PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 32637030-0 2020 RSK inhibitor BI-D1870 inhibits acute myeloid leukemia cell proliferation by targeting mitotic exit. BI D1870 14-22 ribosomal protein S6 kinase A2 Homo sapiens 0-3 19765648-8 2009 While BI-D1870 partially inhibited insulin-stimulated PKB activation in these cells, this only partially inhibited AS160 phosphorylation and did not block GLUT4 trafficking, suggesting that p90RSK might regulate glucose transport after GLUT4 translocation. BI D1870 6-14 insulin Homo sapiens 35-42 19332537-6 2009 RSK-dependent Ser-260 phosphorylation was sensitive to the MEK inhibitor UO126 and the RSK inhibitor BID-1870. BI D1870 101-109 ribosomal protein S6 kinase A2 Homo sapiens 0-3 19332537-6 2009 RSK-dependent Ser-260 phosphorylation was sensitive to the MEK inhibitor UO126 and the RSK inhibitor BID-1870. BI D1870 101-109 ribosomal protein S6 kinase A2 Homo sapiens 87-90 17617058-8 2007 In cells, the IGF-1-stimulated phosphorylations, and certain EGF-stimulated phosphorylations, were inhibited by PI3K (phosphoinositide 3-kinase) inhibitors, whereas the RSK inhibitor BI-D1870 inhibited the PMA-induced phosphorylations. BI D1870 183-191 insulin like growth factor 1 Homo sapiens 14-19 17617058-8 2007 In cells, the IGF-1-stimulated phosphorylations, and certain EGF-stimulated phosphorylations, were inhibited by PI3K (phosphoinositide 3-kinase) inhibitors, whereas the RSK inhibitor BI-D1870 inhibited the PMA-induced phosphorylations. BI D1870 183-191 epidermal growth factor Homo sapiens 61-64 17040210-0 2007 BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. BI D1870 0-8 ribosomal protein S6 kinase A1 Homo sapiens 40-47 17040210-0 2007 BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. BI D1870 0-8 ribosomal protein S6 kinase A1 Homo sapiens 49-68 34602526-4 2021 BI-D1870, a potent inhibitor of RSK, significantly suppressed the proliferation of AML cell lines, among which three encoded wild-type FLT3 and three contained FLT3 driver mutations, compared with chronic myeloid leukemia K562 cells or other adherent cancer cells. BI D1870 0-8 ribosomal protein S6 kinase A2 Homo sapiens 32-35 34602526-4 2021 BI-D1870, a potent inhibitor of RSK, significantly suppressed the proliferation of AML cell lines, among which three encoded wild-type FLT3 and three contained FLT3 driver mutations, compared with chronic myeloid leukemia K562 cells or other adherent cancer cells. BI D1870 0-8 fms related receptor tyrosine kinase 3 Homo sapiens 135-139 34602526-4 2021 BI-D1870, a potent inhibitor of RSK, significantly suppressed the proliferation of AML cell lines, among which three encoded wild-type FLT3 and three contained FLT3 driver mutations, compared with chronic myeloid leukemia K562 cells or other adherent cancer cells. BI D1870 0-8 fms related receptor tyrosine kinase 3 Homo sapiens 160-164 34602526-10 2021 The findings suggested that BI-D1870 alone exerts an adequate antiproliferative effect on AML with or without FLT3 mutations and serves as a novel AML therapeutic agent. BI D1870 28-36 fms related receptor tyrosine kinase 3 Homo sapiens 110-114 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 paired box 5 Homo sapiens 281-285 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 CD19 molecule Homo sapiens 357-361 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 CD79b molecule Homo sapiens 363-368 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 B cell linker Homo sapiens 374-378 32420699-7 2020 In addition, we found favorable combinatory growth inhibitory effects of BI-D1870 with inhibitors of BTK (ibrutinib), AKT (ipatasertib), and BCL2 (venetoclax) in cell characteristic-dependent manners. BI D1870 73-81 Bruton tyrosine kinase Homo sapiens 101-104 32420699-7 2020 In addition, we found favorable combinatory growth inhibitory effects of BI-D1870 with inhibitors of BTK (ibrutinib), AKT (ipatasertib), and BCL2 (venetoclax) in cell characteristic-dependent manners. BI D1870 73-81 AKT serine/threonine kinase 1 Homo sapiens 118-121 32420699-7 2020 In addition, we found favorable combinatory growth inhibitory effects of BI-D1870 with inhibitors of BTK (ibrutinib), AKT (ipatasertib), and BCL2 (venetoclax) in cell characteristic-dependent manners. BI D1870 73-81 BCL2 apoptosis regulator Homo sapiens 141-145 34089554-12 2021 BI-D1870, a specific RSK inhibitor, partly prevented PTTH-stimulated RSK phosphorylation and significantly inhibited PTTH-stimulated ecdysteroid secretion, indicating that PTTH-stimulated RSK phosphorylation is involved in ecdysteroidogenesis. BI D1870 0-8 prothoracicotropic hormone Bombyx mori 53-57 34089554-12 2021 BI-D1870, a specific RSK inhibitor, partly prevented PTTH-stimulated RSK phosphorylation and significantly inhibited PTTH-stimulated ecdysteroid secretion, indicating that PTTH-stimulated RSK phosphorylation is involved in ecdysteroidogenesis. BI D1870 0-8 prothoracicotropic hormone Bombyx mori 117-121 34089554-12 2021 BI-D1870, a specific RSK inhibitor, partly prevented PTTH-stimulated RSK phosphorylation and significantly inhibited PTTH-stimulated ecdysteroid secretion, indicating that PTTH-stimulated RSK phosphorylation is involved in ecdysteroidogenesis. BI D1870 0-8 prothoracicotropic hormone Bombyx mori 172-176 35328342-4 2022 The combinatory treatment of BI-D1870, an inhibitor for N-terminal kinase domain (NTKD) of RSK2, and ipatasertib, an inhibitor for AKT, showed the additive to synergistic anti-tumor effect on human MM-derived cell lines (HMCLs) with active RSK2-NTKD and AKT, by enhancing apoptotic induction with BIM and BID activation. BI D1870 29-37 ribosomal protein S6 kinase A3 Homo sapiens 91-95 35328342-4 2022 The combinatory treatment of BI-D1870, an inhibitor for N-terminal kinase domain (NTKD) of RSK2, and ipatasertib, an inhibitor for AKT, showed the additive to synergistic anti-tumor effect on human MM-derived cell lines (HMCLs) with active RSK2-NTKD and AKT, by enhancing apoptotic induction with BIM and BID activation. BI D1870 29-37 ribosomal protein S6 kinase A3 Homo sapiens 240-244 35328342-4 2022 The combinatory treatment of BI-D1870, an inhibitor for N-terminal kinase domain (NTKD) of RSK2, and ipatasertib, an inhibitor for AKT, showed the additive to synergistic anti-tumor effect on human MM-derived cell lines (HMCLs) with active RSK2-NTKD and AKT, by enhancing apoptotic induction with BIM and BID activation. BI D1870 29-37 AKT serine/threonine kinase 1 Homo sapiens 254-257 35328342-4 2022 The combinatory treatment of BI-D1870, an inhibitor for N-terminal kinase domain (NTKD) of RSK2, and ipatasertib, an inhibitor for AKT, showed the additive to synergistic anti-tumor effect on human MM-derived cell lines (HMCLs) with active RSK2-NTKD and AKT, by enhancing apoptotic induction with BIM and BID activation. BI D1870 29-37 BH3 interacting domain death agonist Homo sapiens 305-308 32667058-6 2020 METHODS: Our study examined the effect of cisplatin, BI-D1870 (RSK inhibitor) or their combination on cell migration, apoptosis, autophagy and cell cycle in A549 human lung adenocarcinoma cells. BI D1870 53-61 ribosomal protein S6 kinase A3 Homo sapiens 63-66 32667058-7 2020 RESULTS: The combination of cisplatin and BI-D1870 potentiated the antimigration rate, the activation of caspases-3 and was associated with a significant decrease in RSK1 and ERK expression when compared to cisplatin alone. BI D1870 42-50 ribosomal protein S6 kinase A1 Homo sapiens 166-170 32667058-7 2020 RESULTS: The combination of cisplatin and BI-D1870 potentiated the antimigration rate, the activation of caspases-3 and was associated with a significant decrease in RSK1 and ERK expression when compared to cisplatin alone. BI D1870 42-50 mitogen-activated protein kinase 1 Homo sapiens 175-178 32420699-3 2020 BI-D1870, an inhibitor specific to RSK2-NTKD, caused RSK2Ser227 dephosphorylation, and thereby, induced dose-dependent growth inhibition via G2 /M cell cycle blockade and apoptosis in four of the five cell lines, while one cell line showed only modest sensitivity. BI D1870 0-8 ribosomal protein S6 kinase A3 Homo sapiens 35-39 32420699-4 2020 In addition, RSK2 gene knockdown caused growth inhibition in the four BI-D1870-sensitive cell lines. BI D1870 70-78 ribosomal protein S6 kinase A3 Homo sapiens 13-17 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 ribosomal protein S6 kinase A3 Homo sapiens 94-98 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 MYC proto-oncogene, bHLH transcription factor Homo sapiens 163-166 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 MYB proto-oncogene, transcription factor Homo sapiens 171-174 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 BCL2 apoptosis regulator Homo sapiens 206-210 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 BCL2 like 1 Homo sapiens 215-221 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 IKAROS family zinc finger 1 Homo sapiens 263-268 32420699-5 2020 Comparative gene expression profiling of the MCL-derived cell lines showed that inhibition of RSK2Ser227 by BI-D1870 caused downregulation of oncogenes, such as c-MYC and MYB; anti-apoptosis genes, such as BCL2 and BCL2L1; genes for B cell development, including IKZF1, IKZF3, and PAX5; and genes constituting the B cell receptor signaling pathway, such as CD19, CD79B, and BLNK. BI D1870 108-116 IKAROS family zinc finger 3 Homo sapiens 270-275 32637030-3 2020 To examine the role of RSK in AML, we analyzed apoptosis and the cell cycle profile following treatment with BI-D1870, a potent inhibitor of RSK. BI D1870 109-117 ribosomal protein S6 kinase A2 Homo sapiens 141-144 32637030-6 2020 BI-D1870 treatment impeded the association of activator CDC20 with APC/C, but increased binding of inhibitor MAD2 to CDC20, preventing mitotic exit. BI D1870 0-8 cell division cycle 20 Homo sapiens 56-61 32637030-6 2020 BI-D1870 treatment impeded the association of activator CDC20 with APC/C, but increased binding of inhibitor MAD2 to CDC20, preventing mitotic exit. BI D1870 0-8 mitotic arrest deficient 2 like 1 Homo sapiens 109-113 32637030-6 2020 BI-D1870 treatment impeded the association of activator CDC20 with APC/C, but increased binding of inhibitor MAD2 to CDC20, preventing mitotic exit. BI D1870 0-8 cell division cycle 20 Homo sapiens 117-122 32637030-7 2020 Moreover, the inactivation of spindle assembly checkpoint or MAD2 knockdown released cells from BI-D1870-induced metaphase arrest. BI D1870 96-104 mitotic arrest deficient 2 like 1 Homo sapiens 61-65 24241211-6 2014 In addition, BI-D1870 also induced G2/M arrest by modulating the expression of p21 and other cell cycle regulators. BI D1870 13-21 H3 histone pseudogene 16 Homo sapiens 79-82 27040869-5 2016 The combined use of the S6K inhibitor BI-D1870 with TNF-alpha inhibited the PKC-zeta to p47(phox) interaction, inhibited ROS production, degraded PKC-zeta, and activated caspases-3 and -8 to block transformation from blebbishields. BI D1870 38-46 protein kinase C zeta Homo sapiens 76-84 27040869-5 2016 The combined use of the S6K inhibitor BI-D1870 with TNF-alpha inhibited the PKC-zeta to p47(phox) interaction, inhibited ROS production, degraded PKC-zeta, and activated caspases-3 and -8 to block transformation from blebbishields. BI D1870 38-46 pleckstrin Homo sapiens 88-91 27040869-5 2016 The combined use of the S6K inhibitor BI-D1870 with TNF-alpha inhibited the PKC-zeta to p47(phox) interaction, inhibited ROS production, degraded PKC-zeta, and activated caspases-3 and -8 to block transformation from blebbishields. BI D1870 38-46 protein kinase C zeta Homo sapiens 146-187 26386981-3 2016 The pan-RSK inhibitor BI-D1870 also inhibits TH17 differentiation, but the effect of BI-D1870 in vivo remains unclear. BI D1870 22-30 ribosomal protein S6 kinase polypeptide 1 Mus musculus 8-11 26580203-7 2015 On the other hand, both the EGF-stimulated phosphorylation of T1736 and the EGF-induced dissolution of HDs are dependent on a functional MAPK signaling pathway, and treatment with the RSK inhibitor BI-D1870 prevented EGF-stimulated phosphorylation of beta4-T1736. BI D1870 198-206 mitogen-activated protein kinase 3 Homo sapiens 137-141 26580203-7 2015 On the other hand, both the EGF-stimulated phosphorylation of T1736 and the EGF-induced dissolution of HDs are dependent on a functional MAPK signaling pathway, and treatment with the RSK inhibitor BI-D1870 prevented EGF-stimulated phosphorylation of beta4-T1736. BI D1870 198-206 ribosomal protein S6 kinase A1 Homo sapiens 184-187 26580203-7 2015 On the other hand, both the EGF-stimulated phosphorylation of T1736 and the EGF-induced dissolution of HDs are dependent on a functional MAPK signaling pathway, and treatment with the RSK inhibitor BI-D1870 prevented EGF-stimulated phosphorylation of beta4-T1736. BI D1870 198-206 tubulin beta 3 class III Homo sapiens 251-256 25889895-0 2015 Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner. BI D1870 32-40 ribosomal protein S6 kinase A2 Homo sapiens 16-19 25889895-0 2015 Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner. BI D1870 32-40 CREB regulated transcription coactivator 1 Mus musculus 59-65 25889895-0 2015 Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner. BI D1870 32-40 ribosomal protein S6 kinase A2 Homo sapiens 81-84 25889895-3 2015 BI-D1870 and SL0101 are two widely used inhibitors of RSK. BI D1870 0-8 ribosomal protein S6 kinase A2 Homo sapiens 54-57 25889895-14 2015 We thus conclude that SL0101 and BI-D1870 induce distinct off-target effects in mTORC1-p70S6K signaling, and thus, the functions previously ascribed to RSK based on these inhibitors should be reassessed. BI D1870 33-41 CREB regulated transcription coactivator 1 Mus musculus 80-86 25889895-14 2015 We thus conclude that SL0101 and BI-D1870 induce distinct off-target effects in mTORC1-p70S6K signaling, and thus, the functions previously ascribed to RSK based on these inhibitors should be reassessed. BI D1870 33-41 ribosomal protein S6 kinase B1 Homo sapiens 87-93 25889895-14 2015 We thus conclude that SL0101 and BI-D1870 induce distinct off-target effects in mTORC1-p70S6K signaling, and thus, the functions previously ascribed to RSK based on these inhibitors should be reassessed. BI D1870 33-41 ribosomal protein S6 kinase A2 Homo sapiens 152-155 25579842-5 2015 Nodular melanoma cells were more sensitive to RSK1 inhibition using siRNA and the pharmacological inhibitor BI-D1870 compared with superficial spreading cells. BI D1870 108-116 ribosomal protein S6 kinase A1 Homo sapiens 46-50 24057571-8 2014 Treatment with rapamycin, an mTOR inhibitor, MK2206, an Akt inhibitor, and BI-D1870, a RSK inhibitor, partially suppressed CdCl2-induced ATF4 expression. BI D1870 75-83 ribosomal protein S6 kinase A3 Homo sapiens 87-90 24057571-8 2014 Treatment with rapamycin, an mTOR inhibitor, MK2206, an Akt inhibitor, and BI-D1870, a RSK inhibitor, partially suppressed CdCl2-induced ATF4 expression. BI D1870 75-83 activating transcription factor 4 Homo sapiens 137-141 24241211-2 2014 This study aims to investigate the role of BI-D1870, a specific inhibitor of p90 RSKs, in a panel of OSCC cell lines. BI D1870 43-51 transferrin receptor Homo sapiens 77-80 27080258-7 2016 FSH-stimulated phosphorylation of YB-1(Ser(102)) is prevented by pretreatment of GCs with the PKA-selective inhibitor PKA inhibitor (PKI), the MEK inhibitor PD98059, or the ribosomal S6 kinase-2 (RSK-2) inhibitor BI-D1870. BI D1870 213-221 Y-box binding protein 1 Homo sapiens 34-38 27080258-7 2016 FSH-stimulated phosphorylation of YB-1(Ser(102)) is prevented by pretreatment of GCs with the PKA-selective inhibitor PKA inhibitor (PKI), the MEK inhibitor PD98059, or the ribosomal S6 kinase-2 (RSK-2) inhibitor BI-D1870. BI D1870 213-221 ribosomal protein S6 kinase A3 Homo sapiens 173-194 27049728-7 2016 Similarly, BI-D1870, a specific inhibitor of p90RSK, significantly inhibited the metastatic potential of highly invasive MDA-MB-231 and moderately invasive MDA-MB-468 TNBC cells, but was minimally effective in non-invasive Hs578T TNBC cells. BI D1870 11-19 ribosomal protein S6 kinase A1 Homo sapiens 45-51 25670857-10 2015 The tPA-mediated macrophage survival was eliminated by PD98059, BI-D1870, or sc68376, the specific inhibitors for Erk1/2, p90RSK, or p38, respectively. BI D1870 64-72 plasminogen activator, tissue Mus musculus 4-7 25670857-10 2015 The tPA-mediated macrophage survival was eliminated by PD98059, BI-D1870, or sc68376, the specific inhibitors for Erk1/2, p90RSK, or p38, respectively. BI D1870 64-72 mitogen-activated protein kinase 3 Mus musculus 114-120 25670857-10 2015 The tPA-mediated macrophage survival was eliminated by PD98059, BI-D1870, or sc68376, the specific inhibitors for Erk1/2, p90RSK, or p38, respectively. BI D1870 64-72 ribosomal protein S6 kinase polypeptide 1 Mus musculus 122-128 25670857-10 2015 The tPA-mediated macrophage survival was eliminated by PD98059, BI-D1870, or sc68376, the specific inhibitors for Erk1/2, p90RSK, or p38, respectively. BI D1870 64-72 mitogen-activated protein kinase 14 Mus musculus 133-136 27919044-0 2014 A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. BI D1870 111-119 ribosomal protein S6 kinase polypeptide 1 Mus musculus 97-100 27919044-5 2014 We confirmed that these kinases, including Slk, Lok and Mst1, are inhibited by BI-D1870 but to a much lesser extent by BIX 02565 and that phosphorylation of some of their substrates is blocked by BI-D1870 in living cells. BI D1870 79-87 STE20-like kinase Mus musculus 43-46 27919044-5 2014 We confirmed that these kinases, including Slk, Lok and Mst1, are inhibited by BI-D1870 but to a much lesser extent by BIX 02565 and that phosphorylation of some of their substrates is blocked by BI-D1870 in living cells. BI D1870 79-87 serine/threonine kinase 10 Mus musculus 48-51 27919044-5 2014 We confirmed that these kinases, including Slk, Lok and Mst1, are inhibited by BI-D1870 but to a much lesser extent by BIX 02565 and that phosphorylation of some of their substrates is blocked by BI-D1870 in living cells. BI D1870 79-87 macrophage stimulating 1 (hepatocyte growth factor-like) Mus musculus 56-60 27919044-5 2014 We confirmed that these kinases, including Slk, Lok and Mst1, are inhibited by BI-D1870 but to a much lesser extent by BIX 02565 and that phosphorylation of some of their substrates is blocked by BI-D1870 in living cells. BI D1870 196-204 STE20-like kinase Mus musculus 43-46 27919044-5 2014 We confirmed that these kinases, including Slk, Lok and Mst1, are inhibited by BI-D1870 but to a much lesser extent by BIX 02565 and that phosphorylation of some of their substrates is blocked by BI-D1870 in living cells. BI D1870 196-204 serine/threonine kinase 10 Mus musculus 48-51 27919044-5 2014 We confirmed that these kinases, including Slk, Lok and Mst1, are inhibited by BI-D1870 but to a much lesser extent by BIX 02565 and that phosphorylation of some of their substrates is blocked by BI-D1870 in living cells. BI D1870 196-204 macrophage stimulating 1 (hepatocyte growth factor-like) Mus musculus 56-60 24403857-9 2013 Genetic as well as pharmacological inhibition of RPS6KA2 by the inhibitor BI-D1870 acted synergistically with erlotinib. BI D1870 74-82 ribosomal protein S6 kinase A2 Homo sapiens 49-56 23940083-14 2014 Inhibiting RSK with siRNA or BI-D1870 suppressed growth, induced apoptosis, and sensitized cells to SHH agents. BI D1870 29-37 sonic hedgehog signaling molecule Homo sapiens 100-103 23516539-6 2013 During both Ca(2+)- and agonist (U46619) induced SM contraction, RSK inhibition by the highly selective compound BI-D1870 (which has no effect on MLCK or ROCK) resulted in significant suppression of contractile force. BI D1870 113-121 ribosomal protein S6 kinase A2 Homo sapiens 65-68 24136223-0 2013 The p90 ribosomal S6 kinase (RSK) inhibitor BI-D1870 prevents gamma irradiation-induced apoptosis and mediates senescence via RSK- and p53-independent accumulation of p21WAF1/CIP1. BI D1870 44-52 ribosomal protein S6 kinase A1 Homo sapiens 29-32 24136223-0 2013 The p90 ribosomal S6 kinase (RSK) inhibitor BI-D1870 prevents gamma irradiation-induced apoptosis and mediates senescence via RSK- and p53-independent accumulation of p21WAF1/CIP1. BI D1870 44-52 ribosomal protein S6 kinase A1 Homo sapiens 126-129 24136223-0 2013 The p90 ribosomal S6 kinase (RSK) inhibitor BI-D1870 prevents gamma irradiation-induced apoptosis and mediates senescence via RSK- and p53-independent accumulation of p21WAF1/CIP1. BI D1870 44-52 tumor protein p53 Homo sapiens 135-138 24136223-0 2013 The p90 ribosomal S6 kinase (RSK) inhibitor BI-D1870 prevents gamma irradiation-induced apoptosis and mediates senescence via RSK- and p53-independent accumulation of p21WAF1/CIP1. BI D1870 44-52 cyclin dependent kinase inhibitor 1A Homo sapiens 175-179 24136223-3 2013 Here, we report that BI-D1870, a potent small molecule inhibitor of RSKs, induces apoptosis, although preferentially, in a p21-deficient background. BI D1870 21-29 cyclin dependent kinase inhibitor 1A Homo sapiens 123-126 24136223-5 2013 Although we identified p21 in in vitro kinase assays as a novel RSK substrate that specifically becomes phosphorylated by RSK1-3 at Ser116 and Ser146, RNA-interference, overexpression and co-immunoprecipitation studies as well as the use of SL0101, another specific RSK inhibitor, revealed that BI-D1870 mediates p21 accumulation via a yet unknown pathway that, besides its off-site targets polo-like kinase-1 and AuroraB, also does also not involve RSKs. BI D1870 295-303 cyclin dependent kinase inhibitor 1A Homo sapiens 23-26 24136223-5 2013 Although we identified p21 in in vitro kinase assays as a novel RSK substrate that specifically becomes phosphorylated by RSK1-3 at Ser116 and Ser146, RNA-interference, overexpression and co-immunoprecipitation studies as well as the use of SL0101, another specific RSK inhibitor, revealed that BI-D1870 mediates p21 accumulation via a yet unknown pathway that, besides its off-site targets polo-like kinase-1 and AuroraB, also does also not involve RSKs. BI D1870 295-303 ribosomal protein S6 kinase A1 Homo sapiens 64-67 24136223-5 2013 Although we identified p21 in in vitro kinase assays as a novel RSK substrate that specifically becomes phosphorylated by RSK1-3 at Ser116 and Ser146, RNA-interference, overexpression and co-immunoprecipitation studies as well as the use of SL0101, another specific RSK inhibitor, revealed that BI-D1870 mediates p21 accumulation via a yet unknown pathway that, besides its off-site targets polo-like kinase-1 and AuroraB, also does also not involve RSKs. BI D1870 295-303 ribosomal protein S6 kinase A1 Homo sapiens 122-126 24136223-5 2013 Although we identified p21 in in vitro kinase assays as a novel RSK substrate that specifically becomes phosphorylated by RSK1-3 at Ser116 and Ser146, RNA-interference, overexpression and co-immunoprecipitation studies as well as the use of SL0101, another specific RSK inhibitor, revealed that BI-D1870 mediates p21 accumulation via a yet unknown pathway that, besides its off-site targets polo-like kinase-1 and AuroraB, also does also not involve RSKs. BI D1870 295-303 ribosomal protein S6 kinase A1 Homo sapiens 122-125 23510923-9 2013 Furthermore, BI-D1870, an inhibitor of the p90(RSK)s, protein kinases which are activated by ERK, blocks PE-activated rRNA synthesis, as did a second p90(RSK) inhibitor, SL0101. BI D1870 13-21 transferrin receptor Homo sapiens 43-46 23510923-9 2013 Furthermore, BI-D1870, an inhibitor of the p90(RSK)s, protein kinases which are activated by ERK, blocks PE-activated rRNA synthesis, as did a second p90(RSK) inhibitor, SL0101. BI D1870 13-21 ribosomal protein S6 kinase A2 Homo sapiens 47-50 23510923-9 2013 Furthermore, BI-D1870, an inhibitor of the p90(RSK)s, protein kinases which are activated by ERK, blocks PE-activated rRNA synthesis, as did a second p90(RSK) inhibitor, SL0101. BI D1870 13-21 mitogen-activated protein kinase 1 Homo sapiens 93-96 23510923-9 2013 Furthermore, BI-D1870, an inhibitor of the p90(RSK)s, protein kinases which are activated by ERK, blocks PE-activated rRNA synthesis, as did a second p90(RSK) inhibitor, SL0101. BI D1870 13-21 transferrin receptor Homo sapiens 150-153 23510923-9 2013 Furthermore, BI-D1870, an inhibitor of the p90(RSK)s, protein kinases which are activated by ERK, blocks PE-activated rRNA synthesis, as did a second p90(RSK) inhibitor, SL0101. BI D1870 13-21 ribosomal protein S6 kinase A2 Homo sapiens 154-157 23215897-12 2013 PD184352 or BI-D1870 prevented the increased surface area induced by endothelin-1 in cardiomyocytes. BI D1870 12-20 endothelin 1 Rattus norvegicus 69-81 24303063-6 2013 In addition, MEK inhibitors and the RSK-inhibitor BI-D1870 interfere in mTORC1 activity, suggesting that RSK acts as a bypass for Rheb in activating mTORC1. BI D1870 50-58 ribosomal protein S6 kinase polypeptide 1 Mus musculus 36-39 24303063-6 2013 In addition, MEK inhibitors and the RSK-inhibitor BI-D1870 interfere in mTORC1 activity, suggesting that RSK acts as a bypass for Rheb in activating mTORC1. BI D1870 50-58 CREB regulated transcription coactivator 1 Mus musculus 72-78 24303063-6 2013 In addition, MEK inhibitors and the RSK-inhibitor BI-D1870 interfere in mTORC1 activity, suggesting that RSK acts as a bypass for Rheb in activating mTORC1. BI D1870 50-58 ribosomal protein S6 kinase polypeptide 1 Mus musculus 105-108 24303063-6 2013 In addition, MEK inhibitors and the RSK-inhibitor BI-D1870 interfere in mTORC1 activity, suggesting that RSK acts as a bypass for Rheb in activating mTORC1. BI D1870 50-58 Ras homolog enriched in brain Mus musculus 130-134 24303063-6 2013 In addition, MEK inhibitors and the RSK-inhibitor BI-D1870 interfere in mTORC1 activity, suggesting that RSK acts as a bypass for Rheb in activating mTORC1. BI D1870 50-58 CREB regulated transcription coactivator 1 Mus musculus 149-155 24036112-7 2013 Inhibition of RSK using either the pharmacological inhibitor BI-D1870 or after adenoviral expression of a dominant negative RSK1 mutant (RSK1-DN) showed that RSK selectively phosphorylates IRS-1 on Ser-1101. BI D1870 61-69 ribosomal protein S6 kinase A1 Rattus norvegicus 124-128 24036112-7 2013 Inhibition of RSK using either the pharmacological inhibitor BI-D1870 or after adenoviral expression of a dominant negative RSK1 mutant (RSK1-DN) showed that RSK selectively phosphorylates IRS-1 on Ser-1101. BI D1870 61-69 insulin receptor substrate 1 Rattus norvegicus 189-194 23516539-6 2013 During both Ca(2+)- and agonist (U46619) induced SM contraction, RSK inhibition by the highly selective compound BI-D1870 (which has no effect on MLCK or ROCK) resulted in significant suppression of contractile force. BI D1870 113-121 myosin light chain kinase Homo sapiens 146-150 21344389-8 2011 We found that the MEK inhibitor U0126 and the RSK inhibitor BI-D1870 both reduced IL-1B-dependent MMP-1 gene expression in SW1353 cells. BI D1870 60-68 ribosomal protein S6 kinase A2 Homo sapiens 46-49 22674792-5 2012 Despite enrichment for TICs, these cells were sensitive to RSK inhibition when treated ex vivo with BI-D1870. BI D1870 100-108 ribosomal protein S6 kinase A3 Homo sapiens 59-62 21344389-8 2011 We found that the MEK inhibitor U0126 and the RSK inhibitor BI-D1870 both reduced IL-1B-dependent MMP-1 gene expression in SW1353 cells. BI D1870 60-68 interleukin 1 beta Homo sapiens 82-87 21344389-8 2011 We found that the MEK inhibitor U0126 and the RSK inhibitor BI-D1870 both reduced IL-1B-dependent MMP-1 gene expression in SW1353 cells. BI D1870 60-68 matrix metallopeptidase 1 Homo sapiens 98-103 21501342-6 2011 The RSK inhibitor BI-D1870 suppressed SH3P2 phosphorylation and tumor cell motility as effectively as did the MEK inhibitor PD184352. BI D1870 18-26 ribosomal protein S6 kinase polypeptide 1 Mus musculus 4-7 21501342-6 2011 The RSK inhibitor BI-D1870 suppressed SH3P2 phosphorylation and tumor cell motility as effectively as did the MEK inhibitor PD184352. BI D1870 18-26 osteoclast stimulating factor 1 Mus musculus 38-43