Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G125654-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $116.90 | |
G125654-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $526.90 | |
G125654-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $640.90 |
Potent and selective PERK inhibitor
Synonyms | AC-29016 | 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone | Ethanone, 1-(5-(4-amino-7-methyl-7H-pyrrolo(2,3-d)pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl)-2-(3-(trifluoromethyl)phenyl)- | 1-[5-(4-a |
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Specifications & Purity | ≥98% |
Biochemical and Physiological Mechanisms | Potent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC50= 0.4 nM). Exhibits >1000-fold selectivity for PERK over HR1 and PKR. Inhibits thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells. Attenuates subcutaneous pancr |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Note | 卖完停产,不再备货 |
Product 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. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone |
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INCHI | 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) |
InChi Key | SIXVRXARNAVBTC-UHFFFAOYSA-N |
Canonical SMILES | CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F |
Isomeric SMILES | CN1C=C(C2=C(N=CN=C21)N)C3=CC4=C(C=C3)N(CC4)C(=O)CC5=CC(=CC=C5)C(F)(F)F |
PubChem CID | 53469448 |
Molecular Weight | 451.44 |
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Solubility | Solvent:DMSO, Max Conc. mg/mL: 45.14, Max Conc. mM: 100 |
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1. Xiaohua Xie, Xiaofeng Wu, Dongsheng Zhao, Ying Liu, Qiyue Du, Yitian Li, Yaping Xu, Yuhang Li, Yan Qiu, Yungang Yang. (2023) Fluvoxamine alleviates bleomycin-induced lung fibrosis via regulating the cGAS-STING pathway. PHARMACOLOGICAL RESEARCH, 187 (106577). [PMID:36435270] |
1. Xiaohua Xie, Xiaofeng Wu, Dongsheng Zhao, Ying Liu, Qiyue Du, Yitian Li, Yaping Xu, Yuhang Li, Yan Qiu, Yungang Yang. (2023) Fluvoxamine alleviates bleomycin-induced lung fibrosis via regulating the cGAS-STING pathway. PHARMACOLOGICAL RESEARCH, 187 (106577). [PMID:36435270] |