aurora kinase inhibitor-2

Aurora kinase inhibitor-2 (IUN-70219) is a cell-permeable anilinoquinazoline that inhibit the activity of Aurora A (IC50 = 0.39 M).

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).

Aurora kinase inhibitor-13 (Compound 2) is an inhibitor of Aurora kinase, with an IC50 value of 2.3 μM for Aurora kinase A.

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007)

Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 μM), specifically inhibiting it in a dose-dependent manner while exhibiting minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. At 40 μM, Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells and prevents the assembly of a contractile ring during cell division in Drosophila S2 cells, but it does not affect ring ingression, indicating that Aurora B kinase activity is not required for that process.

CD532 hydrochloride is a potent inhibitor of Aurora A kinase, having an IC50 of 45 nM. It not only blocks the activity of Aurora A kinase but also facilitates the degradation of the protein MYCN. Furthermore, CD532 hydrochloride interacts directly with AURKA, inducing a significant conformational change. Its utility in cancer research has been demonstrated [1][2].

JH295 is a highly potent and selective inhibitor of NIMA-related kinase 2 (Nek2), exhibiting irreversible inhibition activity with an IC 50 value of 770 nM. This compound effectively inhibits cellular Nek2 using the alkylation of Cys22. Importantly, JH295 does not exhibit any inhibitory effects toward Cdk1, Aurora B, or Plk1, which are kinases involved in mitotic processes. Furthermore, JH295 has no impact on bipolar spindle assembly or the spindle assembly checkpoint mechanism.

Tinengotinib is a multikinase inhibitor targeting a series of kinases involved in cancer cell proliferation, angiogenesis, and regulation of immune response, including Aurora kinase A B, Janus kinase (JAK1 2), fibroblast growth factor receptor (FGFR1 2 3), vascular endothelial growth factor receptors (VEGFRs), and other tyrosine kinases. Tinengotinib has shown good tolerability and preliminary efficacy in clinical trials in a variety of advanced solid tumors.

JH295 hydrate is a potent, irreversible, and selective NIMA-related kinase 2 (Nek2) inhibitor that inhibits cellular Nek2 by Cys22 alkylation (IC50 = 770 nM). JH295 hydrate is not active against the mitotic kinases Cdk1, Aurora B, or Plk1, and does not interfere with bipolar spindle assembly or the spindle assembly checkpoint [1].

GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B C with IC50 of 3.5 nM 6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.

Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM.

AKI603 is a novel small molecule inhibitor of Aurora kinase A (AurA)(IC50 = 12.3 nM). AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells[1][2].