39
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12034 |
Microtubule inhibitor 1
|
Others | Others |
Microtubule inhibitor 1 is an antitumor agent with microtubule polymerization inhibitory activity(IC50 = 9-16 nM, in cancer cells). | |||
T22661 |
CHM-1
|
Apoptosis; Others; Microtubule Associated | Apoptosis; Cytoskeletal Signaling; Others |
CHM-1 是细胞凋亡的诱导剂,通过激活 Cdc2 激酶活性在人肝细胞癌中显示出有效的抗肿瘤能力。 CHM-1 在体外和体内抑制微管蛋白聚合。 | |||
T4029 |
BTB-1
BTB 1,NSC156750 |
Microtubule Associated | Cytoskeletal Signaling |
BTB-1 (NSC156750) 是一种新型的有丝分裂运动蛋白 Kif18A 的小分子抑制剂,IC50值为1.69 μM。 | |||
T1992 |
Mertansine
DM1,Maytansinoid DM1 |
Microtubule Associated | Cytoskeletal Signaling |
Mertansine (DM1) 是一种微管蛋白抑制剂,也是一种抗体可缀合的美登木素生物碱。它通过连接体连接到单克隆抗体上,形成抗体偶联药物。 | |||
T13224 |
Tubulin inhibitor 6
iHAP1 |
Microtubule Associated | Cytoskeletal Signaling |
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。 | |||
T9831 |
MKC-1
Ro-31-7453 |
Apoptosis; Akt; Microtubule Associated; mTOR | Apoptosis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
MKC-1 (Ro-31-7453) 是一种口服生物可利用的小分子双吲哚基马来酰亚胺细胞周期抑制剂,具有潜在的抗肿瘤活性。 | |||
T21408 |
DM1-SMe
DM1-SSMe |
Microtubule Associated | Cytoskeletal Signaling |
DM1-SMe (DM1-SSMe) 是美登木素微管的有效抑制剂。 DM1-SMe 的效力是母体药物美登素的 3 至 10 倍,在一组人类肿瘤细胞系中,DM1-SMe 的 IC50 为 0.003 至 0.01 nM。 | |||
T6864 |
Ixabepilone
BMS 247550,Ixempra,Azaepothilone B,伊沙匹隆,BMS 247550-1 |
Apoptosis; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
Ixabepilone (Azaepothilone B) 是一种可口服的微管抑制剂,能够与微管蛋白结合,促进微管蛋白的聚合和微管的稳定,使细胞停滞在 G2-M 期,诱导细胞凋亡。 | |||
T15576 |
Indibulin
2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺,ZIO 301,D 24851 |
Apoptosis; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
Indibulin (D 24851) 是一种口服有效的微管蛋白合成抑制剂,具有抗有丝分裂和抗肿瘤活性,且神经毒性小。它降低了肌间神经张力,产生异常的纺锤体,激活有丝分裂检查点蛋白 Mad2 和 BubR1,并诱导有丝分裂停滞和细胞凋亡。 | |||
T11947 |
MARK4 inhibitor 1
|
Apoptosis; Others; AMPK | Apoptosis; Chromatin/Epigenetic; Others; PI3K/Akt/mTOR signaling |
MARK4 inhibitor 1 是一种MARK4的抑制剂,IC50值为1.54 μM。它抑制癌细胞增殖、转移,诱导凋亡。 | |||
T36848 |
Combretastatin A-1
Combretastatin A1 |
Akt; Microtubule Associated | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Combretastatin A-1 是一种有效的微管抑制剂,具有抗肿瘤和抗血管活性,通过微管蛋白解聚介导的 AKT 失活抑制 Wnt/β-catenin 通路发挥作用,可用于研究肝癌。 | |||
T11184 |
EML4-ALK kinase inhibitor 1
EML4 ALK kinase inhibitor 1,EML4-ALK kinase inhibitor 1 |
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) 是有效的、具有口服活性的类棘皮细胞微管相关蛋白4-间变性淋巴瘤激酶 (EML4-ALK) 的抑制剂,其 IC50 值为 1 nM。 | |||
T35548 |
Dynapyrazole A
|
Dynamin | Cytoskeletal Signaling |
Dynapyrazole A 是微管动力蛋白的特异性抑制剂,对动力蛋白 1 和动力蛋白 2 依赖性微管滑动的 IC50 分别为 2.3 和 2.6 μM。 Dynapyrazole A 抑制 Hedgehog 信号传导,IC50 为 1.9 μM。 | |||
T60688 |
MKI-1
MASTL Kinase Inhibitor-1 |
Others | Others |
MKI-1 (MASTL Kinase Inhibitor-1) 是微管相关丝氨酸/苏氨酸样激酶 (MASTL) 抑制剂 (IC50= 9.9 μM)。MKI-1 通过激活乳腺癌中的PP2A 发挥放射增敏和抗肿瘤活性。 | |||
T15183 |
Dynarrestin
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
Dynarrestin 是一种细胞质动力蛋白 1 和 2的氨基噻唑抑制剂。它能够快速的、可逆的抑制动力蛋白 1 驱动的微管在体外滑动和细胞内动力蛋白 1 和 2 依赖性过程,且不影响 ATP 水解和干扰纤毛发生。它可抑制神经元前体和肿瘤细胞的刺猬因子依赖性增殖。 | |||
T36816 |
S-trityl-L-Cysteine
STLC |
Kinesin | Cytoskeletal Signaling |
S-Trityl-L-cysteine 是别构驱动蛋白Eg5的选择性抑制剂。rityl-L-cysteine 抑制基础 ATPase 活性的IC50为 1 μM,抑制微管激活的 ATPase 活性的IC50为 140 nM。S-Trityl-L-cysteine 显示出抗肿瘤活性。 | |||
T61749 | Microtubule inhibitor 2 | ||
Microtubule inhibitor 2 is a highly potent and selective microtubule inhibitor, which is orally active. It induces cell death via ferroptosis, and exhibits notable antitumor activity [1]. | |||
T11945 |
MARK-IN-1
|
Others | Others |
MARK-IN-1 is a potent microtubule affinity regulating kinase (MARK) inhibitor, (IC50<0.25 nM). | |||
T18871 |
VCP-Eribulin
|
Others | Others |
VCP-Eribulin, an Eribulin-based drug for antibody conjugates[1], combines the VCP (ADCs linker) with Eribulin, a distinct microtubule inhibitor used in cancer treatments[2]. | |||
T61765 | Microtubule inhibitor 5 | ||
Microtubule inhibitor 5 (compound 17f) is a highly potent cytotoxic agent that inhibits microtubule function. It exhibits a substantial cytotoxic effect on NCI-H460 cells, with an IC50 value of 154.5 nM. Moreover, this compound demonstrates excellent cell permeability [1]. | |||
T17357 |
AcLys-PABC-VC-Aur0101
|
Others | Others |
AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for anti-CXCR4 ADC with potent antitumor activity, comprising the auristatin microtubule inhibitor Aur0101, connected through the cleavable linker AcLys-PABC-VC[1]. | |||
T81850 | MASTL-IN-2 | ||
MASTL-IN-2为MASTL(microtubule-associated Ser/Thr kinase-like)抑制剂,能够抑制人上皮MIA PaCa癌细胞的增殖,其IC50值为2.8 nM。 | |||
T18278 |
Mal-PEG2-VCP-Eribulin
|
Others | Others |
Mal-PEG2-VCP-Eribulin is a chemotherapeutic compound comprising an antibody-drug conjugate (ADC) linker (Mal-PEG2-VCP) and the microtubule inhibitor Eribulin[1]. This compound uniquely targets microtubules, offering a novel approach to cancer treatment. Eribulin is specifically utilized in creating targeted Eribulin-based drugs for antibody conjugates[1]. | |||
T37037 |
Vinflunine ditartrate
|
||
Vinflunine ditartrate, a fluorinated microtubule inhibitor and member of the Vinca alkaloids family, exhibits anti-angiogenic, vascular-disrupting, and anti-metastatic properties. It presents a potential avenue for studying transitional cell carcinoma of the urothelial tract, non-small cell lung cancer, and breast carcinoma[1][2]. | |||
T40367 |
Combretastatin A-1 phosphate tetrasodium
Combretastatin A-1 phosphate tetrasodium,OXi-4503 tetrasodium |
||
Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a prodrug of Combretastatin A-1, is a tubulin-binding microtubule polymerization inhibitor that targets the colchicine-binding site. By inducing tubulin depolymerization, Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway and leads to the deactivation of AKT. It possesses both anti-tumor and anti-vascular properties. | |||
T81851 | MASTL-IN-1 | ||
MASTL-IN-1是一款针对MASTL(微管相关丝氨酸/苏氨酸样激酶)的抑制剂,起到调控细胞增殖、迁移及侵袭的作用。它显示出在癌症研究中的应用潜力。 | |||
T36855 |
Phomopsinamine
|
||
Phomopsinamine is an inhibitor of microtubule polymerization and a derivative of phomopsin A .1It inhibits the rate and extent of polymerization of tubulin isolated from ovine brain (IC50s = 0.53 and 0.59 μM, respectively). 1.Lacey, E., Edgar, J.A., and Culvenor, C.C.Interaction of phomopsin A and related compounds with purified sheep brain tubulinBiochem. Pharmacol.36(13)2133-2138(1987) | |||
T62251 |
MARK-IN-4
|
||
MARK-IN-4 是一种有效的微管亲和调节激酶 (MARK) 抑制剂 (IC50: 1 nM)。抑制 MARK 是一种潜在的、有吸引力的方法用于阻止阿尔茨海默病中神经纤维缠结病变。 | |||
T79232 |
MARK4 inhibitor 2
|
AMPK | Chromatin/Epigenetic; PI3K/Akt/mTOR signaling |
MARK4 inhibitor 2作为MARK4的高效抑制剂,展现出对微管亲和调节激酶 4 (MARK4) 的Km值为6.3×10^7,及IC50为0.82 μM的特异性。它能够抑制癌细胞生长,适用于癌症的科学研究。 | |||
T60402 | Tubulin inhibitor 14 | ||
Tubulin inhibitor 14 是一种有效的 NQO2(醌氧化还原酶 2)抑制剂,IC50 为 1.0 μM,也抑制微管蛋白聚合和内皮细胞毛细管样管的形成。Tubulin inhibitor 14 是一种微管去稳定剂,具有潜在的肿瘤选择性以及抗血管生成和血管破坏的功能[1]。 | |||
T79408 |
KGP591
|
||
KGP591为微管蛋白聚合抑制剂(IC50 0.57µM),能显著诱导MDA-MB-231细胞G2/M停滞,同时抑制细胞迁移,破坏微管结构及细胞形态。在RENCA原位肾癌模型中,KGP591展现了抗肿瘤活性。 | |||
T73195 |
EAPB 02303
|
||
EAPB 02303 是一种微管破坏剂和抑制剂。EAPB 02303 诱导有丝分裂停止和纺锤体组装损伤。因此,EAPB 02303 诱导细胞凋亡 (apoptosis) 并表现出抗肿瘤活性。EAPB 02303 在较低浓度下也表现出与紫杉醇 的强协同作用。 | |||
T77823 |
Polatuzumab vedotin
|
||
Polatuzumab vedotin是一种抗体药物偶联物,靶向CD79b。该化合物结合了人源化抗CD79b IgG1单克隆抗体和微管抑制剂monomethyl auristatin E (MMAE),展现出针对大B细胞淋巴瘤(LBCL)的治疗潜力。 | |||
T79629 |
Tubulin polymerization-IN-46
|
||
Tubulin polymerization-IN-46(compound 9q)是一种微管蛋白抑制剂,能够阻断微管蛋白聚合并诱发细胞凋亡。该化合物通过抑制有丝分裂,导致MCF-7细胞在G2/M期停滞,对MCF-7乳腺癌细胞展现出抗增殖效果,其IC50值为10 nM。 | |||
T79645 |
Tubulin polymerization-IN-48
|
||
Tubulin polymerization-IN-48 (Compound 4k) 是一种中等强度破坏微管网络的微管蛋白聚合抑制剂。其对神经母细胞瘤癌细胞增殖的抑制效果显著,Chp-134 细胞系和 Kelly 细胞系的IC50值分别为79 nM和165 nM。 | |||
T60936 |
Tubulin polymerization-IN-24
|
||
Tubulin aggregation-IN-24 (compound HMBA) 是一种有效的微管蛋白聚合抑制剂,可提高 GTP 水解速率并抑制微管组装。Tubulin aggregation-IN-24 诱导细胞凋亡和细胞周期停滞在 G2/M 期。Tubulin aggregation-IN-24 抑制乳腺癌细胞 MCF-7 的增殖。 | |||
T79708 |
SSE1806
|
||
SSE1806是鬼臼毒素(天然的抗有丝分裂剂)的一个衍生物,也是微管蛋白(Microtubule/Tubulin)的抑制剂,展现出显著的抗增殖和抗癌活性。该化合物抑制癌细胞生长的GI50在1.29-21.15 μM范围内。SSE1806能引发有丝分裂异常和G2/M期阻滞,升高p53蛋白的表达,并抑制结肠癌样器官的生长。此外,SSE1806能克服MDR-1高表达细胞系的多药耐药性。 | |||
T60953 | BSc5367 | ||
BSc5367 是Nek1激酶结构域的有效抑制剂,IC50值为 11.5 nM。Nek1 是一种NIMA 相关的蛋白激酶,在细胞周期调节、DNA 修复和微管调节中起着关键作用。Nek1 功能障碍在肌萎缩侧索硬化症 (ALS)、多囊肾病 (PKD) 和几种类型的放疗耐药性癌症中发挥关键作用。BSc5367 为更好的理解上述疾病提供了有用工具。 | |||
T83874 |
S-72
|
||
S-72是一种微管聚合抑制剂,以1, 3, 10 µM的浓度在无细胞测定中抑制微管聚合,并在MCF-7和耐紫杉醇的MCF-7/T乳腺癌细胞中降低细胞活性(IC50分别为15.64和26.32 nM)。50 nM浓度的S-72能抑制MCF-7和MCF-7/T细胞的迁移和侵袭,并减少划痕实验中的伤口闭合百分比。100 nM的S-72在MCF-7/T细胞中诱导G2/M期的细胞周期阻滞以及凋亡,并在同一浓度下抑制这些细胞中干扰素基因激活剂(STING)的激活。以每天15 mg/kg的剂量,S-72抑制了耐紫杉醇的MCF-7/T和MX-1/T小鼠异种移植模型中的肿瘤生长。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10928 |
Cytochalasin A
|
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Cytochalasin A is a cell-permeable fungal toxin and is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50 = 3 μM), inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhy | |||
T75521 | PM050489 | ||
PM050489 是一种有效的聚酮类微管/微管蛋白 (Microtubule/Tubulin) 抑制剂,可从马达加斯加海绵Lithoplocamia lithistoides 中分离。PM050489 抑制有丝分裂,IC50值为 26.4 nM。PM050489 具有抗肿瘤活性,能用于癌症研究。 | |||
T74761 |
Eleutherobin
|
||
Eleutherobin 是一种有效的 β 微管蛋白 (β-microtubule),IC50为 2 μM。Eleutherobin 可从海洋软珊瑚中提取。Eleutherobin 对癌细胞的细胞毒活性具有与紫杉醇 (Paclitaxel)) 相似的效力。具有抗癌活性。 |