AX 15836 - ≥98%(HPLC), high purity , CAS No.2035509-96-5, Inhibitor of mitogen-activated protein kinase 7

Item Number
A287667
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SKUSizeAvailabilityPrice Qty
A287667-2mg
2mg
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$129.90
A287667-5mg
5mg
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$224.90
A287667-10mg
10mg
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$331.90
A287667-25mg
25mg
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$688.90
A287667-50mg
50mg
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$1,163.90
A287667-100mg
100mg
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$2,095.90

Potent and selective ERK5 inhibitor

Basic Description

Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent 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 TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of mitogen-activated protein kinase 7

Associated Targets(Human)

MAPK7 Tchem Mitogen-activated protein kinase 7 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAPK7 Tchem Mitogen-activated protein kinase 7 (929 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

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
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

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolvent:1eq. HCl, Max Conc. mg/mL: 64.88, Max Conc. mM: 100; Solvent:DMSO, Max Conc. mg/mL: 64.88, Max Conc. mM: 100

Related Documents

References

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]

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