Ralimetinib (LY2228820) dimesylate

For research use only. Not for use in humans.

目录号:S1494

Ralimetinib (LY2228820) dimesylate Chemical Structure

CAS No. 862507-23-1

Ralimetinib (LY2228820) dimesylate 是一种新型有效的p38 MAPK抑制剂,无细胞试验中IC50为7 nM,不改变p38 MAPK的活化。Phase 1/2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2344.86 现货
RMB 1403.05 现货
RMB 7927.27 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Ralimetinib (LY2228820) dimesylate发表文献55篇:

产品安全说明书

p38 MAPK抑制剂选择性比较

生物活性

产品描述 Ralimetinib (LY2228820) dimesylate 是一种新型有效的p38 MAPK抑制剂,无细胞试验中IC50为7 nM,不改变p38 MAPK的活化。Phase 1/2。
特性 LY2228820是新型有效的p38有丝分裂原活化蛋白激酶(MAPK)通路抑制剂。
靶点
p38α [1]
(Cell-free assay)
7 nM
体外研究

LY2228820作用于RAW 264.7细胞,抑制p38α,和磷酸MAPKAPK-2(pMK2)水平,IC50分别为7 nM 和 34.3 nM。而且, LY2228820作用于小鼠腹腔巨噬细胞,抑制脂多糖 (LPS)-诱导的TNFα形成, IC50为5.2 nM。[1] 200 nM-800 nM LY2228820作用于多发性骨髓瘤(MM)细胞, 包括INA6, RPMI-8226, U266, 和RPMI-Dox40,通过抑制HSP27磷酸化而显著抑制p38MAPK信号, HSP27是p38MAPK下游靶点,不影响 HSP27表达水平。200 nM-400 nM LY2228820增强Bortezomib诱导的细胞毒性和凋亡, 但是LY2228820 单独处理不会抑制MM.1S细胞生长。200 nM-800 nM LY2228820作用于长期骨髓基质干细胞(LT-BMSCs),骨髓单个核细胞(BMMNCs),外周血(PB)CD138+,CD138-或外周血(PB)CD14+细胞,也抑制IL-6和MIP-1α分泌。400 nM-800 nM LY2228820也抑制CD14+ 细胞形成破骨细胞。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI-8226 NYmzVWpiU2mwYYPlJIF{e2G7 MVL+PFAxKG6P NWrLbI9wTE2VTx?= M16zSIlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= M2fKPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
U266 NE\sRoNMcW6jc3WgZZN{[Xl? NUWxV2Z[hjhyMDDuUS=> MU\EUXNQ NIPyR29qdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NWmyTGtmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
MM.1S NXq2cZB1U2mwYYPlJIF{e2G7 Mn31glgxOCCwTR?= M33ze2ROW09? NEjRVVZqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NWribFRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
RPMI-Dox40 NGHU[lhMcW6jc3WgZZN{[Xl? NHq1S3Z,QDByIH7N MYrEUXNQ MXrpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? M1XHVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
RPMI-LR5 M1LqUGtqdmG|ZTDhd5NigQ>? NXiyWXM{hjhyMDDuUS=> NH\QNFFFVVOR M3LHfYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= MkP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
INA-6 NEjIcI5McW6jc3WgZZN{[Xl? MlvoglgxOCCwTR?= M4KwU2ROW09? M2DCVolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
RPMI-8226 M{\acGN6fG:6aXPpeJkh[XO|YYm= MoXSglExODBibl2= NFeyVmNFVVOR NVXDVVRmdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 M2X0dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
U266 M{HpUWN6fG:6aXPpeJkh[XO|YYm= NHzYW49,OTByMDDuUS=> NEHuWYhFVVOR M32xb45wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NY\ZdG9PRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
MM.1S NV62dW1RS3m2b4jpZ4l1gSCjc4PhfS=> MXL+NVAxOCCwTR?= NH7sVndFVVOR MU\uc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NHTlTIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
RPMI-Dox40 Mk\qR5l1d3irY3n0fUBie3OjeR?= NGPs[HR,OTByMDDuUS=> NXrsbHpJTE2VTx?= Ml;Dco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 M1PHSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
RPMI-LR5 MkHHR5l1d3irY3n0fUBie3OjeR?= MkSzglExODBibl2= NXrLTYdTTE2VTx?= MXTuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
INA-6 MoHmR5l1d3irY3n0fUBie3OjeR?= NWLoPXpQhjFyMECgcm0> M4G4fmROW09? MWHuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M{jlZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
CD14+ NE[4dlVHfW6ldHnvckBie3OjeR?= M1;Jdp45ODBibl2= NFPK[|lFVVOR NGjSU29qdmirYnn0d{Bwe3Snb3PsZZN1d2enbnXzbZMh\nKxbTDDSFE1KHCxc3n0bZZmKGOnbHzz MonNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
U-87-MG NIfiNJFHfW6ldHnvckBie3OjeR?= NFfLR28yKM7:TR?= M1Hve2ROW09? MYTy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NF;0WpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OzOVUxPid-MkOzN|U2ODZ:L3G+
MDA-MB-231 MU\GeY5kfGmxbjDhd5NigQ>? NIDKOI4yKM7:TR?= M3ywW2ROW09? NXLJR5RiemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> M4rSclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{O1OVA3Lz5{M{OzOVUxPjxxYU6=
A-2780 M2jWZmZ2dmO2aX;uJIF{e2G7 MUWxJO69VQ>? MVjEUXNQ NV75eoV7emWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> M2HrWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{O1OVA3Lz5{M{OzOVUxPjxxYU6=
SK-OV-3 M33q[mZ2dmO2aX;uJIF{e2G7 M2fCc|Eh|ryP NHzIUnpFVVOR NUCz[YdPemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NXHQSWUxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzN|U2ODZpPkKzN|M2PTB4PD;hQi=>
LXFA-629 M3f5TGZ2dmO2aX;uJIF{e2G7 M1f6XVEh|ryP MVfEUXNQ MnvpdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
NCI-H1650 NEPH[3hHfW6ldHnvckBie3OjeR?= MVOxJO69VQ>? NITTRplFVVOR NEjD[|Vz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> M1\O[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{O1OVA3Lz5{M{OzOVUxPjxxYU6=
PC-3 MofTSpVv[3Srb36gZZN{[Xl? M{HKU|Eh|ryP M4HLUGROW09? M{TsVZJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u M4O0VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{O1OVA3Lz5{M{OzOVUxPjxxYU6=
RAW264.7 MWHGeY5kfGmxbjDhd5NigQ>? NHnlcGd,OjBizszN MYTEUXNQ MYDpcohq[mm2czDBcol{d227Y3nuMZN1cW23bHH0[YQhVUt{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gN|UvOyCwTR?= NVjXZVZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVY5OTRpPkK0N|U3QDF2PD;hQi=>
mouse peritoneal macrophages M3PkNWZ2dmO2aX;uJIF{e2G7 NF7jXJd,OjBizszN NF7Y[2NFVVOR NX;vcYcyVFCVL1nGUk3Pu+LCk4P0bY12dGG2ZXSgWG5HNc7zIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDZwMzDuUS=> NUPEe5BWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOVY5OTRpPkK0N|U3QDF2PD;hQi=>
A549 NGDBVGpHfW6ldHnvckBie3OjeR?= MkfwglIxKM7:TR?= MlLxSG1UVw>? M2\BPYlvcGmkaYTzJGxRWy2rbnT1Z4VlKEO[Q1y4JJBzd2S3Y4Tpc44hf2m2aDDJR|UxKG:oIEG0OE46KG6P NGXqVnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1OlgyPCd-MkSzOVY5OTR:L3G+
MDA-231 MoHWSpVv[3Srb36gZZN{[Xl? M4LOfZ4yOCEQvF2= MXjzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= NWq5cpZHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0NFc5PDNpPkK2OFA4QDR|PD;hQi=>
MCF-7 NG\1WHFHfW6ldHnvckBie3OjeR?= Mkf4glExKM7:TR?= MXHzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= NHntZmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkSwO|g1Oyd-Mk[0NFc5PDN:L3G+
MDA-435 NWXrSIQ6TnWwY4Tpc44h[XO|YYm= MoTpglExKM7:TR?= M1LQV5N2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NFHzdno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkSwO|g1Oyd-Mk[0NFc5PDN:L3G+
PC3 M3yz[GZ2dmO2aX;uJIF{e2G7 NEjYW2x,OTBizszN MVPEUXNQ M4nsOpN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NH\mUFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkmxN|YxQCd-Mk[5NVM3ODh:L3G+
TC32 M1OwbZFJXFNiYYPzZZk> NFf3fW5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVFOzNkBk\Wyucx?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 NGDqPIVyUFSVIHHzd4F6 NEnSZVByUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY MoLSdWhVWyCjc4PhfS=> NYnzPI52eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO= M2e3SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 MnrzdWhVWyCjc4PhfS=> Mn32dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD NVnsXnFpeUiWUzDhd5NigQ>? MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> NVPlNJZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 M2fPdpFJXFNiYYPzZZk> MlfrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| M2SxPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 MlLEdWhVWyCjc4PhfS=> NUK1OWxMeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> M1PobVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 NH7OW5VyUFSVIHHzd4F6 NV3tSJFpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 MlTidWhVWyCjc4PhfS=> NEjNZppyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= MnTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh30 NE[4Z5pyUFSVIHHzd4F6 MmrEdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqM{CgZ4VtdHN? M13o[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-p38 / p38α / p38β / p-MK2 / MK2 / p-HSP27 / HSP27; 

PubMed: 23335506     


whole cell protein extracts were isolated from ECFCs or ADSCs following pretreatment with DMSO (−) or 1 μm LY2228820 dimesylate (+) for 30 min prior to the addition of 10 ng/ml VEGF, bFGF, EGF, or 100 ng/ml IL-6, and then the extracts were subjected to Western blot analysis using antisera directed against p-p38, p38α, p38β, p-MK2, total MK2, p-HSP27, total HSP27, and β-actin as a loading control.

p-S6K ; 

PubMed: 26844273     


CRC cells were treated with 4 μM LY2228820, 10 μM BIRB796 or 10 μM SB202190 for 2 h and p38 and mTORC1 signaling was analyzed by immunoblot.

23335506 26844273
体内研究 LY2228820 作用于LPS诱导的小鼠,有效抑制TNFα 形成,半数有效剂量最小阈值 (TMED 50)小于1 mg/kg。LY2228820 作用于患胶原性关节炎(CIA)大鼠模型,有效作用于足肿胀, 骨质糜烂, 和软骨破坏, 半数有效剂量最小阈值(TMED50)为 1.5 mg/kg。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

抑制p38α实验:

使用重组人p38α 在标准过滤器中使用ATP[γ-33P] 和EGFR 21肽底物测定抑制p38α的效果。在LY2228820存在时,使用LPS刺激,在小鼠腹腔巨噬细胞测定抑制TNFα效果。在使用LY2228820处理,然后用Anisomycin刺激的RAW 264.7细胞中测定p38α活性。使用磷酸MAPKAPK-2(pMK2)(Thr 334)抗体测定p38α活性水平。
细胞实验: [2]
- 合并
  • Cell lines: MM细胞,包括 INA6, RPMI-8226, U266,和RPMI-Dox40
  • Concentrations: 200 nM-800 nM
  • Incubation Time: 48小时
  • Method: 进行MTT实验和APO 2.7 染色分别测定细胞增殖和凋亡诱导。测定活细胞百分数作为可活力。通过APO 2.7染色测定凋亡。为了测定凋亡细胞中线粒体膜蛋白7A6的表达,用APO 2.7试剂处理细胞20分钟。使用EPICS XL流式细胞仪测定APO 2.7的表达。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 脂多糖(LPS)-诱导的Balb/c小鼠
  • Dosages: 0-20 mg/kg
  • Administration: 口服处理,每天两次,持续14天
    (Only for Reference)

溶解度 (25°C)

体外 Water 100 mg/mL warmed (163.2 mM)
DMSO 4 mg/mL warmed (6.52 mM)
Ethanol '3 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
Saline
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 612.74
化学式

C24H29FN6.2CH4O3S

CAS号 862507-23-1
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

p38 MAPK Signaling Pathway Map

p38 MAPK Inhibitors with Unique Features

相关p38 MAPK产品

Tags: 购买Ralimetinib (LY2228820) dimesylate | Ralimetinib (LY2228820) dimesylate供应商 | 采购Ralimetinib (LY2228820) dimesylate | Ralimetinib (LY2228820) dimesylate价格 | Ralimetinib (LY2228820) dimesylate生产 | 订购Ralimetinib (LY2228820) dimesylate | Ralimetinib (LY2228820) dimesylate代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID