tubulin inhibitor 6

Tubulin inhibitor 6 (iHAP1) 是一种微管蛋白抑制剂，抑制微管蛋白聚合，IC50为 0.87 μM。它抑制多种癌细胞系，抑制 K562 细胞生长，IC50为 840 nM。

BRD9876 是一种 MM1S 生长的选择性抑制剂，可将驱动蛋白 5 锁定在增强微管结合的状态，从而导致 MT 的捆绑和稳定。它特异性靶向微管结合的 Eg5，选择性抑制 CD34 细胞的骨髓瘤，有用于多发性骨髓瘤的研究潜力。

Tubulin polymerization-IN-75 (Compound 6) 是一种微管蛋白聚合 (tubulin polymerization) 抑制剂，其 IC50 为 30 μM。它能抑制癌细胞 Huh7 和 293T 的增殖，IC50 分别为 14.3 μM 和 13.8 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)

PARP1-IN-6 is a dual tubulin/PARP-1 inhibitor with IC 50 values of 0.94 and 0.48 μM, respectively.

Tubulin polymerization-IN-6 (compound 5f) is a potent inhibitor of tubulin polymerization, with an IC50 of 1.09 μM. It not only inhibits cell migration and tube formation but also has anti-angiogenic properties. Additionally, Tubulin polymerization-IN-6 has been found to effectively hinder tumor growth in HT29 xenograft Balb c nude mice [1].

HDAC3 6-IN-2 (化合物 15) 是一种高效的HDAC6和HDAC3抑制剂，IC50值分别为0.368 μM和0.635 μM。此化合物不仅具备抗肿瘤活性，能够诱导癌细胞凋亡，同时通过降低HDAC6和HDAC3水平，与H3乙酰化和α-微管蛋白的上调有关。

Tubulin polymerization-IN-63（化合物6）为一种抑制微管蛋白聚合(Tubulin polymerization)的化合物，其对MES-SA细胞展示出0.29 μM的IC50值，适用于癌症研究领域。