SP600125

For research use only.

Catalog No.S1460 Synonyms: Nsc75890

812 publications

SP600125 Chemical Structure

CAS No. 129-56-6

SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.

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Selleck's SP600125 has been cited by 812 publications

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Choose Selective JNK Inhibitors

Biological Activity

Description SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Targets
serine/threonine kinase [1]
()
JNK1 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
Aurora A [4]
(Cell-free assay)
TrkA [4]
(Cell-free assay)
40 nM 40 nM 60 nM 70 nM
In vitro

SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50 of 5 μM to 12 μM. [1] However, later studies reveal that SP600125 also suppresses aryl hydrocarbon receptor (AhR) [2], Mps1 [3], and a panel of other serine/threonine kinases, including Aurora kinase A, FLT3, MELK, and TRKA [4]. In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation. [5] In HCT116 cells, SP600125 (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep3B MUDGeY5kfGmxbjDBd5NigQ>? M2PuUFExKM7:TR?= MoPYNUBp MmTnRoxw[2u|IHH1eI9xcGGpeTDhcoQhfXC{ZXf1cIF1cW:wIH;mJGJm[2yrbjCxJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSClZYLhcYll\Q>? MoTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlyNkC5NlAoRjF7ME[wPVIxRC:jPh?=
BV-2 NH7nOYRHfW6ldHnvckBCe3OjeR?= NEm5NGczKM7:TR?= M2\mN|EhcA>? NIXxUWxKdmirYnn0d{B1cGViaX7jdoVie2Vib3[gd2JCTkZicnXs[YF{\SCrbjDHcYl5NXS{ZXH0[YQhSlZvMjDj[Yxtew>? MmTvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl2ME[4N|EoRjF7NEC2PFMyRC:jPh?=
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PC3 M3fVcmZ2dmO2aX;uJGF{e2G7 NGroSFczOCEQvF2= NVq4W3kzOSCq NXHnfmxSTGWlcnXhd4V{KHSqZTDNUXAzKGGwZDDNUXA6KGW6cILld5Nqd25? MlXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl4M{O5O|UoRjF7NkOzPVc2RC:jPh?=
Plasmodium falciparum HB3 Mn;iRY51cWKjY4TldolidCCDc4PhfS=> MkSwO|IhcA>? MnnBSG1UVw>? NYnvVHNCSW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDdwOUSzNlgh|ryP MmToQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5M{S5NVAoRjF7N{O0PVExRC:jPh?=
Plasmodium falciparum W2 NXHCW4JqSW62aXLhZ5RmemmjbDDBd5NigQ>? MXS3NkBp NWT6SVh4TE2VTx?= NFr6fXJCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhPy57NEOyPEDPxE1? NHrZPVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUezOFkyOCd-MUm3N|Q6OTB:L3G+
Plasmodium falciparum 7G8 Mne3RY51cWKjY4TldolidCCDc4PhfS=> M1jQZ|czKGh? MnP1SG1UVw>? NWPINGU3SW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDFyIN88US=> NVv0V4NMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3N|Q6OTBpPkG5O|M1QTFyPD;hQi=>
Plasmodium falciparum 3D7 M4HVWGFvfGmkYXP0[ZJq[WxiQYPzZZk> MUS3NkBp NUm2W45zTE2VTx?= M3q1WGFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOi53OEmzJO69VQ>? M3\0cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{O0PVExLz5zOUezOFkyODxxYU6=
Plasmodium falciparum GB4 NI\hUmZCdnSrYnHjeIVzcWGuIFHzd4F6 MXm3NkBp NWi2OGw2TE2VTx?= M37PTGFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOi53OEmz{txO NGTXSIM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUezOFkyOCd-MUm3N|Q6OTB:L3G+
HaCaT MYrGeY5kfGmxbjDBd5NigQ>? NIiyS|QzOCEQvF2= MXy0JIg> NHTYUW9FVVOR MUnCcI9kc3NidHjlJHRPTi4QsT3pcoR2[2WmwrDDXXA1TjFzwrD0doFve2O{aYD0bY9v MnjkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6MUKzOFkoRjF7OEGyN|Q6RC:jPh?=
HaCaT MXHGeY5kfGmxbjDBd5NigQ>? Mn7vNlAh|ryP MV6yOEBp NELVXmFFVVOR MU\CcI9kc3NidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBkNUq3bjDwdo91\Wmw M{TYVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEGyN|Q6Lz5zOUixNlM1QTxxYU6=
A549 Mlz6SpVv[3Srb36gRZN{[Xl? NFnaS3gzOCEQvF2= M2fnT|EhcA>? NFLX[W1KdmirYnn0bY9vKG:oIGTQRU1qdmS3Y3XkJG1OWC1{IHHu[EB2NVCDIHX4dJJme3Orb36= NX7ac4g5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0PVIyPzVpPkKwOFkzOTd3PD;hQi=>
PC12 MVrGeY5kfGmxbjDBd5NigQ>? MnK4NVAh|ryP NIf6RYE2KGh? M1LRSmROW09? NFy5c4dC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFCGOUiwOVk> MkLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEW2PFUoRjJzM{S1Olg2RC:jPh?=
PC12 M1PSSGZ2dmO2aX;uJGF{e2G7 NEnWNYQyOCEQvF2= MXe1JIg> M3O3SGROW09? M2X6WGFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghXTBzMk[= MlPBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEW2PFUoRjJzM{S1Olg2RC:jPh?=
PC12 NFnmfFBHfW6ldHnvckBCe3OjeR?= MVqxNEDPxE1? M33TVlUhcA>? NFra[YxFVVOR NXHDXXNtSWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCVUE[wNFEzPQ>? NYrXeodrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOFU3QDVpPkKxN|Q2Pjh3PD;hQi=>
PC12 NWTV[nRvTnWwY4Tpc44hSXO|YYm= Mlz5NVAh|ryP NWHWUHl3PSCq Ml;QSG1UVw>? M1vuTGFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW0J{MEO1PFA> NITUcos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO0OVY5PSd-MkGzOFU3QDV:L3G+
B16-F10 NXm2TnczTnWwY4Tpc44hSXO|YYm= NHXlbGYyKGh? M1\4e2lvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiYz3KWW4heGixc4Doc5J6dGG2aX;u NFq0eYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUixOVY{PCd-MkG4NVU3OzR:L3G+
LoVo NYTo[HVwTnWwY4Tpc44hSXO|YYm= M2LIeVEh|ryP MXSxJIg> MnfITY5pcWKrdHnvckBw\iCSR1WyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iC3UFGgZY5lKE2PUD25JJNq\26rZnnjZY51dHl? MkT6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF6NUm0O|koRjJzOEW5OFc6RC:jPh?=
LoVo MXTGeY5kfGmxbjDBd5NigQ>? NXHr[mF7OSEQvF2= NX61V|BMOSCq M4O0VWJtd2Otc2DHSVIucW6mdXPl[EBk\WyuIH3p[5JifGmxbjDzbYdvcW[rY3HueIx6 NWC5TnVJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG4OVk1PzlpPkKxPFU6PDd7PD;hQi=>
THP-1 MnnUSpVv[3Srb36gRZN{[Xl? M3;VXlkxKG6P MYGzNEBucW5? NX3xSWQ6UW6qaXLpeIlwdiCxZjD0bZN{fWViZnHjeI9zKGW6cILld5Nqd25? MmT6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7NECwOVkoRjJ{OUSwNFU6RC:jPh?=
PC3 M1j4[GZ2dmO2aX;uJGF{e2G7 MkDpNlUh|ryP M1z3flI1KGh? MVHJcohq[mm2aX;uJI9nKEGSLUGgZY5lKHB{MTDseYNq\mW{YYPlJIFkfGm4aYT5JIlv\HWlZXSgZpkhWzF5OVSgVHJN NX3EcolwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxOlI3PTJpPkKzNVYzPjV{PD;hQi=>
SH-SY5Y M1fZdGZ2dmO2aX;uJGF{e2G7 M{jEPVExKM7:TR?= NVz2U41sOSCq MUPEUXNQ MYXO[ZVzd3C{b4TlZ5RqfmViYXP0bZZqfHliYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGGwaYPvcZlkcW5vaX7keYNm\CClZXzsJIRm[XSq NV\LOWp2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PVg6OTRpPkKzOFk5QTF2PD;hQi=>
SH-SY5Y NGP3V3hMcW6jc3WgRZN{[Xl? NHztWWcyOCEQvF2= NWPxc2VYOSCq M17S[mROW09? MojaTY5pcWKrdHnvckBw\iCMTluzJIF{e2W|c3XkJIF{KGKub3PrZYRmKG:oIHHubZNwdXmlaX6tbY5lfWOnZDDjMYp2diCyaH;zdIhwenmuYYTpc44h[XRic3XyO|M> MnnpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OUi5NVQoRjJ|NEm4PVE1RC:jPh?=
RAW264.7 MYnGeY5kfGmxbjDBd5NigQ>? NI\HbWYyOCEQvF2= NGe5dWczPCCq NHj6U|RCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwuOWKndHGgdoVt\WG|ZR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MUC3PEc,OjN5OUGwO|g9N2F-
RAW264.7 M{f2fWZ2dmO2aX;uJGF{e2G7 MlTqNVAh|ryP NU\peZRDOjRiaB?= MWDBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgbW5QWyCneIDy[ZN{cW:w NXvjXm9oRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVExPzhpPkKzO|kyODd6PD;hQi=>
RAW264.7 NYW4fIp1TnWwY4Tpc44hSXO|YYm= MVexNEDPxE1? NWm2eGlOOiCq MY\BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdg>? NIPzdlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NVA4QCd-MkO3PVExPzh:L3G+
A549 NXLYdFIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXT2ZWY5OjBizszN NHX6V|g4OiCq NVzNTnpiTE2VTx?= MYrSZZBq\CCjbnSgdI91\W62IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9v NXzU[JR1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVI5PDBpPkKzPVEzQDRyPD;hQi=>
RAW264.7 NFnNWGdCdnSraX7mcIFudWG2b4L5JIF{e2G7 MYDBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhVFCVLXnu[JVk\WRiTl:gdJJw\HWldHnvckBz\WyjdHn2[UB1dyClb370do9tNCCLQ{WwJF0hOTdizszNMi=> MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh|MUe5PEc,OjJ6M{G3PVg9N2F-
BMMC MYnGeY5kfGmxbjDhd5NigQ>? MV2xJJRwKDJyIIXN MmTXO{Bl[Xm| MXHJcohq[mm2aX;uJI9nKFKDTlvMM20uS1OILYP0bY12dGG2ZXSgc5N1\W:lbHHzeI9o\W6nc3nzJIlvKEmFUjDtc5V{\SCETV3DJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDUVmFRKHCxc3n0bZZmKG23bITpcpVkdGWjdHXkJINmdGy|IHH0JFEhfG9iMkCgeW0hcW6ldXLheIVlKG[xcjC3JIRigXNiYomgcIlocHRibXnjdo9{[2:yeR?= Mly5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|OUe2O|YoRjJ3M{m3Olc3RC:jPh?=
A673 MmDKdWhVWyCjc4PhfS=> M{XGVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 MmXDdWhVWyCjc4PhfS=> NUTVWmdDeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz M3nBb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH Mn;XdWhVWyCjc4PhfS=> NUPzNIFMeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> MnHhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 NXX0S5BbeUiWUzDhd5NigQ>? MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 MV7xTHRUKGG|c3H5 MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NGHnUFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NXP1[Jp7eUiWUzDhd5NigQ>? NUTo[2RYeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NEm4RVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NVryb454eUiWUzDhd5NigQ>? NFruXpVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> M{[zWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 NV;QRo5neUiWUzDhd5NigQ>? MXXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NWnlbYJjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-JNK; 

PubMed: 25226534     


(A) HepG2 cells were treated with increasing doses of SP600125 for 48 h, followed by western blot analysis of c-Jun N-terminal kinases (JNK) phosphorylation;

p-IGF1R / IGF1R / p-Akt / Akt / p-ERK / ERK; 

PubMed: 25226534     


(B) HepG2 cells were treated with SP600125 for 48 h at the indicated doses, followed by western blot analysis of phosphorylated IGF-1R, Akt, Erk1/2 and total IGF-1R, Akt, Erk1/2; (C) HepG2 cells were treated with 15 µM SP600125 for indicated periods, followed by western blot analysis of phosphorylated IGF-1R, Akt, Erk1/2 and total IGF-1R, Akt, Erk1/2;

p-Src / Src; 

PubMed: 25226534     


HepG2 cells were treated with 15 µM SP600125 for the indicated time. Total protein extracts were harvested and subjected to western blot analysis of phosphorylated Src and total Src.

p-c-Jun / c-Jun / pJNK / JNK; 

PubMed: 27176481     


JNK inhibitor SP600125 suppressed JNK signaling via reducing c-Jun phosphorylation, whereas JNK phosphorylation was not affected

Survivin / Bcl-2 / PARP; 

PubMed: 22870247     


The effect of SP600125 on the apoptosis regulator proteins in SW1116/HCPT cells were measured by Western-blot analysis.

p-FADD / FADD / p-c-Jun / c-Jun ; 

PubMed: 21859840     


A549-FKR cells were treated as described for FKR reporter assay and lysates analyzed with specific antibodies by western blot. Treatment with FADD-kinase inhibitor SP600125 shows dose dependent decrease in phosphorylated FADD protein that correlates with FKR activity.

25226534 27176481 22870247 21859840
Immunofluorescence
AIF / Endo G; 

PubMed: 21738692     


Representative confocal images showing translocation of AIF and Endo G to the nucleus, and nuclear condensation, at the indicated times after treatment with 5 µM of β-lap for 6 h in the presence or absence of SP600125 (30 µM). Nuclear translocation of AIF and Endo G is demonstrated by overlap of AIF or Endo G (green) and nuclear staining (red), resulting in a yellow color. 

E-cadherin / β-catenin ; 

PubMed: 21030692     


Human primary keratinocytes were treated with 10 μM SP600125 for 30 min or transduced with recombinant lentivirus encoding for flag-JNK1DN. Confocal of cells stained for β-catenin (red) and E-cadherin (green). Cell nuclei were stained with Hoechst (blue). 

α-catenin / Actin ; 

PubMed: 21030692     


Confocal images of the cells stained with α-catenin (red) and actin phalloidin (green). Cell nuclei were stained with Hoechst (blue). Scale bars = 20 μm.

21738692 21030692
Growth inhibition assay
Cell viability (U-87 MG); 

PubMed: 27176481     


U-87 MG cells were treated with SP600125 at different concentrations for 48 h. DMSO was used as a carrier control. Cell viability of U-87 MG cells sharply decreased when treated with SP600125.

Cell viability (A549); 

PubMed: 24944614     


Cells were treated with different concentrations of SP600125 (between 0 and 40 nM). The Cell Counting kit (CCK)-8 assay were then performed to measure the A549 cell viability. *P<0.05 vs. control; #P<0.05 vs. ALI.

27176481 24944614
In vivo

In mice, SP600125 (15 mg/kg or 30 mg/kg) significantly inhibits lipopolysaccharide (LPS)-induced TNF-α expression and anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. [1]

Protocol

Kinase Assay:

[4]

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In Vitro Kinase Assays :

The potency of SP600125 towards kinases, including MPS1, JNK, and Aurora kinase A, is determined based on the specific measurement of radioactive phosphotransfer to the substrate. For each enzyme, the absolute Km values for ATP and the specific substrate are initially determined and each assay is then run at optimized [ATP] (2·αKm) and [substrate] (5·Km) concentrations. MPS1 activity is measured using 5 nM of MPS1 recombinant protein in 50 mM HEPES pH 7.5, 2.5 mM MgCl2, 1 mM MnCl2, 1 mM DTT, 3 μM NaVO3, 2 mM β-glycerophosphate, 0.2 mg/mL BSA, 200 μM P38-βtide substrate-peptide (KRQADEEMTGYVATRWYRAE), and 8 μM ATP with 1.5 nM 33P-γ-ATP. Ten serial 1:3 dilutions (from 30 μM to 1.5 nM) of SP600125 are tested and IC50 determined.
Cell Research:

[4]

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  • Cell lines: HCT116, A2780, and U2OS cells
  • Concentrations: 0–5 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are seeded in 384 well-plates. One day after seeding, the cells are treated with SP600125 for 72 hours and the plates are then processed using a CellTiter-Glo assay. Inhibitory activity is evaluated comparing treated versus control data and IC50 value of proliferation is calculated.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Mouse LPS/TNF model (female CD-1)
  • Dosages: 15 or 30 mg/kg
  • Administration: Administered via intravenous injection or orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 44 mg/mL (199.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
2mg/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 220.23
Formula

C14H8N2O

CAS No. 129-56-6
Storage powder
in solvent
Synonyms Nsc75890
Smiles C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
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    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    how to reconstitute the inhibitor for in vivo studies?

  • Answer:

    S1460 can be dissolved in 5% DMSO/corn oil at 5 mg/ml as a clear solution for injection. The inhibitor dissolved in vehicle 30% PEG400/0.5% Tween80/5%Propylene glycol, at 30mg/ml is a suspension and can be used for oral administration.

JNK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID