[CAS NO. 1346704-33-3] GSK343

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PRODUCTS SPECIFICATIONS [1346704-33-3]

Catalog

SLK-S7164

Brand

Selleck

CAS

1346704-33-3

DESCRIPTION [1346704-33-3]

Overview

MDL	MFCD25563250
Molecular Weight	541.69
Molecular Formula	C31H39N7O2
SMILES	C(NCC1=C(CCC)C=C(C)NC1=O)(=O)C2=C3C(N(C(C)C)N=C3)=CC(=C2)C=4C=C(N=CC4)N5CCN(C)CC5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	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	-	-	-
50 mM	-	-	-

Description

GSK343 is a potent and selective inhibitor with of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces .

Features

A chemical probe for the SGC epigenetics initiative. Potential use in a variety of solid tumors.

Targets

EZH2 ^[1] (Cell-free assay)	EZH1 ^[1] (Cell-free assay)
4 nM	240 nM

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.

References

[1] Verma SK, et al. ACS Med Chem Lett. 2012, 3, 1091-1096.
[2] Amatangelo MD, et al. Cell Cycle. 2013, 12(13), 2113-2119.
[3] Wang X, et al. Theranostics. 2022 Jan 31;12(5):2063-2079.

Synonyms

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]-

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

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