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XMD8-92 - ≥97%, high purity , CAS No.1234480-50-2, Inhibitor of doublecortin like kinase 2;Inhibitor of mitogen-activated protein kinase 7;Inhibitor of polo like kinase 4;Inhibitor of tyrosine kinase non receptor 1

  • Moligand™
  • ≥97%
Item Number
X125609
Grouped product items
SKUSizeAvailabilityPrice Qty
X125609-1mg
1mg
In stock
$14.90
X125609-5mg
5mg
In stock
$60.90
X125609-10mg
10mg
In stock
$85.90
X125609-50mg
50mg
In stock
$296.90
X125609-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$494.90

ERK5/BMK1 inhibitor; also BRD4 inhibitor

Basic Description

SynonymsXMD8-92|1234480-50-2|XMD 8-92|2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-B][1,4]benzodiazepin-6-one|2-{[2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl]amino}-5,11-dimethyl-5,11-dihydro-6H-pyrimido[4,5-b][1
Specifications & PurityMoligand™, ≥97%
Biochemical and Physiological MechanismsERK5 (BMK1) and BRD4 inhibitor (Kdvalues are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (Kdvalues are 190, 600 and 890 nM). Blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity inin vitrokinase assays.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of doublecortin like kinase 2;Inhibitor of mitogen-activated protein kinase 7;Inhibitor of polo like kinase 4;Inhibitor of tyrosine kinase non receptor 1
Product Description

XMD8-92 has been used as a specific extracellular signal regulated kinase 5 (ERK5) inhibitor in human umbilical vein endothelial cells (HUVECs) culture.

Associated Targets

DCLK2 Tchem Serine/threonine-protein kinase DCLK2 1 Activities

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

PTK2 Tclin Focal adhesion kinase 1 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)

DCLK1 Tchem Serine/threonine-protein kinase DCLK1 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)

TNK1 Tchem Non-receptor tyrosine-protein kinase TNK1 1 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)

PLK4 Tchem Serine/threonine-protein kinase PLK4 1 Activities

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

PLK1 Tchem Serine/threonine-protein kinase PLK1 0 Activities

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

PI4KA Tchem Phosphatidylinositol 4-kinase alpha 0 Activities

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

RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 0 Activities

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

MAPK7 Tchem Mitogen-activated protein kinase 7 1 Activities

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

MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 0 Activities

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

LRRK2 Tchem Leucine-rich repeat serine/threonine-protein kinase 2 0 Activities

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

BRDT Tchem Bromodomain testis-specific protein 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)

TNK2 Tclin Activated CDC42 kinase 1 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)

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)

MAPK3 Tchem Mitogen-activated protein kinase 3 0 Activities

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

RPS6KA3 Tchem Ribosomal protein S6 kinase alpha-3 0 Activities

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

MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 0 Activities

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

Names and Identifiers

IUPAC Name 2-[2-ethoxy-4-(4-hydroxypiperidin-1-yl)anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one
INCHI InChI=1S/C26H30N6O3/c1-4-35-23-15-17(32-13-11-18(33)12-14-32)9-10-20(23)28-26-27-16-22-24(29-26)30(2)21-8-6-5-7-19(21)25(34)31(22)3/h5-10,15-16,18,33H,4,11-14H2,1-3H3,(H,27,28,29)
InChi Key QAPAJIZPZGWAND-UHFFFAOYSA-N
Canonical SMILES CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(C5=CC=CC=C5C(=O)N4C)C
Isomeric SMILES CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(C5=CC=CC=C5C(=O)N4C)C
PubChem CID 46843772
Molecular Weight 474.57

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Certificate of Analysis(COA)

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5 results found

Lot NumberCertificate TypeDateItem
K2108433Certificate of AnalysisAug 14, 2023 X125609
K2108434Certificate of AnalysisAug 14, 2023 X125609
K2108436Certificate of AnalysisAug 14, 2023 X125609
K2108442Certificate of AnalysisAug 14, 2023 X125609
K2108798Certificate of AnalysisAug 14, 2023 X125609

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 18.98, Max Conc. mM: 40

Related Documents

References

1. Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates 3rd JR, Gray NS, Lee JD.  (2010)  Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein..  Cancer Cell,  18  (3): (258-67).  [PMID:20832753]

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