BI-D1870

For research use only.

Catalog No.S2843

41 publications

BI-D1870 Chemical Structure

CAS No. 501437-28-1

BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.

Selleck's BI-D1870 has been cited by 41 publications

Purity & Quality Control

Choose Selective S6 Kinase Inhibitors

Biological Activity

Description BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. BI-D1870 exhibits anticancer attributes including the generation of reactive oxygen species (ROS) and increases in endoplasmic reticulum (ER) stress and autophagy.
Targets
RSK4 [1]
(Cell-free assay)
RSK3 [1]
(Cell-free assay)
RSK2 [1]
(Cell-free assay)
RSK1 [1]
(Cell-free assay)
15 nM 18 nM 24 nM 31 nM
In vitro

BI-D1870 inhibits RSK1, RSK2, RSK3 and RSK4 with an IC50 of 10–30 nM, but does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. BI-D1870 is cell permeant and prevents the RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in human embry-onic kidney 293 cells and Rat-2 cells. BI-D1870 does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Moreover, BI-D1870 does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EW-3 NGHu[Y9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHyZXRrUW6qaXLpeIlwdiCxZjDoeY1idiCHVz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjB|NUig{txONg>? NHrRPWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
H9 MmL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;tTY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6wOlAyQSEQvF2u Mlj1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
KARPAS-45 MkTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjRTY5pcWKrdHnvckBw\iCqdX3hckBMSVKSQWOtOFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwMU[1NlUh|ryPLh?= NVHlOmR7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
NCI-H720 M1fp[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDG[YI2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFczOCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6xO|E6PCEQvF2u MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
CTV-1 NELIfJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGNVXi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlQ4QDd{IN88UU4> NH7uOlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
DU-4475 MlvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGn0RZJKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwNUC0NVch|ryPLh?= NFvrTmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
A172 Mo\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoKxTY5pcWKrdHnvckBw\iCqdX3hckBCOTd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlUyPzB3IN88UU4> M1LVWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
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SBC-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlY6PTJ2IN88UU4> NITM[og9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
ECC10 MoLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrvO3Q4UW6qaXLpeIlwdiCxZjDoeY1idiCHQ1OxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC55MEC5OEDPxE1w M2[yb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
GAMG MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDoUmlKdmirYnn0bY9vKG:oIHj1cYFvKEeDTVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPzR5MUeg{txONg>? NIXoWJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
NCI-H209 NYLNTGpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkC5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjd4OEKg{txONg>? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
MC-IXC MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXuTY5pcWKrdHnvckBw\iCqdX3hckBOSy2LWFOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPzl3OEmg{txONg>? Mmq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
HSC-3 Ml:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGhUSy1|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlgyPzZ7IN88UU4> NY\oUXVWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
IST-SL1 M{[5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrPTY5pcWKrdHnvckBw\iCqdX3hckBKW1RvU1yxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjh2NUe0JO69VS5? NH3MRlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
LU-139 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H1W2lvcGmkaYTpc44hd2ZiaIXtZY4hVFVvMUO5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjh2OUW4JO69VS5? MlPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
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HL-60 NHHxTJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rRV2lvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvQDh|NkKg{txONg>? NEPwT2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
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TGW M3XJWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHRIXyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMT6wOVEzPCEQvF2u M3npNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
LAMA-84 NHnpTo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37FSGlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOS5zMke5OEDPxE1w NGK0Ook9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
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RPMI-7951 Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\tSmlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST23PVUyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB|LkO5O|Mh|ryPLh?= M1XNc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
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BB65-RCC MkPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLTTY5pcWKrdHnvckBw\iCqdX3hckBDSjZ3LWLDR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOy52NUO5OkDPxE1w NV7kfHNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
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KG-1 M2PpOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq0RlJKdmirYnn0bY9vKG:oIHj1cYFvKEuJLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFMvPjFzME[g{txONg>? NVWxbotFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
COLO-829 NIfKbnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPUeVdpUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVgzQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMz62OlYyQCEQvF2u NHGwVIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
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LB2241-RCC NXjaNWRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzhTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB|Lk[4OlI2KM7:TT6= M4[1RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
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OAW-28 NWXXSXIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXReWNKdmirYnn0bY9vKG:oIHj1cYFvKE:DVz2yPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOzh|LkS5N{DPxE1w MoDzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
NMC-G1 NYjBd5NnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xjb2lvcGmkaYTpc44hd2ZiaIXtZY4hVk2FLVexJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA{QTVwOUS3JO69VS5? MlfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
NCI-H1563 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfTZmdKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVU3OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iM{m4MlA6PiEQvF2u NUK0bZJDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
SW900 MkfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHNYQTByIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0NFEvOzJ4IN88UU4> Mn24QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
SW948 NV7u[plyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XCSmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7NEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQyOS5yOUSg{txONg>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
CAPAN-1 NHHJSVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJcohq[mm2aX;uJI9nKGi3bXHuJGNCWEGQLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQyOS5{OUKg{txONg>? MlnzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
UACC-257 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDHTY5pcWKrdHnvckBw\iCqdX3hckBWSUOFLUK1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDN|LkG1OUDPxE1w NXjLUJprRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
ZR-75-30 MmfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3LTY5pcWKrdHnvckBw\iCqdX3hckBbWi15NT2zNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDR7LkmzOEDPxE1w M3nkeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
NCI-H1993 NUTmWXZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnCZopbUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE6QTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IES4NE4zPjRizszNMi=> M3;UZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
LB996-RCC NXjOW4JkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rTfGlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ7OU[tVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSB2OUWuNlQyKM7:TT6= MonoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
L-428 NI\MfZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jrOmlvcGmkaYTpc44hd2ZiaIXtZY4hVC12MkigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFU2PC55ODFOwG0v NHviV|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
C3A MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnmU|BrUW6qaXLpeIlwdiCxZjDoeY1idiCFM1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFU3Oy55ODFOwG0v NX3hNIZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
IRF4 / MYC / MCL-1 / PARP ; 

PubMed: 25395420     


(B) H929 cells were incubated with BI-D1870 (BI, 3 μM) at indicated time points, followed by immunoblotting analysis. (C) JJN3 cells were incubated with BI-D1870 at indicated doses for 6 hours, followed by immunoblotting analysis.

p-YB1 / YB1 / p-Bad / Bad / p-RSK / RSK ; 

PubMed: 28415756     


Western Blot analysis of RSK activity (P(S102)-YB-1, P(S112)-Bad) of double resistant SKMel28 RR after treatment with increasing concentrations of BI-D1870 for 24 h. GAPDH was detected as a loading control.

p-GSK3 / p-ERK / ERK / p-CREB / CREB / p-S6 / p-LKB1 / LKB1; 

PubMed: 17040210     


(A) HEK-293 cells that had been deprived of serum for 16 h, were incubated in the absence or presence of 10 μM BI-D1870 for the indicated times, then stimulated with 400 ng/ml PMA (TPA) for 20 min. The cells were lysed and the lysates were immunoblotted with the indicated antibodies as described in the Materials and methods section. (B) As in (A), except that cells were incubated for 30 min with the indicated concentrations of BI-D1870 prior to stimulation with PMA. Similar results were obtained in two separate experiments.

IRF4 / MYC / MCL-1 / PARP ; 

PubMed: 25395420     


(B) H929 cells were incubated with BI-D1870 (BI, 3 μM) at indicated time points, followed by immunoblotting analysis. (C) JJN3 cells were incubated with BI-D1870 at indicated doses for 6 hours, followed by immunoblotting analysis.

p-YB1 / YB1 / p-Bad / Bad / p-RSK / RSK ; 

PubMed: 28415756     


Western Blot analysis of RSK activity (PS102-YB-1, PS112-Bad) of double resistant SKMel28 RR after treatment with increasing concentrations of BI-D1870 for 24 h. GAPDH was detected as a loading control.

p-GSK3 / p-ERK / ERK / p-CREB / CREB / p-S6 / p-LKB1 / LKB1 ; 

PubMed: 17040210     


(A) HEK-293 cells that had been deprived of serum for 16 h, were incubated in the absence or presence of 10 μM BI-D1870 for the indicated times, then stimulated with 400 ng/ml PMA (TPA) for 20 min. The cells were lysed and the lysates were immunoblotted with the indicated antibodies as described in the Materials and methods section. (B) As in (A), except that cells were incubated for 30 min with the indicated concentrations of BI-D1870 prior to stimulation with PMA. Similar results were obtained in two separate experiments.

25395420 28415756 17040210
Immunofluorescence
PDCD4 / F-actin ; 

PubMed: 25002506     


A375 cells treated as in (E) were imaged using immunofluorescence microscopy. Cells were stained with anti-PDCD4 antibodies to visualize endogenous PDCD4, phalloidin to visualize F-actin, and DAPI to visualize nuclei.

PDCD4 / F-actin ; 

PubMed: 25002506     


A375 cells treated as in E were imaged using immunofluorescence microscopy. Cells were stained with anti-PDCD4 antibodies to visualize endogenous PDCD4, phalloidin to visualize F-actin, and DAPI to visualize nuclei.

25002506
Growth inhibition assay
Cell viability; 

PubMed: 28415756     


(D–F) Cell viability (MUH assay) of double resistant melanoma cells after a 72 h-treatment with increasing concentrations of vemurafenib (D), trametinib (E) or vemurafenib and trametinib (F), as well as of BI-D1870 and the combination of MAPK inhibitors and BI-D1870 (n = 6; mean ± SD). Signals were normalized to the DMSO-treated controls.

Cell viability; 

PubMed: 28415756     


(D–F) Cell viability (MUH assay) of double resistant melanoma cells after a 72 h-treatment with increasing concentrations of vemurafenib (D), trametinib (E) or vemurafenib and trametinib (F), as well as of BI-D1870 and the combination of MAPK inhibitors and BI-D1870 (n = 6; mean ± SD). Signals were normalized to the DMSO-treated controls.

28415756

Protocol

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.27 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/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 391.42
Formula

C19H23F2N5O2

CAS No. 501437-28-1
Storage powder
in solvent
Synonyms N/A
Smiles CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C

In vivo Formulation Calculator (Clear solution)

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

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / 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 )

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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Molecular Weight Calculator

Molecular Weight Calculator

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

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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.

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Frequently Asked Questions

  • Question 1:

    BI-D1870 (catalog No.S2843) is found as a racemic mixture?

  • Answer:

    Yes, BI-D1870 (catalog No.S2843) is found as a racemic mixture.

S6 Kinase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID