SML1382
XMD8-92
≥98% (HPLC)
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
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所有图片(1)
About This Item
经验公式（希尔记法）:
C26H30N6O3
CAS号:
分子量:
474.55
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
推荐产品
质量水平
方案
≥98% (HPLC)
表单
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 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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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
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.
Qiang Li et al.
Journal of clinical neuroscience : official journal of the Neurosurgical Society of Australasia, 34, 264-270 (2016-10-16)
Angiographic vasospasm, especially in the early phases (<72h) of subarachnoid hemorrhage (SAH), is one of the major complications after an aneurysm rupture and is often the cause of delayed neurological deterioration. Scutellarin (SCU), a flavonoid extracted from the traditional Chinese
Junko Wakao et al.
Biochemical and biophysical research communications, 488(2), 368-373 (2017-05-16)
The skeletal muscle consists of contractile myofibers and plays essential roles for maintenance of body posture, movement, and metabolic regulation. During the development and regeneration of the skeletal muscle tissue, the myoblasts fuse into multinucleated myotubes that subsequently form myofibers.
Hui Wang et al.
International journal of oncology, 51(1), 91-103 (2017-06-01)
Malignant pleural mesothelioma (MPM) is an aggressive cancer for which more effective treatments are needed. In this study, strong to moderate staining of MET and ERK5 was detected in 67.1 and 48% of the analyzed 73 human mesothelioma tumors, and significant
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