PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 32240651-0 2020 PAK1 inhibitor IPA-3 mitigates metastatic prostate cancer-induced bone remodeling. 1-isopropyldiazen-1-ium-1,2-diolate 15-20 p21 (RAC1) activated kinase 1 Homo sapiens 0-4 33495806-9 2021 A Cell Counting Kit-8 assay showed that PAK1 inhibition following treatment of HCFs with 5 microM IPA-3 or PAK1-shRNA, significantly attenuated AngII-induced proliferation of fibroblasts. 1-isopropyldiazen-1-ium-1,2-diolate 98-103 p21 (RAC1) activated kinase 1 Homo sapiens 40-44 25956913-5 2015 Finally, we disrupted the signaling network downstream of KRAS by blocking KRAS/PAK1/Crk axis with PAK1 inhibitors (i.e., IPA-3, FRAX597 or FRAX1036) along with partial inhibition of all other KRAS effectors by prenylation inhibitors (FTI + GGTI) and examined the motility, morphology and proliferation of the NSCLC cells. 1-isopropyldiazen-1-ium-1,2-diolate 122-127 p21 (RAC1) activated kinase 1 Homo sapiens 80-84 31614827-7 2019 PAK1 was inhibited by small-molecule inhibitor IPA-3 (p21-activated kinase inhibitor III), PAK2 was downregulated by specific short hairpin RNA (shRNA), and BCR-ABL1 tyrosine kinase was inhibited by imatinib (IM). 1-isopropyldiazen-1-ium-1,2-diolate 47-52 p21 (RAC1) activated kinase 1 Homo sapiens 0-4 31304555-3 2019 A small molecule, IPA-3, which inhibits p21-activated kinase 1 (PAK1), has shown therapeutic potential in various types of malignancies. 1-isopropyldiazen-1-ium-1,2-diolate 18-23 p21 (RAC1) activated kinase 1 Homo sapiens 40-62 31304555-3 2019 A small molecule, IPA-3, which inhibits p21-activated kinase 1 (PAK1), has shown therapeutic potential in various types of malignancies. 1-isopropyldiazen-1-ium-1,2-diolate 18-23 p21 (RAC1) activated kinase 1 Homo sapiens 64-68 31516713-10 2019 PAK-1 inhibition increased the cytotoxicity of IPA-3, and the cytotoxicity of SSL-IPA-3 to levels comparable to that of free drug. 1-isopropyldiazen-1-ium-1,2-diolate 47-52 p21 (RAC1) activated kinase 1 Homo sapiens 0-5 31516713-11 2019 These data demonstrate that both pharmacological and molecular inhibition of PAK-1 decreased growth in prostate, breast, and melanoma cancer cell lines, and increased the toxicity of IPA-3 and its liposomal formulation. 1-isopropyldiazen-1-ium-1,2-diolate 183-188 p21 (RAC1) activated kinase 1 Homo sapiens 77-82 31516713-12 2019 These data also show the specificity of IPA-3 for PAK-1, are some of the first data suggesting that IPA-3 is a therapeutic treatment for breast cancer and melanoma, and demonstrate the efficacy of liposome-encapsulated IPA-3 in breast cancer cells. 1-isopropyldiazen-1-ium-1,2-diolate 40-45 p21 (RAC1) activated kinase 1 Homo sapiens 50-55 28972183-8 2017 Importantly, all of these associations were ablated by the PAK inhibitor IPA3, suggesting that PAK1 activation lies upstream of these actin-polymerizing complexes. 1-isopropyldiazen-1-ium-1,2-diolate 73-77 p21 (RAC1) activated kinase 1 Homo sapiens 59-62 28972183-8 2017 Importantly, all of these associations were ablated by the PAK inhibitor IPA3, suggesting that PAK1 activation lies upstream of these actin-polymerizing complexes. 1-isopropyldiazen-1-ium-1,2-diolate 73-77 p21 (RAC1) activated kinase 1 Homo sapiens 95-99 26255026-9 2015 Moreover, p38 activation, filopodia formation and cell migration were significantly reduced by blocking the PAK1 activity with its pharmacological inhibitor, IPA-3. 1-isopropyldiazen-1-ium-1,2-diolate 158-163 p21 (RAC1) activated kinase 1 Homo sapiens 108-112 26379399-6 2015 IPA-3 was used as a specific small molecule inhibitor of p21-activated protein kinase 1 (Pak1) to target Pak1 signaling. 1-isopropyldiazen-1-ium-1,2-diolate 0-5 p21 (RAC1) activated kinase 1 Homo sapiens 57-87 26379399-6 2015 IPA-3 was used as a specific small molecule inhibitor of p21-activated protein kinase 1 (Pak1) to target Pak1 signaling. 1-isopropyldiazen-1-ium-1,2-diolate 0-5 p21 (RAC1) activated kinase 1 Homo sapiens 89-93 26379399-6 2015 IPA-3 was used as a specific small molecule inhibitor of p21-activated protein kinase 1 (Pak1) to target Pak1 signaling. 1-isopropyldiazen-1-ium-1,2-diolate 0-5 p21 (RAC1) activated kinase 1 Homo sapiens 105-109 25956913-5 2015 Finally, we disrupted the signaling network downstream of KRAS by blocking KRAS/PAK1/Crk axis with PAK1 inhibitors (i.e., IPA-3, FRAX597 or FRAX1036) along with partial inhibition of all other KRAS effectors by prenylation inhibitors (FTI + GGTI) and examined the motility, morphology and proliferation of the NSCLC cells. 1-isopropyldiazen-1-ium-1,2-diolate 122-127 p21 (RAC1) activated kinase 1 Homo sapiens 99-103 23246867-3 2013 Similar to MIN6 beta cells, human islets elicited glucose-stimulated PAK1 activation that was sensitive to the PAK1 inhibitor, IPA3. 1-isopropyldiazen-1-ium-1,2-diolate 127-131 p21 (RAC1) activated kinase 1 Homo sapiens 69-73 24844382-9 2014 Interestingly, IPA-3, an inhibitor of serine/threonine kinase p21-activated kinase (PAK1), an important protein of macropinocytosis, directly inhibited SubAB-mediated BiP cleavage and SubAB internalization. 1-isopropyldiazen-1-ium-1,2-diolate 15-20 p21 (RAC1) activated kinase 1 Homo sapiens 84-88 25174975-6 2014 To study the viability/apoptotic effects of combining the PAK1 inhibitor IPA-3 and TQ, crystal violet assay and AnnexinV/PI staining were employed. 1-isopropyldiazen-1-ium-1,2-diolate 73-78 p21 (RAC1) activated kinase 1 Homo sapiens 58-62 23894351-0 2013 IPA-3 inhibits the growth of liver cancer cells by suppressing PAK1 and NF-kappaB activation. 1-isopropyldiazen-1-ium-1,2-diolate 0-5 p21 (RAC1) activated kinase 1 Homo sapiens 63-67 23894351-4 2013 Consistent with other reports, inhibition of PAK1 activity was observed in several human HCC cell lines treated with various dosages of IPA-3. 1-isopropyldiazen-1-ium-1,2-diolate 136-141 p21 (RAC1) activated kinase 1 Homo sapiens 45-49 23246867-3 2013 Similar to MIN6 beta cells, human islets elicited glucose-stimulated PAK1 activation that was sensitive to the PAK1 inhibitor, IPA3. 1-isopropyldiazen-1-ium-1,2-diolate 127-131 p21 (RAC1) activated kinase 1 Homo sapiens 111-115 23246867-7 2013 Both IPA3 and a selective inhibitor of the Cdc42 GTPase, ML-141, blunted the glucose-stimulated activation of Raf-1, suggesting Raf-1 to be downstream of Cdc42 PAK1. 1-isopropyldiazen-1-ium-1,2-diolate 5-9 p21 (RAC1) activated kinase 1 Homo sapiens 160-164 23246867-8 2013 IPA3 also inhibited MEK1/2 activation, implicating the MEK1/2 ERK1/2 cascade to occur downstream of PAK1. 1-isopropyldiazen-1-ium-1,2-diolate 0-4 p21 (RAC1) activated kinase 1 Homo sapiens 100-104 25034104-6 2013 Allosteric inhibitors, such as IPA-3, leverage the unique Group I PAK autoregulatory domain for selective inhibition, and this approach might provide an outlet to evade the kinase selectivity challenges observed with ATP-competitive PAK inhibitors. 1-isopropyldiazen-1-ium-1,2-diolate 31-36 p21 (RAC1) activated kinase 1 Homo sapiens 66-69 23361053-10 2013 IPA-3, a specific small MW PAK1 inhibitor, sensitised cells to tamoxifen only when EBP1 was ectopically expressed. 1-isopropyldiazen-1-ium-1,2-diolate 0-5 p21 (RAC1) activated kinase 1 Homo sapiens 27-31 23153508-7 2013 Furthermore, beta-catenin and Snail nuclear translocation were triggered by Rac1/PAK1 axis, which were both markedly reversed via Rac1 gene knockdown or pretreatment of IPA-3, a PAK1 inhibitor. 1-isopropyldiazen-1-ium-1,2-diolate 169-174 p21 (RAC1) activated kinase 1 Homo sapiens 81-85 23153508-7 2013 Furthermore, beta-catenin and Snail nuclear translocation were triggered by Rac1/PAK1 axis, which were both markedly reversed via Rac1 gene knockdown or pretreatment of IPA-3, a PAK1 inhibitor. 1-isopropyldiazen-1-ium-1,2-diolate 169-174 p21 (RAC1) activated kinase 1 Homo sapiens 178-182 21969371-5 2011 Reiteration of this specific defect by human islets treated with the PAK1 signaling inhibitor IPA3 revealed PAK1 signaling to be of primary functional importance. 1-isopropyldiazen-1-ium-1,2-diolate 94-98 p21 (RAC1) activated kinase 1 Homo sapiens 69-73 22869096-0 2012 The response to PAK1 inhibitor IPA3 distinguishes between cancer cells with mutations in BRAF and Ras oncogenes. 1-isopropyldiazen-1-ium-1,2-diolate 31-35 p21 (RAC1) activated kinase 1 Homo sapiens 16-20 22869096-3 2012 IPA3 has been originally identified as a small molecule inhibitor of p21-activated protein kinase 1 (PAK1), a candidate therapeutic target in human malignancies. 1-isopropyldiazen-1-ium-1,2-diolate 0-4 p21 (RAC1) activated kinase 1 Homo sapiens 69-99 22869096-3 2012 IPA3 has been originally identified as a small molecule inhibitor of p21-activated protein kinase 1 (PAK1), a candidate therapeutic target in human malignancies. 1-isopropyldiazen-1-ium-1,2-diolate 0-4 p21 (RAC1) activated kinase 1 Homo sapiens 101-105 22869096-8 2012 Although it remains to be proven that all the effects of IPA3 are exclusively due to inhibition of PAK1, our findings point to the existence of selective vulnerabilities, which are associated with Ras mutations and could be useful for better understanding and treatment of a large subset of tumors. 1-isopropyldiazen-1-ium-1,2-diolate 57-61 p21 (RAC1) activated kinase 1 Homo sapiens 99-103 22369945-6 2012 Furthermore, the Wnt3a-stimulated S663 phosphorylation was inhibited by the PAK1-specific inhibitor, IPA-3, but not by H-89 or LY294002. 1-isopropyldiazen-1-ium-1,2-diolate 101-106 p21 (RAC1) activated kinase 1 Homo sapiens 76-80 21969371-5 2011 Reiteration of this specific defect by human islets treated with the PAK1 signaling inhibitor IPA3 revealed PAK1 signaling to be of primary functional importance. 1-isopropyldiazen-1-ium-1,2-diolate 94-98 p21 (RAC1) activated kinase 1 Homo sapiens 108-112 19723886-5 2009 We show that IPA-3 binds covalently to the Pak1 regulatory domain and prevents binding to the upstream activator Cdc42. 1-isopropyldiazen-1-ium-1,2-diolate 13-18 p21 (RAC1) activated kinase 1 Homo sapiens 43-47 22096607-11 2011 Moreover, BAD phosphorylation at S111 was observed in several other cell lines, and treating one of them with the Pak1 inhibitor 2,2"-Dihydroxy-1,1"-dinaphthyldisulfide (IPA-3) reduced phosphorylation primarily at S112 and to a smaller extent at S111, while Raf inhibitors only reduced phosphorylation at S112. 1-isopropyldiazen-1-ium-1,2-diolate 170-175 p21 (RAC1) activated kinase 1 Homo sapiens 114-118 34403739-9 2021 Moreover, the formation of TNT-like conduits was inhibited by preventing PAK1-dependent internalization of oAbeta using the small-molecule inhibitor IPA-3, a highly selective cell-permeable auto-regulatory inhibitor of PAK1. 1-isopropyldiazen-1-ium-1,2-diolate 149-154 p21 (RAC1) activated kinase 1 Homo sapiens 73-77 18420139-5 2008 Remarkably, preactivated Pak1 is resistant to IPA-3. 1-isopropyldiazen-1-ium-1,2-diolate 46-51 p21 (RAC1) activated kinase 1 Homo sapiens 25-29 34403739-9 2021 Moreover, the formation of TNT-like conduits was inhibited by preventing PAK1-dependent internalization of oAbeta using the small-molecule inhibitor IPA-3, a highly selective cell-permeable auto-regulatory inhibitor of PAK1. 1-isopropyldiazen-1-ium-1,2-diolate 149-154 p21 (RAC1) activated kinase 1 Homo sapiens 219-223