XMD 8-92

• Supplier: Tocris Bioscience
• Catalog: 5493
• Prices: $225.00, $925.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 1234480-50-2
• Chemical 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
• Formula: C26H30N6O3
• Molecular Weight: 474.55
• Purity: >98 %
• Description: ERK5 (BMK1) and BRD4 inhibitor (K d values are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (K d values are 190, 600 and 890 nM). Blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity in in vitro kinase assays. Also reduces BMK1-dependent transactivating activity of MEF2C. Inhibits proliferation in a variety of cancer cell lines; blocks tumor cell proliferation and tumor-associated angiogenesis.

Product References

Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic - Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic

Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates JR 3rd, Gray NS, Lee JD. Cancer Cell. 2010 Sep 14;18(3):258-67.

Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and - Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and

Deng X, Yang Q, Kwiatkowski N, Sim T, McDermott U, Settleman JE, Lee JD, Gray NS. ACS Med Chem Lett. 2011 Mar 10;2(3):195-200. Epub 2011 Jan 12.

Targeting the BMK1 MAP kinase pathway in cancer therapy. - Targeting the BMK1 MAP kinase pathway in cancer therapy.

Yang Q, Lee JD. Clin Cancer Res. 2011 Jun 1;17(11):3527-32.

Canonical and kinase activity-independent mechanisms for extracellular - Canonical and kinase activity-independent mechanisms for extracellular

Erazo T, Moreno A, Ruiz-Babot G, Rodriguez-Asiain A, Morrice NA, Espadamala J, Bayascas JR, Gomez N, Lizcano JM. Mol Cell Biol. 2013 Apr;33(8):1671-86.