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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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E610266-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $920.90 | |
E610266-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $3,220.90 |
Synonyms | Ezurpimtrostat | Gns 561 | GNS 561 [WHO-DD] | GNS561 | GNS-561 | GTPL11991 | 4-[4-(tert-butylamino)piperidin-1-yl]-N-[(4-chlorophenyl)methyl]quinolin-2-amine | 1914148-72-3 | SCHEMBL17713568 | CS-0143466 | UNII-MS6LGW5JFK | AKOS040757126 | MS6LGW5JFK | 2- |
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Specifications & Purity | Moligand™ |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of palmitoyl-protein thioesterase 1 |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | 4-[4-(tert-butylamino)piperidin-1-yl]-N-[(4-chlorophenyl)methyl]quinolin-2-amine |
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INCHI | InChI=1S/C25H31ClN4/c1-25(2,3)29-20-12-14-30(15-13-20)23-16-24(28-22-7-5-4-6-21(22)23)27-17-18-8-10-19(26)11-9-18/h4-11,16,20,29H,12-15,17H2,1-3H3,(H,27,28) |
InChi Key | QVXSJSXAVQJXOV-UHFFFAOYSA-N |
Canonical SMILES | CC(C)(C)NC1CCN(CC1)c1cc(nc2ccccc12)NCc1ccc(cc1)Cl |
Isomeric SMILES | CC(C)(C)NC1CCN(CC1)C2=CC(=NC3=CC=CC=C32)NCC4=CC=C(C=C4)Cl |
PubChem CID | 121305180 |
PubChem CID | 121305180 |
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CAS Registry No. | 1914148-72-3 |
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1. Brun S, Pascussi JM, Gifu EP, Bestion E, Macek-Jilkova Z, Wang G, Bassissi F, Mezouar S, Courcambeck J, Merle P et al.. (2021) GNS561, a New Autophagy Inhibitor Active against Cancer Stem Cells in Hepatocellular Carcinoma and Hepatic Metastasis from Colorectal Cancer.. J Cancer, 12 (18): (5432-5438). [PMID:34405006] [10.1021/op500134e] |
2. Brun S, Bestion E, Raymond E, Bassissi F, Jilkova ZM, Mezouar S, Rachid M, Novello M, Tracz J, Hamaï A et al.. (2022) GNS561, a clinical-stage PPT1 inhibitor, is efficient against hepatocellular carcinoma via modulation of lysosomal functions.. Autophagy, 18 (3): (678-694). [PMID:34740311] [10.1021/op500134e] |
3. Bestion E, Zandi K, Belouzard S, Andreani J, Lepidi H, Novello M, Rouquairol C, Baudoin JP, Rachid M, La Scola B et al.. (2022) GNS561 Exhibits Potent Antiviral Activity against SARS-CoV-2 through Autophagy Inhibition.. Viruses, 14 (1): (1755-70). [PMID:35062337] [10.3390/v14010132] |
4. Brun S, Bassissi F, Serdjebi C, Novello M, Tracz J, Autelitano F, Guillemot M, Fabre P, Courcambeck J, Ansaldi C et al.. (2019) GNS561, a new lysosomotropic small molecule, for the treatment of intrahepatic cholangiocarcinoma.. Invest New Drugs, 37 (6): (1135-1145). [PMID:30778887] [10.1021/op500134e] |
5. Halfon P, Bestion E, Zandi K, Andreani J, Baudoin JP, La Scola B, Mege JL, Mezouar S, Schinazi RF. (2020) GNS561 exhibits potent in vitro antiviral activity against SARS-CoV-2 through autophagy inhibition.. bioRxiv, 71 (13): (1755-70). [PMID:33052342] [10.1021/op500134e] |