aurora-in-1

Zatosetron is a serotonin antagonists.

FAK-IN-22 (Compound 26) 是FAK、JAK3和Aurora B的抑制剂，其IC50值分别为50.94 nM、9.99 nM和0.49 nM，有效抑制胰腺导管腺癌 (PDAC) 的肿瘤发生和转移。FAK-IN-22 抑制 PANC-1 细胞的增殖，IC50值为0.15 μM，并通过抑制FAK PI3K Akt信号通路，在 PANC-1 细胞中诱导凋亡和 G2 M 期阻滞。

Aurora-A ligand 1 是一种高亲和力且特异性的Aurora-A抑制剂，其解离常数 (Kd) 为0.85 nM。作为靶蛋白配体 (PROTAC靶蛋白配体)，Aurora-A ligand 1 可用于开发具有抗肿瘤活性的PROTACAurora-A降解剂，并可用于合成HLB-0532259。HLB-0532259 对神经母细胞瘤具有抗肿瘤活性。

BET Aurora kinase-IN-1 (Compound 38) 是一种双效BET Aurora kinase抑制剂。其对多种肿瘤细胞系展现抗增殖活性，并在肾细胞癌和结肠癌的异种移植模型中表现出显著的抗肿瘤效果，肿瘤生长抑制 (TGI) 分别达到45.99%和53.06%。

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)

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].

Aurora LIM kinase-IN-1 (Compound F114) 是aurora 和lim 激酶的有效双重抑制剂。Aurora LIM kinase-IN-1 可抑制胶质母细胞瘤的增殖和侵袭，可能用于胶质母细胞瘤和其他癌症相关的药物研发。Aurora 和 LIM 激酶是分别参与肿瘤细胞分裂和细胞运动的激酶。

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. In addition to targeting SYK, GSK2646264 also inhibits several other kinases, including LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B, and Aurora A, with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3, respectively. Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

Aurora A PKC-IN-1 (Compound 2e) 是一种有效的 Aurora A (AurA) 和 PKC (α, β1, β2, θ) 双重抑制剂，作用于 AurA (IC50: 6.9 nM) 和 PKCα (IC50: 16.9 nM)。Aurora A PKC-IN-1 对乳腺癌细胞表现出抗增殖和抗转移作用。

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。

SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A); 1 nM (Aurora B incenp); 3 nM (Aurora C incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expression. It induced significant modulation of Aurora A and Aurora B biomarkers (p-Aurora A and pHH3, respectively) and cell polyploidy, as expected from Aurora A B inhibitors.

XMD-12, also known as DUN57447, Aurora inhibitor (compound 1) or Aurora-IN-1, is an Auroro inhibitor, which targets Aurora A B C. (5.6 18.4 24.6 nM).

Aurora kinase-IN-1 是aurora kinase 的有效抑制剂。Aurora kinase-IN-1 上调 G1 细胞周期抑制蛋白 (包括 p21 和 p27) 以及 G1 进行性细胞周期蛋白 D1 的表达，并下调 G1-to-S 进行性细胞周期蛋白，导致细胞周期停滞在 G1 S 边界。Aurora 激酶-IN-1 还诱导细胞凋亡 (apoptosis）。Aurora 激酶-IN-1 是化疗药物的先导化合物。

JB170 是一种强效且高度特异性的PROTAC 介导的AURORA-A 降解剂 (DC50=28 nM)，通过将 Alisertib 连接至Cereblon 配体 Thalidomide 而形成。JB170 优先结合 AURORA-A (EC50=193 nM) 而不是 AURORA-B (EC50=1.4µM)。JB170 介导的 S 期阻滞是由 AURORA-A 耗竭引起的。JB170 对 AURORA-A 激酶的非催化功能具有很好的抑制能力。

Aurora Kinases-IN-4（Compound 11c）是共价ATP竞争型aurora kinaseA抑制剂，具有IC50为1.7 nM。该化合物对SJSA-1、MDA-MB-231、A549和HeLa细胞系的增殖抑制效果显著，其IC50分别为4.27、1.54、3.08和6.99 μM。Aurora Kinases-IN-4适用于三阴性乳腺癌（TNBC）的相关研究。

GRK2 Inhibitor 2 (Compound 8h) 作为一种高效的抑制剂，对GRK2有显著的抑制活性（IC50: 19 nM），同样对Aurora-A也表现出抑制作用（IC50: 137 nM）。该化合物能增强GRK2过表达的HEK293细胞中β-AR介导的cAMP积累。此外，GRK2 Inhibitor 2适用于充血性心力衰竭（HF）的相关研究。

FAK aurora Kinase-IN-1，作为FAK与极光激酶抑制剂，其IC50为6.61 nM和0.91 nM，分别针对FAK和极光激酶。此化合物显示了其抗癌潜力（WO2018019252A1; compound 11）。

AURKA against 1(compound Ac13) 作为针对Aurora激酶(AURKA)的抑制剂，其IC50值低于0.5 nM，专门靶向K162位点的内源性赖氨酸乙酰化，并展示了阻断肿瘤细胞增殖的能力。在HCT116细胞中转染了SIRT3后，AURKA against 1诱导的K162位点乙酰化的AURKA激酶活性能够被逆转。