GSK-343 chemical structure
Chemical structureResearch use only
CAT. NO. DC7143Featured

GSK-343

Pack Sizes & Prices

TotalUS$500
We match the best price and quality on market.
Product overview

Description & Application

GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

ParameterValue
Chemical NameGSK-343
CAS No.1346704-33-3
SynonymsGSK343;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;1-(1-Methylethyl)-N-;1-(1-Methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl...;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-i;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;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;GSK-343;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-[(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-indazole-4-carboxamide;GSK 343;C31H39N7O2;compou;N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-pro
FormulaC31H39N7O2
M.Wt541.6871
SMILESO=C(C1C([H])=C(C([H])=C2C=1C([H])=NN2C([H])(C([H])([H])[H])C([H])([H])[H])C1C([H])=C([H])N=C(C=1[H])N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])N([H])C([H])([H])C1C(N([H])C(C([H])([H])[H])=C([H])C=1C([H])([H])C([H])([H])C([H])([H])[H])=
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

In Vitro

GSK343, which contains an n-propyl group at the 4-position of the pyridone, has EZH2 Kiapp=1.2±0.2 nM. In this 6-day proliferation assay, among the cell lines evaluated in this study, the prostate cancer cell line LNCaP is the most sensitive to EZH2 inhibition, with growth IC50 value of 2.9 μM for GSK343[1]. GSK343 is found to have half maximal inhibitory concentration values of 13 μM in HeLa cells and 15 μM in SiHa cells[2].

In Vivo

Compare with the controls, GSK343 (5 mg/kg)-treated mice exhibits significantly inhibited tumor growth. The average tumor volume and weight of the GSK343-treated cohort is remarkably reduced. As early as 20 days post-implantation, a significant reduction in tumor growth is observed in the GSK343-treated cohort relative to the control cohort; this difference persisted through the remainder of the study. In addition, compare with the control cohort, the GSK343-treated animals in the xenograft model show a remarkable increase in messenger RNA levels of E-cadherin but a significant decrease in vimentin messenger RNA levels[2].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

View online datasheetRequest COA / MSDS

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

Related research products

UNC-1215 chemical structureDC7332

UNC-1215

UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.

View activity & prices
UNC-0638 chemical structureDC7331

UNC-0638

UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.

View activity & prices
UNC0321 chemical structureDC7915

UNC0321

UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.It was found that replacing the 5-carbon chain in…

View activity & prices
UNC0379 chemical structureDC7671

UNC0379

UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 uM; selective over 15 other methyltransferases.UNC0379 is a synthetic small-molecule inhibitor that…

View activity & prices
EPZ011989 chemical structureDC7927

EPZ011989

EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt…

View activity & prices

Cart

Request quotation