JNK Inhibitor VIII

Catalog No.S7794 Synonyms: TCS JNK 6o

For research use only.

JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively.

JNK Inhibitor VIII Chemical Structure

CAS No. 894804-07-0

Selleck's JNK Inhibitor VIII has been cited by 4 Publications

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Biological Activity

Description JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively.
Targets
JNK1 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
JNK1 [1]
(Cell-free assay)
JNK3 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
2 nM(Ki) 4 nM(Ki) 45 nM 52 nM(Ki) 160 nM
In vitro

TCS-JNK-6a binds competitively and reversibly to the ATP site. This compound demonstrates a remarkable selectivity profile. Additionally, it shows some inhibition of c-Jun phosphorylation in hepG2 cells. TCS-JNK-6o is a 2,5-dimethoxy analogue of TCS-JNK-6a with the dimethoxy substitution of the phenyl ring. TCS-JNK-6o shows further gains in potency.[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB7 NX3GNFJpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEPhc2dKdmirYnn0bY9vKG:oIHj1cYFvKE6ENzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNlc1PzQQvF2= M33mXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODZzOD:nQnNCVkeHUkyvZV4>
LB2241-RCC NYHjPIpqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYnJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjV5N{O5{txO MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA3OThxJ{7TRW5ITVJ:L3G+
NCI-H1299 MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVu0WoRCUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFEzQTliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6yNFE6|ryP NYX2OWY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyNkG4M{c,W0GQR1XSQE9iRg>?
BV-173 NImyc2hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4SzVGlvcGmkaYTpc44hd2ZiaIXtZY4hSlZvMUezJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvODVyNd88US=> MlLUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPjF6Lze+V2FPT0WUPD;hQi=>
HPAF-II NUDl[m5PT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFXEdWtKdmirYnn0bY9vKG:oIHj1cYFvKEiSQV[tTWkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC53OEez{txO MoPMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPjF6Lze+V2FPT0WUPD;hQi=>
RS4-11 NUHzfG5JT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoPCTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk43Pzl3zszN NITGTIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB4MUivK|5USU6JRWK8M4E,
EW-1 M3rC[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn;NTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUeuNVg5O87:TR?= NEnvcGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB4MUivK|5USU6JRWK8M4E,
NCI-H1581 Mmq3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYDJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUW4NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE4NjJ3OElOwG0> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA3OThxJ{7TRW5ITVJ:L3G+
SK-PN-DW MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{jpdmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvUF6tSHch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy57NEi1{txO MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA3OThxJ{7TRW5ITVJ:L3G+
KP-4 NYDXToIzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWjkT4hHUW6qaXLpeIlwdiCxZjDoeY1idiCNUD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvOTB6N988US=> M1PYdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODZzOD:nQnNCVkeHUkyvZV4>
DU-145 MnfhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG\CW|JKdmirYnn0bY9vKG:oIHj1cYFvKESXLUG0OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE6Njh5NElOwG0> NUCzZWtZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyNkG4M{c,W0GQR1XSQE9iRg>?
ACHN MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn3mTY5pcWKrdHnvckBw\iCqdX3hckBCS0iQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkCuOlIyO87:TR?= NXTHVpdERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyNkG4M{c,W0GQR1XSQE9iRg>?
A172 M{PNe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIm4THhKdmirYnn0bY9vKG:oIHj1cYFvKEFzN{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU4zPjQQvF2= NXnBVXltRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyNkG4M{c,W0GQR1XSQE9iRg>?
HuO-3N1 NVjUc|h1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1jUZWlvcGmkaYTpc44hd2ZiaIXtZY4hUHWRLUPONUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjR|MUlOwG0> NWX6[Y55RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyNkG4M{c,W0GQR1XSQE9iRg>?
QIMR-WIL M3XuO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXizVHJ2UW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ{LkOyO|TPxE1? MoPJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPjF6Lze+V2FPT0WUPD;hQi=>
NCI-H1650 MnnzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnWzTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOi55OEez{txO M37SSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODZzOD:nQnNCVkeHUkyvZV4>
SW1088 M{nsXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{HzNmlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMEi4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvOTZ2Md88US=> M{DpbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODZzOD:nQnNCVkeHUkyvZV4>
Mewo NVfnRXJET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWXJcohq[mm2aX;uJI9nKGi3bXHuJG1mf29iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Mz6zPVk4|ryP MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA3OThxJ{7TRW5ITVJ:L3G+
NCI-H1355 MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHvlUlhKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVM2PSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ2Lk[zOlXPxE1? M2H5PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODZzOD:nQnNCVkeHUkyvZV4>
SK-LU-1 NYLRU|BFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWDJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyXLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO{4xPTkQvF2= NULGVVl6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyNkG4M{c,W0GQR1XSQE9iRg>?
KYSE-70 M13CVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoD3TY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvOTJ3zszN MkT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPjF6Lze+V2FPT0WUPD;hQi=>
KP-N-YS NGnJUWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVvLTlB4UW6qaXLpeIlwdiCxZjDoeY1idiCNUD3OMXlUKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjdwNUewOu69VQ>? NF3NXIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB4MUivK|5USU6JRWK8M4E,
HTC-C3 NXX0c3hFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVT0e2FZUW6qaXLpeIlwdiCxZjDoeY1idiCKVFOtR|Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPy55M{S1{txO M4niXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODZzOD:nQnNCVkeHUkyvZV4>
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BEN MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGj6XmNKdmirYnn0bY9vKG:oIHj1cYFvKEKHTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5Mlg3Pc7:TR?= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA3OThxJ{7TRW5ITVJ:L3G+
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SF295 MkLUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NILF[|ZKdmirYnn0bY9vKG:oIHj1cYFvKFOIMkm1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|IvOTV4zszN NUfmTGE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyNkG4M{c,W0GQR1XSQE9iRg>?
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LCLC-103H M3jtfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{Xib2lvcGmkaYTpc44hd2ZiaIXtZY4hVEOOQz2xNFNJKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRwMkKyN:69VQ>? M17qVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODZzOD:nQnNCVkeHUkyvZV4>
MN-60 MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkXoTY5pcWKrdHnvckBw\iCqdX3hckBOVi14MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2MlAyOzoQvF2= NGrZXpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB4MUivK|5USU6JRWK8M4E,
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BHY M2WyW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIO3[3FKdmirYnn0bY9vKG:oIHj1cYFvKEKKWTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2Mlk3PDYQvF2= NGrMfWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB4MUivK|5USU6JRWK8M4E,
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ES3 Mkn5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1nxWGlvcGmkaYTpc44hd2ZiaIXtZY4hTVN|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{iuNVk1Qc7:TR?= M3PxNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODZzOD:nQnNCVkeHUkyvZV4>
NBsusSR M4nJ[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUDJcohq[mm2aX;uJI9nKGi3bXHuJG5De3W|U2KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPU4{OTN{zszN MnHFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPjF6Lze+V2FPT0WUPD;hQi=>
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ChaGo-K-1 MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWTU[ZFYUW6qaXLpeIlwdiCxZjDoeY1idiCFaHHHc{1MNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12MT6xOVc3|ryP NV\rWZZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyNkG4M{c,W0GQR1XSQE9iRg>?
KYSE-450 NUDyXJYzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkTCTY5pcWKrdHnvckBw\iCqdX3hckBMYVOHLUS1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQyNjR3MUVOwG0> MnHaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPjF6Lze+V2FPT0WUPD;hQi=>
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DBTRG-05MG M{XGbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3LzSmlvcGmkaYTpc44hd2ZiaIXtZY4hTEKWUletNFVOTyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTR2Lk[1OFbPxE1? NF7yZWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB4MUivK|5USU6JRWK8M4E,
HCC1806 NUXnR5hXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVPEdm1OUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxPFA3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDVwMkG2Pe69VQ>? MkH2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPjF6Lze+V2FPT0WUPD;hQi=>
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DOK NWfDW|RtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGRQUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTR6LkO4O|fPxE1? NFTJVpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB4MUivK|5USU6JRWK8M4E,
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In vivo

Pharmacokinetic profiles are determined for JNK Inhibitor VIII (TCS-JNK-6o) in Sprague-Dawley rats. JNK Inhibitor VIII (TCS-JNK-6o) showes a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism is very rapid with this compound.[1]

Protocol (from reference)

Kinase Assay:

[1]

  • Ser/Thr-kinase:

    Ser/Thr-kinase assays are performed using a radioactive FlashPlate-based assay platform. In this format, biotinylated substrate peptide (2 μM), γ-[33P]-ATP (5 μM, 2 mCi/μmol), inhibitors (3-10000 nM in 2% DMSO), and enzyme are incubated for 1 h in buffer containing 25 mM Hepes, pH 7.5, 1 mM DTT, 10 mM MgCl2, 100 μM Na3VO4, and 0.075 mg/mL Triton X-100, stopped with 80 μL of stop buffer containing 100 mM EDTA and 4 M NaCl, transferred to streptavidin-coated 384-well FlashPlates, which are then washed 3 times and read using a TopCount microplate reader.

Cell Research:

[1]

  • Cell lines: hepG2 cells
  • Concentrations: Serial concentrations
  • Incubation Time: 1 h
  • Method:

    HepG2 human hepatoma cells (ATCC) are cultured in low glucose MEM supplemented with 1×NEAA, 1×sodium pyruvate, and 10% FBS. For P-c-Jun assays, cells are plated at 5×104 cells/well in 500 μL of complete media on 24-well collagen-coated plates and incubated overnight. Serial compound dilutions are made in DMSO at 100×, and then 5 μL is added directly to the media on the cells to provide the final inhibitor concentrations. After 1 h, cells are stimulated with vehicle control or TNFR for 30 min and harvested in 70μL of lysis buffer (TBS (54 mM Tris-HCl, pH 7.6, 150 mM NaCl), 1% TritonX-100,0.5% Nonidet P-40, 0.25% sodium deoxycholate, 1 mM EDTA, 1 mM EGTA, 0.5 mM sodium fluoride, 1 mM pervanadate, 1 μM microcystin, 1 mM AEBSF, 1 tablet of complete EDTA Free-Mini inhibitor cocktail) and frozen at -80 °C prior to use in the P-c-Jun assay.

Animal Research:

[1]

  • Animal Models: Sprague-Dawley rat
  • Dosages: 5 mg/kg
  • Administration: IV, Oral gavage

Solubility (25°C)

In vitro

DMSO 71 mg/mL
(199.22 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 356.38
Formula

C18H20N4O4

CAS No. 894804-07-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=C(C(=CC(=N1)NC(=O)CC2=C(C=CC(=C2)OC)OC)N)C#N

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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