tubulin-inhibitory

D64131 是一种微管蛋白聚合抑制剂，IC50 值为 0.53 μM。它具有抗丝分裂活性，可用于癌症研究。

Tubulin polymerization-IN-47 是一种 tubulin 聚合抑制剂和有丝分裂抑制剂，具有抗肿瘤活性，对神经母细胞瘤癌细胞增殖具有抑制作用，对 Chp-134 和 Kelly 细胞系的IC50 分别为 7 和 12 nM。Tubulin polymerization-IN-47 是治疗肝癌、结肠癌、肺癌和乳腺癌的候选化合物。

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) 是一种靶向人表皮生长因子受体2 (HER2) 的 ADC，作为 T-DM1 的活性代谢产物含有微管蛋白聚合抑制剂 DM1，可抑制微管蛋白聚合，常用于乳腺癌的研究。

Valecobulin hydrochloride (CKD-516 hydrochloride) 是 S516 的缬氨酸前体药和血管阻断剂。Valecobulin hydrochloride (CKD-516 hydrochloride) 对β-微管蛋白聚合有强效的抑制作用，对小鼠和人类的实体肿瘤具有显著的抗肿瘤活性。

GGFG-PAB-MMAE (Comp 58054-1) 作为一种高效的 ADC 药物-连接子偶联物，由 ADC linker (GGFG-PAB) 和抑制微管蛋白聚合的有效成分 MMAE 构成。

Tubulin polymerization-IN-76（compound 20b）是一种强效且口服活性的微管蛋白聚合抑制剂。它通过干扰秋水仙碱结合位点，以IC50值2.505 μM抑制微管蛋白的聚合，破坏细胞内的微管网络并干扰细胞有丝分裂。Tubulin polymerization-IN-76 对MGC-803和HGC-27细胞展现显著抑制，IC50值分别为1.61和1.82 nM。该化合物有效抑制MGC-803和HGC-27细胞的集落形成及迁移，并诱导G2 M期细胞周期阻滞和细胞凋亡（Apoptosis）。此外，Tubulin polymerization-IN-76 展示出广谱抗增殖活性。

Dolastatin 10 trifluoroacetate is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have an activity to inhibit tubulin polymerization (IC50: 1.2 μM). Besides that, it

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

Vincristine 属于生物碱类天然产物，可与微管蛋白结合并抑制微管的形成，从而抑制肿瘤细胞的有丝分裂。Vincristine 可用作微管去稳定剂，用于研究治疗血液系统肿瘤，如白血病和淋巴瘤以及儿童肉瘤的相关研究。

TTBK1-IN-1(compound 31)是一种强效和选择性的 tau 微管蛋白激酶 1 (TTBK1) 抑制剂(IC50=315 nM)，具有中枢神经(CNS)渗透性，能够抑制疾病相关的Ser 422表位的tau磷酸化，可用于研究阿尔茨海默病。

Tubulin inhibitor 12 (Hit 9) is a recently developed compound with potent inhibitory effects on tubulin (IC50 = 25.3 μM). This compound exhibits noteworthy anti-tumor and anti-proliferative activities, making it a promising candidate for the treatment of cancer [1].

HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1]

Tubulin inhibitor 19 (compound 9b) is a potent indole chalcone compound that exhibits strong inhibitory activity against tubulin. Its potential in cancer research makes it valuable for studying cancer diseases [1].

EGFR-IN-57 (Compound 25a) 是一种有效的、具有口服活性的EGFR-TK 抑制剂，IC50值为 0.054 μM。EGFR-IN-57 也抑制VEGFR-2、CK2α、topoisomerase IIβ和tubulin polymerization，IC50值分别为 0.087、0.171、0.13 和 3.61 μM。EGFR-IN-57 诱导细胞 G2 M 和 pre-G1 期周期阻滞，诱导癌细胞凋亡 (apoptosis)。

Antitumor Agent-71 是一种抗肿瘤化合物，对微管蛋白 (tubulin) 的聚集表现出抑制作用。Antitumor Agent-71 拥有抗增殖作用，对肿瘤细胞系的 IC50值范围为3.98-15.70 μM。

HDAC-IN-9 是有效的、选择性的 tubulin 和 HDAC 双重抑制剂。HDAC-IN-9 对 A549 细胞的侵袭和迁移表现出抑制作用。HDAC-IN-9 在体外和体内均表现出有效的抗肿瘤和抗血管生成活性。

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4 SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

Tubulin inhibitor 31, 以IC50值4 µM的效力，是一种高效的微管蛋白(Tubulin)抑制剂，具有显著的抗增殖活性，并能抑制HUVEC的迁移。

Tubulin MMP-IN-2是一种针对微管蛋白和基质金属蛋白酶的双重抑制剂，能有效抑制微管蛋白聚合并触发细胞凋亡。该化合物对MMP-2、MMP-3及MMP-9展现出明显的抑制效果，其IC50值分别为24.95 μM、31.60 μM与22.37 μM。Tubulin MMP-IN-2主要应用于癌症研究领域。

HI5 是一种有效的微管蛋白 (tublin)和IDO 抑制剂，对 HeLa 细胞的IC50为 70 nM。HI5 抑制IDO 的表达，减少犬尿氨酸的产生，从而刺激 T 细胞活化和增殖。HI5 对 HeLa 细胞可抑制微管蛋白聚合和细胞迁移，引起 G2 M 期阻滞，同时通过线粒体依赖性凋亡途径诱导细胞凋亡 (apoptosis) 并引起反应性氧化应激。HI5 可用于抗癌研究。

3,4',5-Trismethoxybenzophenone（compound 16a）是一种抑制微管蛋白组装（tubulin assembly）的有效物质，具有2.6 µM的IC50值。

ABT-751 (E7010) hydrochloride 为一种新型磺胺类抗有丝分裂化合物及微管蛋白(tubulin)结合剂,具有高口服生物利用度.该化合物通过与β-微管蛋白的秋水仙碱位点结合,阻断微管蛋白的聚集,从而在G2 M期引起细胞周期阻滞并诱导细胞凋亡(apoptosis).此外,ABT-751 (E7010) hydrochloride 还能通过抑制AKT MTOR信号通路,促进细胞自噬(autophagy).该化合物对包括肺癌、胃癌、结肠癌和乳腺癌在内的多种癌细胞类型展示出显著的抑制效果.