所有图片(1)
别名:
2-((2-Ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl)amino)-5,11-dimethyl-5Hbenzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one, 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
经验公式（希尔记法）:
C26H30N6O3
推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 25 mg/mL, clear
储存温度
2-8°C
SMILES字符串
OC(CC1)CCN1C2=CC=C(NC3=NC(N(C)C(C=CC=C4)=C4C(N5C)=O)=C5C=N3)C(OCC)=C2
InChI
1S/C26H30N6O3/c1-4-35-23-15-17(32-13-11-18(33)12-14-32)9-10-20(23)28-26-27-16-22-24(29-26)30(2)21-8-6-5-7-19(21)25(34)31(22)3/h5-10,15-16,18,33H,4,11-14H2,1-3H3,(H,27,28,29)
InChI key
QAPAJIZPZGWAND-UHFFFAOYSA-N
应用
XMD8-92 has been used as a specific extracellular signal regulated kinase 5 (ERK5) inhibitor in human umbilical vein endothelial cells (HUVECs) culture.
生化/生理作用
XMD8-92 is a potent and selective inhibitor of BMK1/ERK5/MAPK7 and DCAMKL1 (DCLK1), kinases implicated in tumorigenesis. XMD8-92 has a Kd of 80 nM for ERK5 and a Kd of 97 nM for DCAMKL1. The next closest targets are DCAMKL2 (190 nM), TNK1 (890 nM), and PLK4 (600 nM). Through inhibition of BMK1 activity, XMD8-92 blocked tumor cell proliferation in vitro in a wide variety of cancer cell lines and significantly inhibited tumor growth in vivo by 95% in mouse studies. XMD8-92 inhibited AsPC-1 human pancreatic cancer cell proliferation and pancreatic tumor xenograft growth via a DCLK1-dependent mechanism.
其他说明
XMD8-92 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the XMD8-92 probe summary on the Chemical Probes Portal website.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
João Paulo M Luiz et al.
Journal of leukocyte biology, 108(4), 1215-1223 (2020-08-04)
Macrophages are highly plastic cells, responding to diverse environmental stimuli to acquire different functional phenotypes. Signaling through MAPKs has been reported to regulate the differentiation of macrophages, but the role of ERK5 in IL-4-mediated M2 macrophage differentiation is still unclear.
Joyce K Thompson et al.
Oncotarget, 9(1), 293-305 (2018-02-09)
Malignant mesothelioma is an aggressive cancer in desperate need of treatment. We have previously shown that extracellular signaling regulated kinase 5 (ERK5) plays an important role in mesothelioma pathogenesis using ERK5 silenced human mesothelioma cells exhibiting significantly reduced tumor growth
Maria Elena Bravo-Adame et al.
Immunology, 150(1), 87-99 (2016-09-09)
CD43 is one of the most abundant co-stimulatory molecules on a T-cell surface; it transduces activation signals through its cytoplasmic domain, contributing to modulation of the outcome of T-cell responses. The aim of this study was to uncover new signalling
Xiaohui Wang et al.
Molecular immunology, 101, 245-250 (2018-07-22)
Endothelial dysfunction and vascular complications induced by hyperglycemia play an important role in the pathological development of atherosclerosis in diabetes. Humanin, a 24-amino acid mitochondria-derived polypeptide, has displayed its cytoprotective effects in diverse cell types and tissues. In the current
Zhiqi Liu et al.
International journal of oncology, 50(4), 1321-1329 (2017-03-06)
Overexposure to benzidine has been manifested as an important cause of bladder cancer. However, the molecular mechanism of benzidine-induced malignancy is still insufficiently interpreted. Epithelial-mesenchymal transition (EMT) is a crucial pathophysiological process in embryonic development as well as initiation and
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