目录号 | 产品详情 | 靶点 | |
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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。 | |||
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。 | |||
T35762 | |||
MC1742 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.1, 0.11, 0.02, and 0.61 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 7 and 40 nM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb over class IIa HDACs (IC50s = >50 μM for HDAC4, -5, -7, and -9). MC1742 reduces proliferation of HOS, MG-63, RD, A204, SK-ES-1, and A673 sarcoma cancer stem cells (CSCs). It increases levels of acetylated histone H3 and acetylated tubulin and induces apoptosis in MG-63 CSCs when used at a concentration of 2 μM. MC1742 also reactivates HIV-1 in JLAT 10.6 latently infected cells (EC50 = 350 nM).2 |1. Di Pompo, G., Salerno, M., Rotili, D., et al. Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells. J. Med. Chem. 58(9), 4073-4079 (2015).|2. Heffern, E.F.W., Ramani, R., Marshall, G., et al. Identification of isoform-selective hydroxamic acid derivatives that potently reactivate HIV from latency. J. Virus Erad. 5(2), 84-91 (2019). | |||
T83898 | |||
S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine (SFN-Cys) 是一种异硫氰酸酯衍生物及第一类和第二类组蛋白去乙酰化酶(HDAC)抑制剂和抗癌剂硫代硫酸烯醇醚的活性代谢产物。它通过巯基乙酸途径酶从硫代硫酸烯醇醚经DL-硫代硫酸烯醇醚谷胱甘肽和硫代硫酸烯醇醚半胱氨酸甘肽中间体形成。SFN-Cys (20 µM) 通过创伤愈合和腔室分析实验,分别减少了U87MG和U373 MG胶质母细胞瘤细胞的侵袭和迁移。在45 µM的浓度下,它降低了对紫杉醇耐药的A549肺癌细胞(A549/T)中的α-微管蛋白、βIII-微管蛋白、司他敏1和X连锁抑制剂的凋亡(XIAP)的水平,并减少了细胞密度。使用30 µM浓度的SFN-Cys诱导U87MG和U373 MG细胞凋亡和G2/M期细胞周期停滞。 | |||
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...... | |||
T79710 | HDAC | ||
PI3Kα/HDAC6-IN-1(化合物21j)是一种针对PI3Kα/HDAC6的双重抑制剂,其IC50值分别为2.9 nM和26 nM。该化合物还能抑制AKT(Ser473)的磷酸化,诱导α-微管蛋白的积累,并促进其乙酰化,但对乙酰化组蛋白H3和H4无显著影响。在L-363细胞系中,PI3Kα/HDAC6-IN-1显示了高效的抑制活性(IC50=0.17 μM),表现出良好的抗癌潜力。 | |||
T63074 | |||
Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂,具有异羟肟酸部分,能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累,诱导 p53 依赖性反式激活,并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡,并具有抗肿瘤效果。 | |||
T79383 | |||
ER degrader 7 (Compound 35t) 是一种既能降解ERα又能降解ERβ的化合物。该化合物具有抑制微管蛋白聚合的功能,并能有效降低多种细胞系(包括MCF-7、T47D、MCF-10A、LCC2、T47D D538G与T47D Y537S)的细胞活性,相应IC50s值分别为0.06、2.56、15.84、1.59、1.67、1.37 μM。此外,ER degrader 7 对乳腺癌肿瘤生长同样有抑制作用。 | |||
T36800 | |||
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells. 1.Luo, M., Spradlin, J.N., Boike, L., et al.Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product functionCell Chem. Biol.28(4)559-566(2021) | |||
T71055 | |||
Albendazole-d7 is intended for use as an internal standard for the quantification of albendazole by GC- or LC-MS. Albendazole is an orally bioavailable benzimidazole anthelmintic that is active against a variety of helminths, including liver flukes, tapeworms, and roundworms. It eliminates Trichostrongylus in the fourth stomach of cattle and sheep when orally administered at doses ranging from 2.5 to 10 mg/kg as well as other species in the fourth stomach and the small and large intestine. Albendazole (0.05% in the diet) protects mice against lethal infection with A. suum larvae. It also inhibits growth of HT-29 human colorectal cancer cells (IC50 = 0.12 µM), halts the cell cycle at the G2/M phase, and induces apoptosis. In an HT-29 mouse xenograft model, it inhibits peritoneal tumor growth when administered intraperitoneally at a dose of 150 mg/kg but not when administered orally. Albendazole inhibits mammalian tubulin polymerization and inhibits binding of [3H]mebendazole t...... |
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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