CAS 1234480-50-2; xmd8-92

CAS:

1234480-50-2

分子式:

C₂₆H₃₀N₆O₃

分子量:

474.55

英文名称:

xmd8-92

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

用途:

XMD8-92 是强效的选择性的BMK1/ERK5抑制剂，其Kd为80 nM。XMD8-92，通过抑制BMK1活化，显著诱导细胞中p21表达，并介导对癌细胞增殖的抑制作用。[1] XMD8-92显著废除羟基红花黄色素A(HSYA)对肝星状细胞(HSC)活化的抑制作用，并阻断HSYA介导的MEF2C下调。[2]

推荐供应商

货号

品牌

产品名称

规格

包装、参考价格

X872633

MACKLIN

XMD8-92

99%

79元/1mg; 215元/5mg; 305元/10mg; 980元/50mg;

咨询

储存：-20℃
状态：白色到米黄色粉末

X795884

MACKLIN

XMD8-92

10mM in DMSO

648元/1ml;

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储存：-20°C

SML1382

Sigma-Aldrich

XMD8-92

≥98% (HPLC)

2102.31元/5 MG; 6765.81元/25 MG;

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产品说明

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.

包装

5, 25 mg in glass bottle

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.

基本信息

经验(实验)分子式	C₂₆H₃₀N₆O₃
分子量	474.55
MDL编号	MFCD18782742
PubChem化学物质编号	329825830

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 25 mg/mL, clear
储存温度	2-8℃
SMILES string	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

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable