目录号 | 产品详情 | 靶点 | |
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T72522 | |||
Aurora kinase-IN-1 是aurora kinase 的有效抑制剂。Aurora kinase-IN-1 上调 G1 细胞周期抑制蛋白 (包括 p21 和 p27) 以及 G1 进行性细胞周期蛋白 D1 的表达,并下调 G1-to-S 进行性细胞周期蛋白,导致细胞周期停滞在 G1/S 边界。Aurora 激酶-IN-1 还诱导细胞凋亡 (apoptosis)。Aurora 激酶-IN-1 是化疗药物的先导化合物。 | |||
T78841 | |||
Nrf2-IN-3 (Compound R16) 为Nrf2抑制剂,与KEAP1突变体 (G333C mKEAP1) 结合,能够恢复受损的KEAP1/NRF2相互作用。该化合物通过修复mKEAP1/NRF2复合物,增加KEAP1突变癌细胞对Cisplatin和Gefitinib的敏感性。 | |||
T74691 | |||
Aprinocarsen (ISIS 3521) sodium,是针对蛋白激酶C-α(PKC-α)的特异性反义寡核苷酸抑制剂,为一种20-mer寡核苷酸,通过调节细胞分化和增殖来发挥作用。其能有效抑制人类肿瘤细胞系在裸鼠体内的生长,展示了作为人类癌症化疗化合物的潜力。 | |||
TMIH-0181 | |||
Demethoxy Curcumin-d4 是 Demethoxy Curcumin 的氘代化合物。Demethoxy Curcumin 的 CAS 号为 22608-11-3。Demethoxycurcumin是姜黄素的主要活性成分,有抗炎和抗癌作用。 | |||
TN2177 | c-Myc NF-κB | ||
Sanggenol L shows higher cytotoxicity against human oral tumor cell lines (HSC-2 and HSG) than against normal human gingival fibroblasts (HGF), it induces apoptosis via caspase activation and inhibition of NF-κB/IκBα± phosphorylation as a potent chemother | |||
TN4046 | MMP FAK PARP GSK-3 NF-κB Wnt/beta-catenin Akt Caspase PI3K Prostaglandin Receptor JNK | ||
ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP). | |||
TN3152 | ERK BCL Akt HIV Protease PPAR p53 | ||
6-Acetonyldihydrochelerythrine exhibits significant antioxidant activities, it exhibits significant anti-HIV activity in H9 lymphocytes with EC50 and TI (Therapeutic Index) values of 1.77 microg/mL and 14.6, respectively. 6-Acetonyldihydrochelerythrine is | |||
T36650 | |||
Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellular adhesion molecule-1 (ICAM-1; IC50 = 300 nM). Early in vitro studies showed that ansatrienin B potentiates the chemotherapeutic action of 5-fluorouracil , cisplatin , bleomycin , mitomycin C , and 6-mercaptopurine. Ansatrienin B is a hydroquinone form of ansatrienin A . | |||
T38503 | |||
(2-Pyridyldithio)-PEG1-hydrazine is a one-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs). This linker offers the advantage of controlled release of the drug payload from the ADC construct. It is utilized in the conjugation process between the antibody and the cytotoxic drug, enabling the targeted delivery of the drug to cancer cells. The (2-pyridyldithio) group of this linker provides stability during circulation in the bloodstream, while the hydrazine moiety allows for efficient drug release at the tumor site. Overall, the (2-pyridyldithio)-PEG1-hydrazine linker serves as a valuable tool in the development of targeted chemotherapeutic agents for cancer treatment. | |||
T71279 | |||
BPR1K653 is a potent Aurora kinase inhibitor with potential anticancder activity. BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent activity against the growth of xenograft tumors of the human cervical carcinoma KB and KB-derived MDR1-positive KB-VIN10 cells in nude mice. Finally, BPR1K653 also exhibited favorable pharmacokinetic properties in rats., BPR1K653 is a promising anti-cancer compound that has potential for the management of various malignancies, particularly for patients with MDR1-related drug resistance after prolonged chemotherapeutic treatments. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-02646 | NSE/ENO2 Protein, Human, Recombinant (His) | Human | E. coli | ||
The combination of silencing ENO2 and 2-deoxyglucose (2-DG) synergistically inhibited leukemia cell survival. ENO2 may be a biological marker for monitoring chemotherapeutic efficacy and relapse in ALL. Reduced ENO2 expression may be a biomarker for a subset of autistic children. Neuron specific enolase (ENO2, gamma-enolase) has been used as a biomarker to help identify neuroendocrine differentiation in breast cancer.
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TMPY-03407 | NQO1 Protein, Human, Recombinant (His) | Human | E. coli | ||
NQO1 gene is a member of the NAD(P)H dehydrogenase (quinone) family and encodes a cytoplasmic 2-electron reductase. NQO1 forms homodimers and reduces quinones to hydroquinones. NQO1's enzymatic activity prevents the one-electron reduction of quinones that results in the production of radical species. Mutations in the NQO1 gene have been associated with tardive dyskinesia (TD), an increased risk of hematotoxicity after exposure to benzene, and susceptibility to various forms of cancer. Altered expression of NQO1 has been seen in many tumors and is also associated with Alzheimer's disease (AD). Alternate transcriptional splice variants, encoding different isoforms, have been characterized. Recent pharmacological research suggests the feasibility of genotype-directed redox chemotherapeutic intervention targeting NQO1 breast cancer, a common missense genotype encoding a functionally impaired NQO1 protein.
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TMPH-01211 | DGUOK Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Phosphorylates deoxyguanosine and deoxyadenosine in the mitochondrial matrix, with the highest efficiency for deoxyguanosine. In non-replicating cells, where cytosolic dNTP synthesis is down-regulated, mtDNA synthesis depends solely on DGUOK and TK2. Phosphorylates certain nucleoside analogs. Widely used as target of antiviral and chemotherapeutic agents.
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TMPJ-01145 | ABCB5 Protein, Human, Recombinant (Trx) | Human | E. coli | ||
ATP-binding cassette sub-family B member 5(ABCB5) is a plasma membrane-spanning protein. ABCB5 is principally expressed in physiological skin and human malignant melanoma. ABCB5 has been suggested to regulate skin progenitor cell fusion and mediate chemotherapeutic drug resistance in stem-like tumor cell subpopulations in human malignant melanoma. It is commonly over-expressed on circulating melanoma tumour cells. Furthermore, the ABCB5+ melanoma- initiating cells were demonstrated to express FLT1 (VEGFR1) receptor tyrosine kinase which was functionally required for efficient xenograft tumor formation, as demonstrated by shRNA knockdown experiments.
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TMPJ-00922 | DCK Protein, Human, Recombinant (His & T7) | Human | E. coli | ||
Deoxycytidine Kinase (DCK) is a member of the DCK/DGK family. DCK exists as a homodimer and is localized to the nucleus. DCK is required for the phosphorylation of the deoxyribonucleosides deoxycytidine (dC), deoxyguanosine (dG), and deoxyadenosine (dA). DCK has broad substrate specificity, and does not display selectivity based on the chirality of the substrate. In addition, DCK is also an essential enzyme for the phosphorylation of numerous nucleoside analogs widely employed as antiviral and chemotherapeutic agents. DCK is clinically important because of its relationship to drug resistance and sensitivity.
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TMPY-00648 | UNC5A Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
The netrin-1 receptor Uncoordinated Phenotype-5A, or UNC5A, plays an important role in predicting response to DNA damage induced by chemotherapeutic drug and regulating cell death in bladder cancer. Moreover, UNC5A is cumulatively downregulated by the unfolding protein response (UPR) at the transcriptional level in vitro and at the translational level both in vitro and in vivo. Also, UNC5A is a novel transcriptional target of p53 and plays a role in p53-dependent apoptosis. UNC5A Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 58.3 kDa and the accession number is Q6ZN44-1.
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TMPY-03329 | DPEP1 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Dehydropeptidase-I, also known as DPEP1, is a kidney membrane enzyme. Its expression in normal colonic mucosa is very low, but it is highly expressed in colorectal adenoma and cancer specimens and is negatively correlated with parameters of pathological aggressiveness and poor prognosis. The overexpression of DPEP1 suppressed tumor cells invasiveness and increased sensitivity to chemotherapeutic agent Gemcitabine. Growth factor EGF treatment decreased DPEP1 expression. Dehydropeptidase-I may be a candidate target in PDAC for designing improved treatments. It uses zinc as a cofactor and acts as a disulfide-linked homodimer.
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TMPY-00999 | UNC5A Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
The netrin-1 receptor Uncoordinated Phenotype-5A, or UNC5A, plays an important role in predicting response to DNA damage induced by chemotherapeutic drug and regulating cell death in bladder cancer. Moreover, UNC5A is cumulatively downregulated by the unfolding protein response (UPR) at the transcriptional level in vitro and at the translational level both in vitro and in vivo. Also, UNC5A is a novel transcriptional target of p53 and plays a role in p53-dependent apoptosis. UNC5A Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 32.7 kDa and the accession number is Q6ZN44-1.
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TMPY-00924 | SMAC Protein, Human, Recombinant (His) | Human | E. coli | ||
Apoptosis is an essential processes required for normal development and homeostasis of all metazoan organisms. Second Mitochondria-Derived Activator of Caspases (Smac) or Direct IAP Binding Protein with low isoelectric point, pI (Diablo) is a proapoptogenic mitochondrial protein that is released to the cytosol in response to diverse apoptotic stimuli, including commonly used chemotherapeutic drugs. The current knowlege about structure and function of Smac/Diablo during programmed cell death, both in mitochondrial and receptor pathways are presented. It has been shown that Diablo mainly interacts with IAPs in the cytochrome c/Apaf-1/caspase-9 pathway, and promotes apoptosis. Diablo is released from the mitochondria into the cytosol occurring downstream of cytochrome c release in response to apoptotic stimuli such as irradiation, DNA damage or cytotoxic drugs. In the cytosol, Smac/Diablo interacts and antagonizes inhibitors of apoptosis proteins (IAPs), thus allowing the activation of caspases and apoptosis. This activity has prompted the synthesis of peptidomimetics that could potentially be used in cancer therapy. The role of Smac/DIABLO in colorectal carcinogenesis is ill defined. Data continues to accumulate to suggest that decreased levels of Smac/DIABLO may be important in chemoradiation-resistance to apoptosis in advanced colon cancer.
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