GSK343 - CAS 1346704-33-3
Catalog number:
1346704-33-3
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
EZH2
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.
Publictions citing BOC Sciences Products
  • >> More
Synonyms:
GSK343; GSK-343; GSK 343.
MSDS:
Inquire
Current Developer:
GSK
1.In silico and experimental analyses predict the therapeutic value of an EZH2 inhibitor GSK343 against hepatocellular carcinoma through the induction of metallothionein genes.
Liu TP1, Hong YH2, Tung KY2, Yang PM3. Oncoscience. 2016 Jan 29;3(1):9-20. eCollection 2016.
There are currently no effective molecular targeted therapies for hepatocellular carcinoma (HCC), the third leading cause of cancer-related death worldwide. Enhancer of zeste homolog 2 (EZH2), a histone H3 lysine 27 (H3K27)-specific methyltransferase, has been emerged as novel anticancer target. Our previous study has demonstrated that GSK343, an S-adenosyl-L-methionine (SAM)-competitive inhibitor of EZH2, induces autophagy and enhances drug sensitivity in cancer cells including HCC. In this study, an in silico study was performed and found that EZH2 was overexpressed in cancerous tissues of HCC patients at both gene and protein levels. Microarray analysis and in vitro experiments indicated that the anti-HCC activity of GSK343 was associated with the induction of metallothionein (MT) genes. In addition, the negative association of EZH2 and MT1/MT2A genes in cancer cell lines and tissues was found in public gene expression database. Taken together, our findings suggest that EZH2 inhibitors could be a good therapeutic option for HCC, and induction of MT genes was associated with the anti-HCC activity of EZH2 inhibitors.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related EZH2 Products


EPZ011989
(CAS: 1598383-40-4)

EPZ011989 is a potent, orally-available EZH2 inhibitor with robust in vivo activity. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenog...

GSK-503
(CAS: 1346572-63-1)

GSK-503 is a potent EZH2 inhibitor with potential anticancer activity. Increased activity of the epigenetic modifier EZH2 has been associated with different can...

ZLD1039
(CAS: 1826865-46-6)

ZLD1039 potent, highly selective, and orally bioavailable small molecule inhibitor of EZH2, which inhibited the methyltransferase activity of EZH2 with high se...

EPZ011989 trifluoroacetate
(CAS: 1598383-41-5)

EPZ011989 trifluoroacetate is the trifluoroacetate salt form of EPZ011989. EPZ011989 is a potent and orally bioavailable inhibitor that specifically targets the...

CAS 1403254-99-8 EPZ-6438

EPZ-6438
(CAS: 1403254-99-8)

EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation ...

CAS 1396772-26-1 EPZ005687

EPZ005687
(CAS: 1396772-26-1)

EPZ005687 is a selective EZH2 enzyme inhibitor with Ki of 24 nM. It is 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyl...

CAS 102052-95-9 3-Deazaneplanocin A

3-Deazaneplanocin A
(CAS: 102052-95-9)

3-Deazaneplanocin A (DZNep), an inhibitor of S-adenosylmethionine-dependent methyltransferase that targets the degradation of EZH2.

CAS 1431612-23-5 UNC-1999

UNC-1999
(CAS: 1431612-23-5)

UNC1999, the first orally bioavailable inhibitor that has high in vitro potency for wildtype and mutant EZH2 as well as EZH1. UNC1999 was highly selective for E...

CAS 1346574-57-9 GSK126

GSK126
(CAS: 1346574-57-9)

GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. GSK126 decreases global H3...

CAS 1450655-76-1 CPI-169

CPI-169
(CAS: 1450655-76-1)

CPI-169 is a novel and potent EZH2 inhibitor, it decreases cellular levels of H3K27me3 and triggers cell cycle arrest and apoptosis in a variety of cell lines.

CAS 120964-45-6 3-deazaneplanocin A (DZNeP) HCl

3-deazaneplanocin A (DZNeP) HCl
(CAS: 120964-45-6)

3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.

CPI-360
(CAS: 1802175-06-9)

CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.

CAS 1346704-33-3 GSK343

GSK343
(CAS: 1346704-33-3)

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...

CAS 1418308-27-6 EI1

EI1
(CAS: 1418308-27-6)

EI1 inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression.

Chemical Structure

CAS 1346704-33-3 GSK343

Quick Inquiry

Verification code

Featured Items