product summary
Loading...
company name :
Tocris Bioscience
product type :
chemical
product name :
XMD 8-92
catalog :
4132
quantity :
10 mg (also 50 mg)
price :
264 USD
more info or order :
citations: 4
Reference
Thompson J, Shukla A, Leggett A, Munson P, Miller J, Macpherson M, et al. Extracellular signal regulated kinase 5 and inflammasome in progression of mesothelioma. Oncotarget. 2018;9:293-305 pubmed publisher
Pereira D, Simões A, Gomes S, Castro R, Carvalho T, Rodrigues C, et al. MEK5/ERK5 signaling inhibition increases colon cancer cell sensitivity to 5-fluorouracil through a p53-dependent mechanism. Oncotarget. 2016;7:34322-40 pubmed publisher
Simões A, Pereira D, Gomes S, Brito H, Carvalho T, French A, et al. Aberrant MEK5/ERK5 signalling contributes to human colon cancer progression via NF-κB activation. Cell Death Dis. 2015;6:e1718 pubmed publisher
Al Ejeh F, Miranda M, Shi W, Simpson P, Song S, Vargas A, et al. Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. Oncotarget. 2014;5:3145-58 pubmed
product information
brand :
Tocris
master code :
4132
SKU :
4132/10
product name :
XMD 8-92
description :
ERK5/BMK1 inhibitor; also BRD4 inhibitor
target :
ERK Inhibitors
category :
Small Molecules
unit size :
10 mg (also 50 mg)
purity :
98%
observed molecular weight :
474.55
url print :
?utm_source=distributor&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
ERK5 (BMK1) and BRD4 inhibitor (Kd values are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (Kd 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.
catalog number base :
4132
product keywords :
erk5 bmk1 big MAP kinase 1 inhibitors inhibits antitumor antiproliferative antiproliferation XMD8-92 bromodomains BRD4 ERK Bromodomains 4132,
extended description :
ERK5/BMK1 inhibitor; also BRD4 inhibitor
chemical name text :
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 :
C 26 H 30 N 6 O 3
formula text :
C26H30N6O3
cas num :
1234480-50-2
2020 USD :
253
2021 USD :
264 USD
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK