XMD8-92

• Description:

  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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  BRD4; DCAMKL; ERK5

• CAS Number:

  [1234480-50-2]