Haspin inhibitor
WebApr 16, 2024 · Haspin inhibitor potentiates the efficacy of AURKB inhibitor but not AURKA inhibitor. VX-680 inhibits AURKA, AURKB, and AURKC. To gain insights into the specificity of synergistic effect between ... WebAug 25, 2024 · Methods: Anti-tumor activities of the haspin inhibitor CHR-6494 were tested in a number of melanoma cell lines either as a single agent or in combination with the MEK inhibitor Trametinib (GSK1120242). Experiments are based on: 1) Cell viability determined by the crystal violet staining assay; 2) apoptotic responses measured by the caspase 3/7 ...
Haspin inhibitor
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WebAug 30, 2024 · Haspin is required for chromosomal stability; hence, treatment with the haspin inhibitor CHR-6494 has been identified to induce apoptosis in cancer cells by inducing genomic instability (Quadri et al., 2024). Our data suggest that prolonged nuclear accumulation of fascin in response to haspin inhibition may also contribute to these … WebNational Center for Biotechnology Information
WebAug 1, 2011 · From the cellular standpoint, the identified small-molecule Haspin inhibitor causes arrest in G2/M and subsequently apoptosis. … WebFunction and inhibition of Haspin kinase: targeting multiple cancer therapies by antimitosis Here our perspective includes a comprehensive review of the roles and structure of …
WebSep 14, 2024 · We investigated the synergistic effect of a combination of mTOR and HASPIN inhibitors on cell viability, cell cycle, cell apoptosis, DNA damage, and mitotic … WebHASPIN kinase inhibitors were recently isolated, and their antitumor activity reported. Colorectal cancer occurs with high incidence worldwide. In this study, we examined whether HASPIN inhibitor CHR-6494 suppresses cancer progression in Apc Min/+ mice, a familial colon tumor disease model. Mice were treated by intraperitoneal injection of CHR ...
WebJan 14, 2024 · Here, we have examined the effects of 5-Iodotubercidin (5-ITu), a commonly used Haspin inhibitor, on self-renewal and differentiation of mouse embryonic stem cells (ESCs). Treatment with low...
WebOct 1, 2024 · However, no inhibitors targeting haspin have entered clinical trials presently. 5-iTU (5-iodotubercidin) is a useful and classical chemical probe for the investigation of haspin activity, but its ... the art towerWebMar 1, 2012 · Haspin inhibitors identified by radiometric, thermal stability shift and TR-FRET HTS assays. A crystal structure of haspin bound to AMP was used for docking calculation. 7, 14 Analysis of this structure revealed key hydrogen bonds between nitrogen atoms of the adenine ring of AMP and protein backbone atoms of residues E606 and … the art tribeWebJun 8, 2010 · GPP78 is a potent Nampt inhibitor. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells. GPP78 has anti-cancer and anti-tumor activity. ... LDN-192960 is a Dual Haspin and DYRK2 Inhibitor. 2024-10-02. JTE-013 is a Specific S1P2 Antagonist in Neuroblastoma. 2024-10-25. Categories. Others. Neuroblastoma (9) Archives. January … the glenlee whisky reviewWebOct 1, 2024 · Another haspin inhibitor, CX-6258 also impaired proliferation and generated the formation of micronuclei in melanoma cell lines [125]. In some cell lines, co-depletion of either p21 or p53 rescues ... the art triangle movieWebDec 1, 2024 · Haspin is a promising target for the design of inhibitors as potent anticancer drugs for cancer therapy [10], [11]. CHR6494 (3-(1H-indazol-5-yl)-N-propylimidazo[1,2-b]pyridazin-6-amine) is a novel Haspin inhibitor that targets the component of the mitotic machinery other than the microtubule [12]. CHR6494 inhibited cell proliferation and ... thearttrotter.comWebJun 15, 2024 · Abstract. HASPIN, a mitotic kinase to phosphorylate Histone H3 at centromere, has been studied as a promising target for anti-cancer therapy. However, as HASPIN belongs to atypical kinase, lacking the Asp-Phe-Gly (DFG) motif, development from the chemical library of kinase inhibitors with conventional pharmacophore, would be … the art tutorWebJan 13, 2014 · We first examined the effect of Plk1 inhibitors on Haspin in mitotic cells. HeLa Tet-On cells expressing low levels of myc-Haspin in the absence of doxycycline induction [ 2 ] were arrested in mitosis with nocodazole, and then treated with kinase inhibitors for 1 h (in the presence of MG132 to prevent mitotic exit). the glen lewisville