- 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
Biological Activity
GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 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 |
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. |
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.
Catalog Num | A12792 |
---|---|
Actions | Inhibitor |
CAS No. | 1337531-36-8 |
Formula | C24H20F3N5O |
M. Wt | 451.44 |
Purity | >98% |
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 |
Storage | Store lyophilized at -20ºC, keep desiccated. |
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