目录号 | 产品详情 | 靶点 | |
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T69480 | |||
Sagopilone is a fully synthetic low-molecular-weight epothilone with potential antineoplastic activity. Sagopilone binds to tubulin and induces microtubule polymerization while stabilizing microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. The agent is not a substrate for the P-glycoprotein (P-gp) efflux pump and so may exhibit activity in multidrug-resistant (MDR) tumors. The epothilone class of metabolites was originally isolated from the myxobacterium Solangium cellulosum. | |||
T83834 | |||
Sp-Guanosine-5'-O-(1-thiotriphosphate) (Sp-GTP-α-S) 是一种含硫核苷酸衍生物GTP-α-S的异构体。它能结合到微管蛋白上,在20 mM的浓度下用于无细胞实验时可诱导微管组装。 | |||
T77874 | |||
Maytansinoid B 是一种ADC Cytotoxin,用于形成与抗体结合的Antibody-Drug Conjugates (ADCs)。它是一种抗有丝分裂剂,能够结合微管蛋白并阻断其组装,诱导细胞周期在G2/M阶段停滞,进而触发细胞凋亡(apoptosis)。 | |||
T79382 | Estrogen Receptor/ERR | ||
ER degrader 6 (compound 35s) 是高效的雌激素受体 (ER)α降解剂,作用机制为通过抑制微管蛋白聚合破坏微管网络。该化合物能抑制肿瘤生长,并展现出较低的毒性特性。 | |||
T79408 | |||
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。 | |||
T74648 | |||
TAM470 是一种新型的细胞溶素,可抑制微管蛋白聚集和微管解聚。TAM470 可作为有效载荷分子用于合成 OMTX705,OMTX705 是一种具有抗肿瘤活性的FAP 靶向抗体偶联活性分子 (ADCs)。 | |||
T71577 | |||
KOS-1584 is a second-generation epothilone with potential antineoplastic activity. Epothilone KOS-1584 binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2/M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and efficacy with an enhanced pharmaceutical profile, including enhanced water solubility and tumor penetration, and reduced CNS exposure. In addition, epothilone KOS-1584 is a poor substrate for the P-glycoprotein (P-gp) drug efflux pump. | |||
T71116 | |||
MPT0B098 is a potent microtubule inhibitor through binding to the colchicine-binding site of tubulin. MPT0B098 is active against the growth of various human cancer cells, including chemoresistant cells with IC50 values ranging from 70 to 150 nmol/L. MPT0B098 arrests cells in the G2–M phase and subsequently induces cell apoptosis. In addition, MPT0B098 effectively suppresses VEGF-induced cell migration and capillary-like tube formation of HUVECs. Distinguished from other microtubule inhibitors, MPT0B098 not only inhibited the expression levels of HIF-1α protein but also destabilized HIF-1α mRNA. The mechanism of causing unstable of HIF-1α mRNA by MPT0B098 is through decreasing RNA-binding protein, HuR, translocation from the nucleus to the cytoplasm. Notably, MPT0B098 effectively suppresses tumor growth and microvessel density of tumor specimens in vivo. Taken together, our results provide a novel mechanism of inhibiting HIF-1α of a microtubule inhibitor MPT0B098. MPT0B098 is...... | |||
T70808 | |||
Cabazitaxel-d6 is a deuterium labeled cabazitaxel. Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel binds to and stabilizes tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, this agent is a poor substrate for the membrane-associated, multidrug resistance (MDR), P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. In addition, cabazitaxel penetrates the blood-brain barrier (BBB). | |||
T74844 | |||
Antiproliferative agent-23,一种微管去稳定剂(MDA),通过扰乱微管蛋白-微管系统来发挥作用。该化合物通过降低Bcl-2蛋白水平、提高Bax和Cyt c蛋白水平以及激活半胱天冬酶级联反应和线粒体依赖途径来诱导细胞凋亡。此外,Antiproliferative agent-23还能在A549/CDDP细胞(顺铂耐药癌细胞系)中通过PERK/ATF4/CHOP信号通路激活ROS介导的内质网应激,展现出抗肿瘤活性。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPJ-00827 | Tau-D Protein, Human, Recombinant (His) | Human | E. coli | ||
Microtubule-Associated Protein TAU is abundantly expressed in neurons of the central nervous system and less commonly expressed elsewhere, but is also expressed at very low levels in CNS astrocytes and oligodendrocytes. Tau interacts with tubulin to stabilize microtubules and promotes tubulin assembly into microtubules. The C-terminus of TAU binds axonal microtubules while the N-terminus binds neural plasma membrane components, suggesting that tau acts as a linker protein. When tau is defective, and no longer stabilize microtubules properly, it can result in dementias such as Alzheimer's disease and other tauopathies.
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TMPY-03047 | Stathmin 1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Stathmin1 (STMN1) is a cytosolic phosphoprotein that regulates cellular microtubule dynamics and is known to have oncogenic activity. STMN1 is a possible biomarker for paclitaxel sensitivity and poor prognosis in GC and could be a novel therapeutic target in metastatic GC. STMN1 expression might serve as a biomarker for determining patient atypical meningioma prognosis. Stathmin1 (STMN1) is a cytosolic protein involved in microtubule dynamics through inhibition of tubulin polymerization and promotion of microtubule depolymerization, which has been implicated in carcinogenesis and aggressive behavior in multiple epithelial malignancies. Stathmin 1 (STMN1) suppression was reported to reduce cellular viability and migration potential. STMN1 may be a promising candidate for targeted therapies in PDAC.
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TMPH-02304 | Vasohibin-2/VASH2 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Tyrosine carboxypeptidase that removes the C-terminal tyrosine residue of alpha-tubulin, thereby regulating microtubule dynamics and function. Critical for spindle function and accurate chromosome segregation during mitosis since microtuble detyronisation regulates mitotic spindle length and postioning. Acts as an activator of angiogenesis: expressed in infiltrating mononuclear cells in the sprouting front to promote angiogenesis. Plays a role in axon formation. Vasohibin-2/VASH2 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 56.4 kDa and the accession number is Q86V25.
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TMPY-03509 | TCTP/TPT1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Tumor protein, also known as TPT1, is a highly conserved protein among many eukaryotic organisms. Tumor protein is involved in a variety of cellular activities, including microtubule stabilization, calcium-binding activities, and apoptosis. The Mammalian translationally controlled tumour protein (TPT1) (or P23) is a protein that has been found to be preferentially synthesised in cells during the early growth phase of some types of tumour, but which is also expressed in normal cells. It was first identified as a histamine-releasing factor, acting in IgE +-dependent allergic reactions. In addition, TPT1 has been shown to bind to tubulin in the cytoskeleton, has a high affinity for calcium, is the binding target for the antimalarial compound artemisinin, and is induced in vitamin D-dependent apoptosis. TPT1 production is thought to be controlled at the translational as well as the transcriptional level.
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