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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A287667-2mg | 2mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $129.90 | |
A287667-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $224.90 | |
A287667-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $331.90 | |
A287667-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $688.90 | |
A287667-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,163.90 | |
A287667-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,095.90 |
Potent and selective ERK5 inhibitor
Specifications & Purity | Moligand™, ≥98%(HPLC) |
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Biochemical and Physiological Mechanisms | Potent and selective ERK5 inhibitor (IC50= 8 nM). Exhibits >1,000-fold selectivity for ERK5 over a panel of over 200 kinases. Also exhibits selectivity over bromodomain BRD4 (Kd= 3,600 nM). Increases vomocytosis in human macrophagesin vitro, as well as i |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of mitogen-activated protein kinase 7 |
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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 | 2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methyl-11-methylsulfonylpyrimido[4,5-b][1,4]benzodiazepin-6-one |
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INCHI | InChI=1S/C32H40N8O5S/c1-5-45-28-20-22(30(41)39-14-12-23(13-15-39)38-18-16-36(2)17-19-38)10-11-25(28)34-32-33-21-27-29(35-32)40(46(4,43)44)26-9-7-6-8-24(26)31(42)37(27)3/h6-11,20-21,23H,5,12-19H2,1-4H3,(H,33,34,35) |
InChi Key | HTFNVAVTYILUCF-UHFFFAOYSA-N |
Canonical SMILES | CCOC1=C(C=CC(=C1)C(=O)N2CCC(CC2)N3CCN(CC3)C)NC4=NC=C5C(=N4)N(C6=CC=CC=C6C(=O)N5C)S(=O)(=O)C |
Isomeric SMILES | CCOC1=C(C=CC(=C1)C(=O)N2CCC(CC2)N3CCN(CC3)C)NC4=NC=C5C(=N4)N(C6=CC=CC=C6C(=O)N5C)S(=O)(=O)C |
PubChem CID | 122705989 |
Molecular Weight | 648.78 |
PubChem CID | 122705989 |
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ChEMBL Ligand | CHEMBL4541479 |
BindingDB Ligand | 50508013 |
CAS Registry No. | 2035509-96-5 |
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Solubility | Solvent:1eq. HCl, Max Conc. mg/mL: 64.88, Max Conc. mM: 100; Solvent:DMSO, Max Conc. mg/mL: 64.88, Max Conc. mM: 100 |
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1. Lin EC, Amantea CM, Nomanbhoy TK, Weissig H, Ishiyama J, Hu Y, Sidique S, Li B, Kozarich JW, Rosenblum JS. (2016) ERK5 kinase activity is dispensable for cellular immune response and proliferation.. Proc Natl Acad Sci U S A, 113 (42): (11865-11870). [PMID:27679845] |
2. Cook SJ, Tucker JA, Lochhead PA. (2020) Small molecule ERK5 kinase inhibitors paradoxically activate ERK5 signalling: be careful what you wish for….. Biochem Soc Trans, 48 (5): (1859-1875). [PMID:32915196] |