GSK2606414

Catalog No. A12792

GSK2606414是口服有效的选择性PERK抑制剂，IC50为0.4 nM。

Product Citations

Linhao Xu, .et al. Suppression of CHOP Reduces Neuronal Apoptosis and Rescues Cognitive Impairment Induced by Intermittent Hypoxia by Inhibiting Bax and Bak Activation, Neural Plasticity, 2021, 23 Aug
Takashi Shimizu, .et al. PERK inhibition attenuates vascular remodeling in pulmonary arterial hypertension caused by BMPR2 mutation, Sci Signal, 2021, Jan 26;14(667):eabb3616 PMID: 33500333

Technical details

Catalog Num	A12792
M. Wt	451.44
Formula	C24H20F3N5O
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1337531-36-8
Synonyms	GSK-2606414, GSK 2606414
SMILES	CN1C=C(C2=C1N=CN=C2N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F

Biological Activity

GSK2606414是口服有效的选择性PERK抑制剂，IC50为0.4 nM。

Targets

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

Solubility *

In vitro (25°C)	DMSO	87 mg/mL (192.71 mM)
	Water	Insoluble
	Ethanol	18 mg/mL (39.87 mM)
In vivo	5% DMSO+45% PEG 300+ddH2O	19 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	22.15 mL	110.76 mL	221.51 mL
0.5 mM	4.43 mL	22.15 mL	44.3 mL
1 mM	2.22 mL	11.08 mL	22.15 mL
5 mM	0.44 mL	2.22 mL	4.43 mL

*The above data is based on the productmolecular weight 451.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.