A selective ERK5 inhibitor (Kd = 80 nM); less potently inhibits DCAMKL2

XMD8-92 – 10 mg

Brand:
Cayman
CAS:
1234480-50-2
Storage:
-20
UN-No:
Non-Hazardous - /

XMD8-92 is an ERK5 inhibitor (Kd = 80 nM) that less potently inhibits DCAMKL2, TNK1, and Plk4 (Kds = 190, 890, and 600 nM, respectively) in a panel of 402 kinases.{31129} It blocks ERK5 autophosphorylation, ERK5-mediated phosphorylation of promyelocytic leukemia protein (PML), and PML-dependent activation of p21.{31129} XMD8-92 inhibits AP-1 transcriptional activity induced by MEK5-activated ERK5 but not that induced by Cdc37.{31128} It inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice and reduces tumor growth in a HeLa mouse xenograft model when administered at a dose of 50 mg/kg twice per day.{31129} XMD8-92 also binds bromodomain-containing protein 4 (BRD4; Kd = 170 nM for BRD4 bromodomain 1).{42864}  

 

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Description

A selective ERK5 inhibitor (Kd = 80 nM); less potently inhibits DCAMKL2, TNK1, and Plk4 (Kds = 190, 890, and 600 nM, respectively); blocks ERK5 autophosphorylation, ERK5-mediated phosphorylation of PML, and PML-dependent activation of p21; inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice; reduces tumor growth in a HeLa mouse xenograft model at 50 mg/kg twice per day; binds BRD4 (Kd = 170 nM for BRD4 bromodomain 1)

Formal name: 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

Synonyms: 

Molecular weight: 474.6

CAS: 1234480-50-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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