Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H20F3N5O |
Molecular Weight | 451.4437 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C=C(C2=C(N)N=CN=C12)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F
InChI
InChIKey=SIXVRXARNAVBTC-UHFFFAOYSA-N
InChI=1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30)
GSK2606414 is an orally bioavailable, potent, selective inhibitor of PERK. The drug may serve as a potential treatment for cancer and neurodegenerative diseases associated with the accumulation and aggregation of misfolded
disease-specific proteins in the brain. GSK2606414 demonstrated good results on a mouse model of prion disease.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24107777
Curator's Comment: GSK2606414 crossed the blood brain barrier in mice.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: Q9NZJ5 Gene ID: 9451.0 Gene Symbol: EIF2AK3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/22827572 |
0.4 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Sample Use Guides
GSK2606414 was given orally twice a day for 21 days at doses of 50 and 150 mg/kg (preclinical study).
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22827572
Lung carcinoma A549 cells were treated with GSK2606414 at doses of 0.03, 0.1 and 0.3 uM for 1 h to test the effect of the drug on cellular PERK phosphorylation.
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GSK2606414
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DTXSID801045605
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53469448
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DPP2K6EFW8
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1337531-36-8
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admin on Sat Dec 16 17:30:57 GMT 2023 , Edited by admin on Sat Dec 16 17:30:57 GMT 2023
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SUBSTANCE RECORD