XMD8-92

XMD8-92 is a potent ERK5 (BMK1) /BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity[1][2].

Product Specifications

CAS Number

[1234480-50-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

CaMK; Epigenetic Reader Domain; ERK; TNK1

Type

Reference compound

Related Pathways

Epigenetics; MAPK/ERK Pathway; Neuronal Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/xmd8-92.html

Purity

99.48

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CN(C1=O)C2=CN=C(N=C2N(C3=C1C=CC=C3)C)NC4=C(C=C(C=C4)N5CCC(CC5)O)OCC

Molecular Formula

C26H30N6O3

Molecular Weight

474.55

Precautions

H302, H315, H319, H335

References & Citations

[1]Yang Q, et al. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.Cancer Cell. 2010 Sep 14;18 (3) :258-67.|[2]Yang Q, et al. Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin Cancer Res. 2011 Jun 1;17 (11) :3527-32.|[3]Umapathy G, et al. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal. 2014 Oct 28;7 (349) :ra102.|[4]Lin EC, et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A. 2016;113 (42) :11865-11870.