目录号 | 产品详情 | 靶点 | |
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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). | |||
T68743 | |||
AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity. KSP inhibitor AZD4877 selectively inhibits microtubule motor protein KSP (also called kinesin-5 or Eg5), which may result in the inhibition of mitotic spindle assembly; activation of the spindle assembly checkpoint; induction of cell cycle arrest during the mitotic phase; and cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents. Eg5 is essential for the formation of bipolar spindles and the proper segregation of sister chromatids during mitosis. | |||
T75240 | |||
Taltobulin hydrochloride (HTI-286 hydrochloride) 是一种合成的三肽半胱氨酸类似物,为高效抗微管剂,能够在体内外绕过P-糖蛋白介导的药物耐药性。该化合物通过抑制微管蛋白的聚合和破坏细胞内微管结构,进而引起细胞有丝分裂停滞和细胞凋亡。 | |||
T79564 | Sirtuin | ||
Sirt1/2-IN-3 (compound PS9) 作为SIRT1/2的双重抑制剂,其对SIRT1和SIRT2的IC50值分别为1.4 μM 和 2.0 μM。该化合物能够有效抑制p53脱乙酰化,并提升p53与α-微管蛋白的乙酰化水平。Sirt1/2-IN-3还能诱导细胞凋亡,并展现对人白血病细胞系的抗增殖效果。 | |||
T31657 | |||
Epothilone F is a derivative or analogue of Epothilone D. Epothilone F is also an active metabolite of Epothilone D. In molecule of Epothilone F, a hydroxymethyl group is on the thiazole ring. Like taxanes, Epothilone F prevents cancer cells from dividing | |||
T73950 | |||
Flutax-2 (5/6-mixture)为紫杉醇的一种活性荧光衍生物,能与α,β微管蛋白二聚体发生结合。其激发/发射波长分别为496/524 nm。紫杉醇作为红豆杉属植物产生的二萜类次生代谢物,在多种癌症研究中有应用。Flutax-2的储存应避光处理。 | |||
T68860 | |||
Iso-Fludelone is the third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone 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 other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as well as reduced toxicity. In addition, this agent is a not a substrate of the P-glycoprotein (P-gp), a multidrug resistance pump often overexpressed in cancer cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). | |||
T79322 | |||
Antiproliferative agent-30 (Compound 8g) 抑制微管蛋白组装且可抑制FLT3及Abl1。该化合物展现出对血管的破坏活性,并对多种癌细胞系表现出强效的抗增殖能力,包括HCT-116、K562及MV-4-11细胞(IC50值分别为0.054 nM、0.008 nM、0.144 nM)。此外,Antiproliferative agent-30 亦对携带FLT3-ITD-TKD突变的AML显示出抗癌效果。 | |||
T35437 | |||
(-)-Viriditoxin is a mycotoxin originally isolated from A. viridinutans that has antibacterial and antiproliferative activity. It is active against methicillin-sensitive and -resistant S. aureus (MSSA and MRSA, respectively), tetracycline-sensitive and -resistant Staphylococcus, vancomycin-sensitive and -resistant Enterococcus, and penicillin-sensitive and -resistant S. pneumoniae (MICs = 2-32 μg/ml). (-)-Viriditoxin is also active against fish pathogens, including S. iniae and S. parauberis (MICs = 0.16-0.21 μg/ml). It inhibits polymerization and the GTPase activity of E. coli FtsZ, a tubulin-like GTPase involved in bacterial cell division (IC50s = 8.2 and 7 μg/ml, respectively). (-)-Viriditoxin inhibits proliferation of human DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5.36, 0.63, and 7.6 μM, respectively) . It is also toxic to mice (LD50 = 2.8 mg/kg, i.p.). | |||
T83819 | |||
2’-O-甲基鸟苷-5'-O-三磷酸(2’-methyl GTP)作为丙肝病毒(HCV)非结构蛋白5B(NS5B;IC50 = 3.5 µM)的抑制剂,同时是前药IDX184的活性代谢产物,通过2’-methylguanosine中间体生成。在50 µM浓度下,2’-methyl GTP还能促进微管蛋白聚合。患有肝细胞癌的患者体内2’-methyl GTP水平,相比于邻近正常组织有所下降。 |
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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