Adezmapimod (SB203580)

Catalog No.S1076 Synonyms: RWJ 64809, PB 203580

For research use only.

Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

Adezmapimod (SB203580) Chemical Structure

CAS No. 152121-47-6

Selleck's Adezmapimod (SB203580) has been cited by 740 publications

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Other p38 MAPK Products

Biological Activity

Description Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.
Features First reported p38 inhibitor.
Targets
p38 MAPK [1]
(THP-1 cells)
PKB [1]
(THP-1 cells)
0.3 μM-0.5 μM 3 μM-5 μM
In vitro

SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. [1] SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. [2] SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC12 M2PXfmtqdmG|ZTDBd5NigQ>? MYmxNEDPxE1? MnLONVUhdWmw MmTMTY5pcWKrdIOgdFM5KE2DUDDrbY5ie2Vid3n0bEBKSzVyIH;mJFAvPiEQvF2= NX;4OXI4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxN{e1NFU4Pyd-N{e1NFU4PzxxYU6=
THP-1 MYTGeY5kfGmxbjDBd5NigQ>? MkPETY5pcWKrdIOgUHBUNWmwZIXj[YQhXE6IYXzwbIEheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNE4yPiEQvF2= NHnXbWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEOyOVc3QCd-MUizNlU4Pjh:L3G+
PBMC MWHGeY5kfGmxbjDBd5NigQ>? MUCxOUBucW5? NVjJSJVDTE2VTx?= NHrDO5JKdmirYnn0d{B1cGVicnXs[YF{\SCxZjDpcpRmemyndXvpck0yNWKndHGge4l1cCCLQ{WwJI9nKDBwMEO3JO69VQ>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjN4MUO5Okc,OTJ|NkGzPVY9N2F-
SW1353 MmP6SpVv[3Srb36gRZN{[Xl? NWPmWFBYOSCq MYjEUXNQ NETKdZJKdmirYnn0d{BKVC14IIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDBwMEWg{txO NH32c|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUG0NFc1OSd-MUGxOFA4PDF:L3G+
Hela MVLGeY5kfGmxbjDBd5NigQ>? MV3EUXNQ MUXJcohq[mm2czDUZZQucW6mdXPl[EBJUVZzIFzUVkB1emGwc3HjeIl3[XSrb36gbY4hcHWvYX6gTIVN[SClZXzsd{B4cXSqIFnDOVAhd2ZiMD6xJO69VQ>? NHXad2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEmyOlcyOSd-MUi5NlY4OTF:L3G+
PC12 NVj0W5NNTnWwY4Tpc44hSXO|YYm= NWTIcHkyOTBizszN MnO0SG1UVw>? MXfBZ5RqfmG2ZYOgUpJnOi:DUlWgbY4hemG2IGDDNVIh[2WubIOgZZN{\XO|ZXSgZZMhUE9vMTDwdo91\WmwIHnu[JVkfGmxbh?= M3vGbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{S1Olg2Lz5{MUO0OVY5PTxxYU6=
RAW 264.7 MXnDfZRwfG:6aXOgRZN{[Xl? M2X6c|EzNjVizszN MkfINVJp NEnJW2ZFVVOR Ml\xRoxw[2u|IHzleIhidCC2b4jpck1u\WSrYYTl[EBkgXSxdH;4bYNqfHl? MoH1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2OEW1NFQoRjF5NEi1OVA1RC:jPh?=
HCA2 NFfxdotHfW6ldHnvckBCe3OjeR?= NILyRnczNjVizszN Mo\QTY5pcWKrdIOgdFM5KG2nZHnheIVlKE2NMjDhZ5RqfmG2aX;u MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzl4NEe4NEc,OTd7NkS3PFA9N2F-
U937 NX;ueGNzTnWwY4Tpc44hSXO|YYm= MoPVTY5pcWKrdIOgTmFMNW2nZHnheIVlKGmwdHXy[oVzd25vZ3HtcYEw[W6rc3;tfYNqdi2rbnT1Z4VlKFO2YYSxJJBpd3OyaH;yfYxifGmxbh?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDF3N{GyNkc,OThzNUexNlI9N2F-
U937 MXnGeY5kfGmxbjDBd5NigQ>? NYfRV2QyUW6qaXLpeJMhUkGNLX3l[IlifGWmIHnueIVz\mW{b36t[4FudWFxYX7pd49ugWOrbj3pcoR2[2WmIICzPEBxcG:|cHjvdplt[XSrb36= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDF3N{GyNkc,OThzNUexNlI9N2F-
hESCs M2\OV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3z3VVUh|ryP NFyxWpNFVVOR MXfJcoR2[2W|IHPhdoRqd227b3flcolkKGGldHn2bZR6KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4To NF\oOnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[wNlM6QSd-MkO2NFI{QTl:L3G+
RAW264.7 MYLGeY5kfGmxbjDBd5NigQ>? NIPMW3EyOCEQvF2= NVn5NYNSUW6mdXPld{BidnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIJ6KGmwaHnibZRqdmdiSVytNe6zKHKnbHXhd4U> NHzlWWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NVA4QCd-MkO3PVExPzh:L3G+
RAW264.7 MmrpSpVv[3Srb36gRZN{[Xl? M3;xclExKM7:TR?= NUfUTppRUW6mdXPld{BidnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIJ6KGmwaHnibZRqdmdiaV7PV{Bz\WynYYPl MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MUC3PEc,OjN5OUGwO|g9N2F-
RAW264.7 NFPMcZlHfW6ldHnvckBCe3OjeR?= MVmxNEDPxE1? NVfyXHNtUW6mdXPld{BidnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIJ6KGmwaHnibZRqdmdiTl:gdoVt\WG|ZR?= MlLkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUGwO|goRjJ|N{mxNFc5RC:jPh?=
RAW264.7 NHXS[4dHfW6ldHnvckBCe3OjeR?= NYPxcnU1OTBizszN M3zRdWlvcGmkaYTzJGxRWy2rbnT1Z4VlKHB|ODDNRXBMKHCqb4PwbI9zgWyjdHnvci=> NV;2R|NpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVYxPTdpPkK0NFE3ODV5PD;hQi=>
IEC-18 Ml;ESpVv[3Srb36gRZN{[Xl? MXOxNEDPxE1? NUXtcIsyUW6qaXLpeJMhVFCVLXnu[JVk\WRicEO4JG1CWEticHjvd5Bpd3K7bHH0bY9v NYDVT4sxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3OVgyOTBpPkKzO|U5OTFyPD;hQi=>
Sf9 MmrRSpVv[3Srb36gZZN{[Xl? M2LPS|MxKG2rboO= M1nUbGlvcGmkaYTpc44hd2ZiZoXscE1t\W6pdHigSmxCTy14SHnzMXRGXiC2YXfn[YQhcHWvYX6gVmlROiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDheZRweGixc4Doc5J6dGG2aX;uJJBz\S2rbnP1ZoF1\WRiZn;yJFMxKG2rboOg[o9tdG:5ZXSgZpkhcW6ldXLheIlwdiC5aYToJGFVWCCob4KgNkBpenNiYomgRWRRNUeubzDhd5NigSxiSVO1NEA:KDBwMEGg{txONg>? MkPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2NUW2OVQoRjJ4NEW1OlU1RC:jPh?=
sf21 M4[ySWZ2dmO2aX;uJIF{e2G7 NEDzRWNDcW6maX7nJIFn\mmwaYT5JJRwKHerbHSgeJlx\SCqdX3hckBjcW:2aX6gcIFj\WyuZXSgdFM5KGGucHjhJEg6KHSxIEO1NkBz\XOrZIXld{kh\XiycnXzd4VlKGmwIIPmNlEhcW6|ZXP0JINmdGy|IGPQVkBidmGueYPpd{whU2RiPTCwMlAzOTdizszNMi=> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDh|NESzNUc,Ojh6M{S0N|E9N2F-
PBMC NEnsWm1HfW6ldHnvckBie3OjeR?= NEX3UWhKdmirYnn0bY9vKG:oIGTOSk1idHCqYTDwdo9lfWO2aX;uJIJ6KGyrcH;wc4x6e2GlY3jhdoll\S2|dHnteYxifGWmIHj1cYFvKHCncnnwbIVz[WxiYnzvc4QhdW:wb371Z4xm[XJiY3XscJMtKEmFNUCgQUAxNjB{NTFOwG0v M3jnfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl6N{O3N|AoRjl6N{O3N|A9N2F-
PBMC NW[wd2U5TnWwY4Tpc44h[XO|YYm= M1O0XGlvcGmkaYTpc44hd2ZiTGDTMZN1cW23bHH0[YQhXEhtTl[tZYxxcHNicILv[JVkfGmxbjDifUBpfW2jbjDw[ZJqeGincnHsJIJtd2:mIH3vco9vfWOuZXHyJINmdGy|IDjQRm1EeyluIFnDOVAhRSByLkCyOUDPxE1w NV\4eWRGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUe4OFA6Oyd-OUe4OFA6OzxxYU6=
PBMC NGSyNFdHfW6ldHnvckBie3OjeR?= MWTJcohq[mm2aX;uJI9nKHB|ODDNRXAhc2mwYYPlJJJmdGG2ZXSgWG5HNWGucHjhJJJmdGWjc3Wg[pJwdSCyZYLpdIhmemGuIHLsc49lKG2xbn;ueYNt\WG{IHPlcIx{KCiSQl3DLUwhUUN3MDC9JFAvODN5IN88UU4> NGj0U|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkC2NVg4Pid-MUKwOlE5PzZ:L3G+
PBMC M4qxR2Z2dmO2aX;uJIF{e2G7 MUTJcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIFnMNU1j\XSjIIDyc4R2[3Srb36gbY4hcHWvYX6gdIVzcXCqZYLhcEBjdG:xZDDtc45wdnWlbHXhdkBk\WyuczjQRm1EeyluIFnDOVAhRSByLkC0PEDPxE1w M3;zWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl5OESwPVMoRjl5OESwPVM9N2F-
SW1353 MlfoSpVv[3Srb36gZZN{[Xl? MYXDc41xd3WwZDD3ZZMh\X[jbIXheIVlKG[xcjDpeJMh[WKrbHn0fUB1dyCrbnjpZol1KEmOLU[gdJJw\HWldHnvckBqdiCVV{GzOVMh[2WubIOgeJJm[XSnZDD3bZRpKGO7dH;rbY5meyCLTD2xJIFv\CCWTl[sJGlEPTBiPTCwMlA2KM7:TT6= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yODl7OUS2O{c,OTB7OUm0Olc9N2F-
SW1353 NVzD[GVVTnWwY4Tpc44h[XO|YYm= MXvJcohq[mm2aX;uJI9nKFSQRjDhcoQhUUxvMTDpcoR2[2WmIFnMMVYheHKxZIXjeIlwdiCrbjDoeY1idiClaH;u[JJwNXOjcnPvcYEhW1diMUO1N{Bk\WyuczygTWM2OCB;IECuNFUh|ryPLh?= MkDGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB7OUm0OlgoRjFyOUm5OFY5RC:jPh?=
THP1 MoO5SpVv[3Srb36gZZN{[Xl? M4f5bGlvcGmkaYTpc44hd2ZiTGDTMZN1cW23bHH0[YQhUUxzIIDyc4R2[3Srb36gbY4hcHWvYX6gWGhROSClZXzsd{whUUN3MDC9JFAvODVizszNMi=> NFTEcIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEC3O|M3Oyd-MUiwO|c{PjN:L3G+
THP1 MY\GeY5kfGmxbjDhd5NigQ>? MXrJcohq[mm2aX;uJI9nKEySUz3zeIlufWyjdHXkJHRPTmGucHjhJJBzd2S3Y4Tpc44hcW5iaIXtZY4hXEiSMTDj[YxteyxiSVO1NEA:KDBwMEWg{txONg>? M3j1WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEe3N|Y{Lz5zOEC3O|M3OzxxYU6=
THP1 M4SwZmZ2dmO2aX;uJIF{e2G7 NH\EWoVKdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJJR2dW:{IH7lZ5Jwe2m|IH\hZ5Rwei2jbIDoZUApXE6ILXHsdIhiMSCycn;keYN1cW:wIHnuJHRJWC1zIHPlcIx{NCCHQ{WwJF0hOC5yNjFOwG0v MnvuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTJyOE[0PFUoRjF{MEi2OFg2RC:jPh?=
THP1 MU\GeY5kfGmxbjDhd5NigQ>? NE\IcWlKdmirYnn0bY9vKG:oIIT1cY9zKG6nY4Lvd4l{KG[jY4TvdkBidHCqYTDy[Yxm[XOnIHL5JHRJWC1zIHPlcIx{NCCLQ{WwJF0hOC5yNzFOwG0v NH21U2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNU[1PFg2PSd-MUW2OVg5PTV:L3G+
monocytic cell M3rYemZ2dmO2aX;uJIF{e2G7 MkjyTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JHRPTi2jbIDoZUBxem:mdXP0bY9vKHW|aX7nJIxqeG:yb3z5d4Fk[2ijcnnk[UB{fGmvdXzheIVlKGi3bXHuJI1wdm:leYTpZ{Bk\WyuczygTWM2OCB;IECuNFczKM7:TT6= NEHBdGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMkeyPVY{Pyd-MUK3Nlk3Ozd:L3G+
THP1 NVrPUndMTnWwY4Tpc44h[XO|YYm= NVywOlhpUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEySUz3zeIlufWyjdHXkJHRPTi2jbIDoZUBxem:mdXP0bY9vKGmwIHj1cYFvKG2xbn;jfZRq[yClZXzsd{ApXEiSLUGpMEBKSzVyIE2gNE4xPzJizszNMi=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTF|OUe0PUc,OTVzM{m3OFk9N2F-
THP-1 NFroeodHfW6ldHnvckBie3OjeR?= NVfZSIxbUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGyrcH;wc4x6e2GlY3jhdoll\SC|dHnteYxifGWmIGTOSk1idHCqYTDwdo9lfWO2aX;uJIlvKFSKUD2xJINmdGy|IDjoeY1idiCvb37vZ5l1cWNiY3XscJMqNCCLQ{WwJF0hOC5yN{Kg{txONg>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTh|N{OxNEc,OTV6M{ezNVA9N2F-
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PBMC MVzGeY5kfGmxbjDhd5NigQ>? MnTnTY5pcWKrdHnvckBw\iC|dHHwbJltd2OxY3PhcEBmdnSncn;0c5hqdiCEKGPFRkkhe3SrbYXsZZRm\CC2dX3vdkBv\WO{b4Ppd{Bn[WO2b4KgZYxxcGFiKGTOSk1idHCqYTmgdJJw\HWldHnvckBjgSCqdX3hckBx\XKrcHjldoFtKGKub3;kJI1wdm:wdXPs[YFzKGOnbHzzLHBDVUO|KTygTWM2OCB;IECuNVYh|ryPLh?= MmfDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTd6NEC5N{c,QTd6NEC5N|ww[T5?
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macrophage-like cell MVPBcpRqcW6obHHtcYF1d3K7IHHzd4F6 NYLRbW16OzBibXnudy=> MWTBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJIh2dWGwIFjMMVYxKGSncnn2[YQhdWGlcn;wbIFo\S2uaXvlJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgWG5H[WyyaHGgdJJw\HWldHnvckB1emWjdHXkJFMxKG2rboOgZoVnd3KnIFzQV{B{fGmvdXzheIlwdiCvZXHzeZJm\CCjZoTldkAzPCCqcoOgZpkhTUyLU1GsJGlEPTBiPTC4MlYh|ryPLh?= MoTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MUGwPFkoRjJ|OEGxNFg6RC:jPh?=
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A673 NFLLeFhyUFSVIHHzd4F6 MXfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 NWKwe2h[eUiWUzDhd5NigQ>? M3LHZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= M4\WR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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OHS-50 NGWxUlhyUFSVIHHzd4F6 Mnz0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= NFr4TII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MUPxTHRUKGG|c3H5 NVK5WIZPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> Mnf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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Assay
Methods Test Index PMID
Western blot phospho-p38 / p38 ; p-ASK1 / ASK1 / P-JNK / p-MKK4 / p-ERK ; phospho-MK2(T334) / phospho-HSP27(S82) / phospho-Akt(T308) / phospho-Akt(S473) 25747578 24082073 21737674
Immunofluorescence dsRNA / hnRNP A1 25747578
Growth inhibition assay Cell viability 23001390
In vivo SB203580 protects pig myocardium against ischemic injury in an in vivo model. [4]SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE). [5]

Protocol (from reference)

Kinase Assay:

[1]

  • Cellular receptor kinase phosphorylation assay :

    4 μg of sheep anti-PKBα is immobilized on 25 μL of protein G-Sepharose overnight (or 1.5 hours) and washed in Buffer A (50 mm Tris, pH 7.5, 1 mm EDTA, 1 mm EGTA, 0.5 mm Na3VO4, 0.1% β-mercaptoethanol, 1% Triton X-100, 50 mm sodium fluoride, 5 mm sodium pyrophosphate, 0.1 mm phenylmethylsulfonyl fluoride, 1 μg/mL aprotinin, pepstatin, leupeptin, and 1 μm microcystin). The immobilized anti-PKB is then incubated with 0.5 ml of lysate (from 5 × 106 cells) for 1.5 hours and washed three times in 0.5 mL of Buffer A supplemented with 0.5 m NaCl, two times in 0.5 mL of Buffer B (50 mm Tris-HCl, pH 7.5, 0.03% (w/v) Brij-35, 0.1 mm EGTA, and 0.1% β-mercaptoethanol), and twice with 100 μl of assay dilution buffer; 5× assay dilution buffer is 100 mm MOPS, pH 7.2, 125 mm β-glycerophosphate, 25 mm EGTA, 5 mm sodium orthovanadate, 5 mm DTT. To the PKB enzyme immune complex is added 10 μL of assay dilution buffer, 40 μm protein kinase A inhibitor peptide, 100 μm PKB-specific substrate peptide, and 10 μCi of [γ-32P]ATP, all made up in assay dilution buffer. The reaction is incubated for 20 minutes at room temperature with shaking, then samples are pulse spun, and 40 μL of reaction volume are removed into another tube to which is added 20 μL of 40% trichloroacetic acid to stop the reaction. This is mixed and incubated for 5 minutes at room temperature, and 40 μL is transferred onto P81 phosphocellulose paper and allowed to bind for 30 seconds. The P81 piece is washed three times in 0.75% phosphoric acid then in acetone at room temperature. γ-32P incorporation is then measured by scintillation counting.

Cell Research:

[1]

  • Cell lines: CT6 cell , BA/F3 F7 cell
  • Concentrations: 0–30 μM
  • Incubation Time: 1 hour
  • Method:

    CT6 cell and BA/F3 F7 cell are rested by washing three times in RPMI and culturing overnight in RPMI, 5% fetal calf serum in the absence of growth factor, antibiotics, or β-mercaptoethanol supplements. 2–5 × 106 rested CT6 cells are resuspended in 2 mL of RPMI, 5% fetal calf serum and preincubated with SB203580 or vehicle control as indicated in figure legends. Cells are then stimulated with 20 ng/ml recombinant human IL-2 for 5 minutes at 37  °C and pelleted in a minifuge for 30 seconds, medium is aspirated, and the pellet is lysed in the appropriate buffer. BA/F3 cells stably expressing deletion mutants of IL-2 receptor β chain are maintained in glutamine containing RPMI further supplemented with 5% fetal calf serum and 0.2 μg/mL G418. The cells are then washed extensively, rested overnight, and washed again before activating with IL-2; such cell preparations are >90% T cells. Cellular proliferation assays are performed by measurement of [3H]thymidine incorporation.

  • (Only for Reference)
Animal Research:

[5]

  • Animal Models: Systemic lupus erythematosus (SLE) are established in female MRL/lpr mice and female C57BL/6 mice
  • Dosages: 0.1 M/day
  • Administration: Orally administered
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 43 mg/mL warmed
(113.92 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 377.43
Formula

C21H16FN3OS

CAS No. 152121-47-6
Storage 3 years -20°C(in the dark) powder
Smiles CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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