aurora kinase inhibitor-2

Aurora kinase inhibitor-2 (IUN-70219) 是一种可渗透细胞的苯胺喹唑啉，可抑制极光激酶的活性，对Aurora A 和Aurora B 的IC50分别为 390 nM 和 240 nM。

Palmatine chloride 是口服具有活力的不可逆 IDO-1抑制剂。它能够减轻结肠损伤，预防肠道菌群失调和调节色氨酸分解代谢，并改善 DSS 诱发的结肠炎。

Alisertib (MLN 8237) 是一种 Aurora A 激酶抑制剂 (IC50=1.2 nM)，具有口服活性和选择性。Alisertib 具有抗肿瘤活性，可以诱导细胞凋亡和自噬，诱导细胞周期阻滞。

XL228 是一种多靶点酪氨酸激酶抑制剂，对 Bcr-Abl、Aurora A、IGF-1R、Src 和 Lyn 的 IC50 分别为 5、3.1、1.6、6.1和 2 nM。

Aurora kinase inhibitor-13 (Compound 2) 是一种极光激酶抑制剂，其对极光激酶A的IC50值为2.3 μM。

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), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.

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(替恩戈替尼)是一种多激酶抑制剂，靶向一系列参与癌细胞增殖，血管生成和免疫反应调节的激酶，包括Aurora激酶A B、Janus激酶（JAK1 2）、成纤维细胞生长因子受体（FGFR1 2 3）、血管内皮生长因子受体（VEGFRs）等多种激酶，在多种晚期实体瘤的临床试验中显示出良好的耐受性和初步疗效。

JH295 hydrate 通过 Cys22 烷基化从而抑制细胞Nek2，它是有效的，不可逆和选择性的NIMA 相关激酶 2 (Nek2)抑制剂 (IC50 = 770 nM)。JH295 hydrate 对有丝分裂激酶 Cdk1，Aurora B 或 Plk1 不具有活性，不干扰双极纺锤体组件或纺锤体组件检查点。

GSK-1070916 (GSK-1070916A) 是一种选择性，ATP 竞争型的极光激酶B C 抑制剂，Ki 值分别为0.38和1.5 nM。

Aurora A inhibitor 2 (Compound 16h) 是一个 Aurora A kinase 的有效抑制剂 (IC50: 21.94 nM)。Aurora A inhibitor 2 能诱导 MDA-MB-231 细胞中的 caspase 依赖性凋亡。

AKI603 是一种极光激酶 A 抑制剂，IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性，可用于克服白血病中 BCR-ABL-T315I 耐药性突变。

CCT129202 是一种 ATP 竞争性泛极光激酶抑制剂，作用于 Aurora A、Aurora B 和 Aurora C，IC50 分别为 0.042 μM、0.198 μM 和 0.227 μM。

Tripolin A 是一种特异性的非 ATP 竞争性 Aurora A 激酶抑制剂，对Aurora A 和Aurora B 的IC50分别为1.5 μM 和7 μM。