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AZ 191 - 98%, high purity , CAS No.1594092-37-1, Inhibitor of dual specificity tyrosine phosphorylation regulated kinase 1B

  • Moligand™
  • ≥98%
Item Number
A288802
Grouped product items
SKUSizeAvailabilityPrice Qty
A288802-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$49.90
A288802-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$79.90
A288802-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$159.90
A288802-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$256.90
A288802-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$409.90

Potent DYRK1B inhibitor

Basic Description

SynonymsN-[2-Methoxy-4-(4-methyl-1-piperazinyl)phenyl]-4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-pyrimidinamine
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPotent DYRK1B inhibitor (IC50values are 17, 88 and 1890 nM for DYRK1B, DYRK1A and DYRK2 respectively). Inhibits DYRK1B-induced Giphase cell cycle arrest in Panc-1 cellsin vitro.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of dual specificity tyrosine phosphorylation regulated kinase 1B

Associated Targets

DYRK1B Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1B 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK2 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK3 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK4 Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK1A Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK5R1 Tchem Cyclin-dependent kinase 5 activator 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1E Tclin Casein kinase I isoform epsilon 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK1 Tchem Dual specificity protein kinase CLK1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK2 Tchem Dual specificity protein kinase CLK2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CLK4 Tchem Dual specificity protein kinase CLK4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1-methylpyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
INCHI InChI=1S/C24H27N7O/c1-29-10-12-31(13-11-29)17-4-5-21(23(14-17)32-3)28-24-26-9-7-20(27-24)19-16-30(2)22-15-25-8-6-18(19)22/h4-9,14-16H,10-13H2,1-3H3,(H,26,27,28)
InChi Key ZYVXTMKTGDARKR-UHFFFAOYSA-N
Canonical SMILES CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=CC(=N3)C4=CN(C5=C4C=CN=C5)C)OC
Isomeric SMILES CN1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=CC(=N3)C4=CN(C5=C4C=CN=C5)C)OC
PubChem CID 72716071
Molecular Weight 429.52

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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9 results found

Lot NumberCertificate TypeDateItem
A2404097Certificate of AnalysisDec 18, 2023 A288802
A2404098Certificate of AnalysisDec 18, 2023 A288802
A2404099Certificate of AnalysisDec 18, 2023 A288802
A2404100Certificate of AnalysisDec 18, 2023 A288802
A2404101Certificate of AnalysisDec 18, 2023 A288802
A2404431Certificate of AnalysisDec 18, 2023 A288802
A2404432Certificate of AnalysisDec 18, 2023 A288802
A2404433Certificate of AnalysisDec 18, 2023 A288802
A2404435Certificate of AnalysisDec 18, 2023 A288802

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 42.95, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 8.59, Max Conc. mM: 20

Related Documents

References

1. Ashford AL, Oxley D, Kettle J, Hudson K, Guichard S, Cook SJ, Lochhead PA.  (2014)  A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288)..  Biochem J,  457  (1): (43-56).  [PMID:24134204]
2. Kettle JG, Ballard P, Bardelle C, Cockerill M, Colclough N, Critchlow SE, Debreczeni J, Fairley G, Fillery S, Graham MA et al..  (2015)  Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis..  J Med Chem,  58  (6): (2834-44).  [PMID:25738750]

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