in many sorts of tumors demonstrating that ezh2 is an attractive target for the treatment of cancers. as a potent ezh2 inhibitor, gsk343 inhibits the activity of the enzyme via competing with the cofactor sam [1, 2].gsk343 is a selective ezh2 inhibitor. it showed no significant inhibitory effects on other enzymes requiring sam as cofactor, including dnmt, mll, prmt and setmar. gsk343 exerted a certain degree of effective on ezh1 with ic50 value of 240 nm since ezh1 was quite homologous to ezh2. in cultured hcc1806 breast cancer cells, treatment of gsk343 dose-dependently reduced h3k27me3 with ic50 value of 174 nm. besides that, 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. it enhanced the antitumor activity of sorafenib which was a multikinase inhibitor and could decrease the expression of ezh2 in hepg2 cells [1, 3 and 4].gsk343 is only used as a tool to investigate ezh2 in vitro because of its high clearance in the animal model [1].
  • Biochem/physiol Actions GSK343 is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase EZH2. GSK343 inhibits EZH2 enzymatic activity with an IC50 of 4 nM. The compound displays 60 fold selectivity for EZH2 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. For full characterization details, please visit the GSK343 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
  • target EZH2
  • storage Store at -20°C
  • References [1] verma s k, tian x, lafrance l v, et al. identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase ezh2. acs medicinal chemistry letters, 2012, 3(12): 1091-1096.
    [2] ferraro a, boni t, pintzas a. ezh2 regulates cofilin activity and colon cancer cell migration by targeting itga2 gene. plos one, 2014, 9(12): e115276.
    [3] amatangelo m, garipov a, li h, et al. three-dimensional culture sensitizes epithelial ovarian cancer cells to ezh2 methyltransferase inhibition. cell cycle, 2013, 12(13): 2113-2119.
    [4] liu t p, lo h l, wei l s, et al. s-adenosyl-l-methionine-competitive inhibitors of the histone methyltransferase ezh2 induce autophagy and enhance drug sensitivity in cancer cells. anti-cancer drugs, 2015, 26(2): 139.
GSK 343 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK 343 Suppliers
Global(154)Suppliers
  • Supplier：
    career henan chemical co
  • Tel：+86-0371-86658258<br/>+8613203830695
  • Email：factory@coreychem.com
  • Country：China
  • ProdList：29808
  • Advantage：58
  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：+1-781-999-5354<br/>+1-00000000000
  • Email：marketing@targetmol.com
  • Country：United States
  • ProdList：32159
  • Advantage：58
GSK 343 Spectrum
1346704-33-3, GSK 343Related Search:
  • Inhibitors
  • API
  • 医用原料
  • 抑制剂
  • 化工试剂
  • 合成有机化合物配体
  • 药靶配体
  • 细胞生物学试剂
  • 小分子抑制剂，天然产物
  • 医药原料
  • 细胞周期
  • C31H39N7O2
  • 化合物GSK343,10 MM DMSO 溶液
  • GSK343,HISTONE H3-LYSINE 27 (H3K27) METHYLTRANSFERASE EZH2抑制剂
  • GSK343,细胞可穿透的HISTONE H3-赖氨酸27(H3K27)甲基转移酶EZH2抑制剂
  • 1-异丙基-N-((6-甲基-2-氧代-4-丙基-1,2-二氢吡啶-3-基)甲基)-6-(2-(4-甲基哌嗪-1-基)吡啶-4-基)-1H-吲唑-4-甲酰胺
  • N-((2-羟基-6-甲基-4-丙基-3-吡啶基)甲基)-1-异丙基-6-(2-(4-甲基-1-哌嗪基)-4-吡啶基)-1H-吲唑-4-甲酰胺
  • 化合物GSK343
  • EZH2抑制剂(GSK343)
  • 1-异丙基-N-[(6-甲基-2-氧代-4-丙基-1,2-二氢-3-吡啶基)甲基]-6-[2-(4-甲基-1-哌嗪基)-4-吡啶基]-1H-吲唑-4-甲酰胺
  • 2-二氢-3-吡啶基)甲基]-6-[2-(4-甲基-1-哌嗪基)-4-吡啶基]-1H-吲唑-4-甲酰胺
  • 1-异丙基-N-[(6-甲基-2-氧代-4-丙基-1
  • 1346704-33-3
  • GSK343, 10 mM in DMSO
  • GSK343, histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor
  • 1-(1-Methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[2-(4-methyl-1-piper
  • 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
  • N-[(6-METHYL-2-OXO-4-PROPYL-1H-PYRIDIN-3-YL)METHYL]-6-[2-(4-METHYLPIPERAZIN-1-YL)PYRIDIN-4-YL]-1-PROPAN-2-YLINDAZOLE-4-CARBOXAMIDE
  • N-((2-hydroxy-6-methyl-4-propylpyridin-3-yl)methyl)-1-isopropyl-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide
  • GSK343;GSK 343;GSK-343
  • 1-isopropyl-n-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)m Ethyl]-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1h-indazole-4-c Arboxamide
  • CS-728
  • GSK 343 USP/EP/BP
  • 1-Isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazi
  • GSK343, >=98%
  • N-[(6-Methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-(propan-2-yl)-1H-<WBR
  • 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
  • N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-py
  • 1-(1-Methylethyl)-N-[(6-Methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)Methyl]-6-[2-(4-Methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxaMide
  • GSK-343/GSK343
  • GSK-343
  • GSK343
  • GSK 343
  • 1-(1-Methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide GSK343
  • 1H-Indazole-4-carboxamide, N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-

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