Home > Products > Apoptosis > JAK > PERK > GSK2606414 (Free base)

GSK2606414 (Free base)

(CAS No:1337531-36-8)

GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.

CAS No:1337531-36-8

Molecular Weight(MW):451.44

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

Price and large packaging, please e-mail consultation:info@SuperLan-chem.com

QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	1337531-36-8
Molecular formula(MF)	C₂₄H₂₀F₃N₅O
Molecular Weight(MW):	451.44
Alias

Solubility

In vitro	DMSO	90 mg/mL (199.36 mM)
	Ethanol	19 mg/mL (42.08 mM)
	Water	<1 mg/mL
In vivo	5% DMSO+45% PEG 300+ddH2O	20mg/mL

Biological Activity

Description

GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.

Features

The first PERK-selective inhibitor with good oral bioavailability and crosses the blood-brain barrier.

Targets

EIF2AK3 (PERK) ^[1] (Cell-free assay)	EIF2AK1 (HRI) ^[1] (Cell-free assay)	EIF2AK2 (PKR) ^[1] (Cell-free assay)
0.4 nM	420 nM	696 nM

In vitro

GSK2606414 inhibits PERK Autophosphorylation in A459 Cells with IC50 of <0.3 μM. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human A549 cells	Function assay		2 h	Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting	22827572
human A549 cells	Function assay	0.03 Î¼M	2 h	Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells at 0.03 uM after 2 hrs by Western blotting	22827572
human A549 cells	Function assay		1 h	Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis	24900593

... Click to View More Cell Line Experimental Data

In vivo

GSK2606414 exhibits high oral availability, and low to moderate blood clearance in mouse, rat, and dog. GSK2606414, administered orally, inhibits tumor growth in a dose-dependent manner in mice bearing pancreatic human BxPC3 tumors. ^[1]