目录号 | 产品详情 | 靶点 | |
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T79708 | |||
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。 | |||
T25025 | |||
ALB-109564 dihydrochloride 是长春碱生物碱的半合成衍生物,是一种微管蛋白抑制剂和抗肿瘤药物。它与微管蛋白单体结合并抑制微管的形成,导致有丝分裂纺锤体组装的破坏和肿瘤细胞停滞在细胞周期的G2/M 期。 | |||
T60421 | |||
Antitumor agent-68 是一种有效的微管蛋白抑制剂,具有良好的抗肿瘤活性,对宫颈癌细胞系 HeLa 和乳腺癌细胞系 MCF-7 细胞的IC50值分别为 3.6 和 3.8 μM。Antitumor agent-68 以剂量依赖的方式表现出良好的 ROS 和DPPH 自由基的清除活性。 | |||
T74003 | |||
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。 | |||
T74074 | |||
OSu-Glu-VC-PAB-MMAD是由微管抑制剂MMAD与可降解的ADC linker OSu-Glu-VC-PAB通过一种高度特异性的连接方式构成,作为抗体-活性分子偶联物(antibody-drug conjugates, ADCs)中的关键组成部分。 | |||
T79563 | Sirtuin | ||
Sirt1/2-IN-2 (compound hsa55)是一种针对SIRT1/2的双重抑制剂,具有分别针对SIRT1和SIRT2的IC50值为1.8 μM和2.4 μM。该化合物能有效阻止p53的脱乙酰化作用,并提高p53及α-微管蛋白的乙酰化水平。此外,Sirt1/2-IN-2能诱导细胞凋亡,并展示出对人白血病细胞系的抗增殖效果。 | |||
T71218 | |||
AEZS-112, also known as ZEN012, is an orally active small mol. anti-cancer drug which inhibits the polymn. of tubulin at low micromolar concns. AEZS 112 dose-dependently increased non-vital hypodiploid cells and the cytotoxic effect was least pronounced in G2 phase of the cell cycle, indicating cell death during mitosis, as detd. by FACS anal. AEZS 112 showed anti-tumor activity in human ovarian and endometrial cancer cell lines at low micromolar concns., which could not be abrogated by caspase inhibition and is therefore a good candidate for in vivo studies in these tumors. | |||
T78780 | |||
Anticanceragent 139(Compound 6h)展现了针对多种癌细胞株的抗癌效能。该化合物能够与Tubulin的Lys352残基发生π-阳离子相互作用。在对SNB-19、OVCAR-8和NCI-H460细胞株的测试中,Anticanceragent 139展现出较高的生长抑制率(PGI),数值分别为86.61、85.26和75.99。同时,该化合物对于HOP-62、SNB-75、ACHN、NCI/ADR-RES、786-O、A549/ATCC、HCT-116以及MDA-MB-231细胞株亦表现出中等的生长抑制作用,其PGI值分别为67.55、65.46、59.09、59.02、57.88、56.88、56.53和56.4、51.88。 | |||
T69305 | |||
Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize 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, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). | |||
T71217 | |||
MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria/caspase 9-dependent pathway. Notably, several KB-derived multidrug-resistant cancer cell lines were also sensitive to MPT0B214 treatment. ( PLoS One. 2013;8(3):e58953). |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-03059 | Tubulin cofactor A Protein, Human, Recombinant | Human | E. coli | ||
Tubulin folding cofactor A belongs to the TBCA family. It is one of four proteins (cofactors A, D, E, and C) involved in the early step of the tubulin folding pathway. These proteins can fold intermediates and finally lead to correctly folded beta-tubulin. It is believed that tubulin folding cofactors A and D play a role in capturing and stabilizing beta-tubulin intermediates in a quasi-native confirmation. Tubulin folding cofactor E binds to the cofactor D/beta-tubulin complex; interaction with tubulin folding cofactor C then causes the release of beta-tubulin polypeptides that are committed to the native state.
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TMPJ-00773 | TUBB4A Protein, Human, Recombinant (His) | Human | E. coli | ||
Tubulin Beta-4A Chain (TUBB4A) is a cytoplasmic peptide containing 444 amino acids. TUBB4A is a member of the Tubulin family. Tubulin is the major constituent of microtubules. Tubulin is a dimer composed of one alpha and one beta tubulin molecule; there are many forms of beta tubulins, Beta II and Beta IV Tubulin are ubiquitously expressed. Beta-III Tubulin, also known as Tubulin Beta-4, is regarded as a neuron-specific marker. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain.
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TMPY-03392 | CKAP1/TBCB Protein, Human, Recombinant (His) | Human | E. coli | ||
Tubulin-folding cofactor B, also known as TBCB, belongs to the TBCB family. It contains 1 CAP-Gly domain and can be detected in most tissues. TBCB binds to alpha-tubulin folding intermediates after their interaction with cytosolic chaperonin in the pathway. The cytoskeleton is composed of 3 structural elements: actin filaments, microtubules, and intermediate filaments. TBCB is involved in regulation of tubulin heterodimer dissociation. It may function as a negative regulator of axonal growth.
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TMPH-00383 | Tubulin beta-1 chain Protein, Chicken, Recombinant (His) | Chicken | E. coli | ||
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain. Tubulin beta-1 chain Protein, Chicken, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 53.3 kDa and the accession number is P09203.
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TMPY-04110 | TPPP2 Protein, Human, Recombinant (His) | Human | E. coli | ||
TPPP2 Protein, Human, Recombinant (His) is expressed in E. coli expression system with His tag. The predicted molecular weight is 20.3 kDa and the accession number is AAH38970.1.
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TMPY-03397 | TPPP3 Protein, Human, Recombinant (His) | Human | E. coli | ||
TPPP3, a member of the Tubulin polymerization-promoting protein family, is an intrinsically unstructured protein that induces tubulin polymerization. TPPP3 is a marker in the developing musculoskeletal system. In tendons, Tppp3 is expressed in cells at the circumference of the developing tendons, likely the progenitors of connective tissues that surround tendons: the tendon sheath, epitenon, and paratenon. Tppp3 is also expressed in forming synovial joints. The onset of Tppp3 expression in joints coincides with cavitation, representing a molecular marker that can be used to indicate this stage in joint transition in joint differentiation. In late embryonic stages, Tppp3 expression highlights other demarcation lines that surround differentiating tissues in the forelimb. Depletion of TPPP3 by microRNA-based RNA interference (RNAi) inhibits cell growth, arrests cell cycles, and causes mitotic abnormalities in HeLa cells. C57BL/6 mice that received subcutaneously injected LLC (Lewis lung carcinoma) cells in which TPPP3 was knocked down showed a pronounced reduction in tumor progression. The migration/invasion activity of TPPP3-knockdown LLC cells was significantly suppressed in a transwell chamber migration assay. When these cells were injected into the tail veins of C57BL/6 mice, they exhibited milder lung metastasis compared with control tumor cells. Taken together, these findings suggested that the TPPP3 gene played an important role in tumorigenesis and metastasis, and it could potentially become a novel target for cancer therapy.
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TMPY-01203 | RP2 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
XRP2, also known as Protein XRP2 and RP2, is a member of the TBCC (tubulin cofactor C) family and contains one C-CAP/cofactor C-like domain. This protein is encoded by the RP2 gene in humans. XRP2 stimulates the GTPase activity of tubulin, but does not enhance tubulin heterodimerization. XRP2 acts as guanine nucleotide dissociation inhibitor for ARL3. Defects in RP2 gene are the cause of retinitis pigmentosa type 2 (RP2), also known as X-linked retinitis pigmentosa 2 (XLRP-2). It leads to degeneration of retinal photoreceptor cells. Patients typically have night vision blindness and loss of midperipheral visual field. As their condition progresses, they lose their far peripheral visual field and eventually central vision as well.
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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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TMPH-02261 | TUBB2A Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
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TMPH-02260 | TUBB Protein, Human, Recombinant (His) | Human | E. coli | ||
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain. TUBB Protein, Human, Recombinant (His) is expressed in E. coli expression system with C-6xHis tag. The predicted molecular weight is 50.6 kDa and the accession number is P07437.
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TMPY-03750 | CRIPT Protein, Human, Recombinant (His) | Human | E. coli | ||
CRIPT, also known as cysteine-rich PDZ-binding protein, belongs to the CRIPT family. It interacts with TUBB1. CRIPT also interacts strongly with the PDZ3 domain of members of the DLG4 family. It is involved in the cytoskeletal anchoring of DLG4 in excitatory synapses. CRIPT is highly conserved from mammals to plants and binds selectively to the third PDZ domain (PDZ3) of PSD-95 via its C terminus. n heterologous cells, CRIPT causes a redistribution of PSD-95 to microtubules. In brain, CRIPT colocalizes with PSD-95 in the postsynaptic density and can be coimmunoprecipitated with PSD-95 and tubulin. These findings suggest that CRIPT may regulate PSD-95 interaction with a tubulin-based cytoskeleton in excitatory synapses.
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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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TMPJ-01270 | ZMYND19 Protein, Human, Recombinant (His) | Human | E. coli | ||
Human Zinc Finger MYND Domain-Containing Protein 19 (ZMYND19) is a protein that contains 1 MYND-Type Zinc Finger. ZMYND19 can be expressed by the brain, testis, placenta, heart, liver, skeletal muscle, kidney, and stomach. ZMYND19 interacts with GPR24/MCH-R1. It binds to the C terminus of Melanin-Concentrating Hormone Receptor-1 and the N Termini of α-Tubulin. ZMYND19 may be involved as a regulatory molecule in GPR24/MCH-R1 signaling.
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TMPJ-01387 | PACSIN2 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Protein Kinase C and Casein Kinase Substrate in Neurons Protein 2 (PACSIN2) is a member of the PACSIN family. PACSIN2 is localized to the plasma membrane via its coiled-coil domain. PACSIN2 is widely expressed and contains one FCH domain and one SH3 domain. PACSIN2 forms homo- and hetero-aggregates with other PACSINs. PACSIN2 may play a role in vesicle formation and transport. In addition, PACSIN2 is involved in linking the actin cytoskeleton with vesicle formation by regulating tubulin polymerization.
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TMPH-02183 | CCT2 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Component of the chaperonin-containing T-complex (TRiC), a molecular chaperone complex that assists the folding of proteins upon ATP hydrolysis. The TRiC complex mediates the folding of WRAP53/TCAB1, thereby regulating telomere maintenance. As part of the TRiC complex may play a role in the assembly of BBSome, a complex involved in ciliogenesis regulating transports vesicles to the cilia. The TRiC complex plays a role in the folding of actin and tubulin. CCT2 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 70.3 kDa and the accession number is P78371.
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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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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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