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BI-D1870

For research use only.

Catalog No.S2843

36 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.

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Selleck's BI-D1870 has been cited by 36 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
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H9 NWnnfZpCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3zfYZKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlA3ODF7IN88UU4> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
KARPAS-45 MlzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLENJdKdmirYnn0bY9vKG:oIHj1cYFvKEuDUmDBV{01PSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6xOlUzPSEQvF2u NEXXeWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
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CTV-1 NWjYWIJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjMcJhKdmirYnn0bY9vKG:oIHj1cYFvKEOWVj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjR5OEeyJO69VS5? NFnaUI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
DU-4475 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlKzTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjVyNEG3JO69VS5? M{nhVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
A172 MoDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW1TY5pcWKrdHnvckBw\iCqdX3hckBCOTd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlUyPzB3IN88UU4> NICzTWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,
EW-18 MmfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml2zTY5pcWKrdHnvckBw\iCqdX3hckBGXy1zODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE43OjJzMTFOwG0v M2POTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
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KP-N-YS NYnTWoRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGtRNU5vWWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFAvPjh{MkOg{txONg>? M4DlWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
SBC-1 NFr0bnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTCwMlY6PTJ2IN88UU4> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
ECC10 NVmxS2NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHjbWZNUW6qaXLpeIlwdiCxZjDoeY1idiCHQ1OxNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOC55MEC5OEDPxE1w M2fSbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
GAMG M174U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGdCVUdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IECuO|Q4OTdizszNMi=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
NCI-H209 Mnz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnCRXVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLke2PFIh|ryPLh?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
MC-IXC MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXriWGEzUW6qaXLpeIlwdiCxZjDoeY1idiCPQz3JXGMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDBwN{m1PFkh|ryPLh?= M{D0U|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
HSC-3 M1LnO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnywTY5pcWKrdHnvckBw\iCqdX3hckBJW0NvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE45OTd4OTFOwG0v NX20THhRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
IST-SL1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTFWYhNUW6qaXLpeIlwdiCxZjDoeY1idiCLU2StV2wyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLki0OVc1KM7:TT6= NWnHcJpoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
LU-139 NWG3SYlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJcohq[mm2aX;uJI9nKGi3bXHuJGxWNTF|OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE45PDl3ODFOwG0v NYPybpRIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
ML-2 NXe5d|QyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTvU4VbUW6qaXLpeIlwdiCxZjDoeY1idiCPTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjh3NUe1JO69VS5? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
CAL-62 NH;5THNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jNSGlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjh6MUWyJO69VS5? M4GzSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
HL-60 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHu5VmRKdmirYnn0bY9vKG:oIHj1cYFvKEiOLU[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjh6M{[yJO69VS5? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
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UACC-893 MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fTb2lvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz24PVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDN4OD65OFgh|ryPLh?= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
OAW-28 NVn2[2M1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfMU5RUUW6qaXLpeIlwdiCxZjDoeY1idiCRQWetNlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDN6Mz60PVMh|ryPLh?= NXfle2hJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
NMC-G1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gN|k2Njl2NzFOwG0v NXriXWJvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
NCI-H1563 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUW2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hOzl6LkC5OkDPxE1w M1P2fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
SW900 NGrRUIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIf1N|VKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUCwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1ODFwM{K2JO69VS5? M4WwVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
SW948 M{\EcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnHOotKdmirYnn0bY9vKG:oIHj1cYFvKFOZOUS4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1OTFwMEm0JO69VS5? NYLSPHoxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
CAPAN-1 MlvZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7VTY5pcWKrdHnvckBw\iCqdX3hckBESVCDTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUA1OTFwMkmyJO69VS5? MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly1O|MyODdxJ{7TRW5ITVJ:L3G+
UACC-257 NVL5VnVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rFeGlvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDR|Mz6xOVUh|ryPLh?= M1G1VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
ZR-75-30 NX7GT3ZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWe2[FByUW6qaXLpeIlwdiCxZjDoeY1idiCcUj23OU0{OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iNES5Mlk{PCEQvF2u M{DheVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFU4OzFyNz:nQnNCVkeHUkyvZV4>
NCI-H1993 Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUm5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDhyLkK2OEDPxE1w Mnz1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
LB996-RCC MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW3TY5pcWKrdHnvckBw\iCqdX3hckBNSjl7Nj3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDR7NT6yOFEh|ryPLh?= NVLF[odlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTd|MUC3M{c,W0GQR1XSQE9iRg>?
L-428 NVTwfIZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJcohq[mm2aX;uJI9nKGi3bXHuJGwuPDJ6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC1OVQvPzhizszNMi=> MnvFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVc{OTB5Lze+V2FPT0WUPD;hQi=>
C3A Mm[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrSTY5pcWKrdHnvckBw\iCqdX3hckBEO0FiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OCB;IEW2N{44QCEQvF2u NEjZe3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2PzNzMEevK|5USU6JRWK8M4E,

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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.

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.

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-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.

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.

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.

17040210 28415756 25395420
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 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 )

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* 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):
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    C4=C3/X C4: LOG(C4):
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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:

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.

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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