目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T83951 | |||
TM2 TEAD抑制剂是一种有效并且可逆的TEA领域转录因子抑制剂(IC50为TEAD4自动棕榈酰化和TEAD2棕榈酰化分别为38 nM和156 nM)。它抑制TEAD-YAP的结合和转录活性。TM2 TEAD抑制剂在YAP依赖型癌症细胞中,无论是单独使用还是与MEK抑制剂联合使用,都显示出强大的抗增殖效果。同时抑制体外YAP依赖的肝脏类器官生长。 | |||
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.). | |||
T77038 | |||
Interferon alfa 是 I 型干扰素,可激活新基因,对靶细胞产生有效抗病毒和抗增殖活性。Interferon alfa 的信号传导需要 Stat1和 Stat2 的受体依赖性激活,形成异源二聚化 STAT。STAT 复合物与 DNA 结合蛋白 IRF-9 (p48) 结合并形成 ISGF-3 (IFN 刺激基因因子 3)。随后由 ISGF-3 进一步激活驱动基因,实现抗病毒功能。 | |||
T35409 | Apoptosis Antibacterial | ||
(+)-δ-Cadinene 是一种从G. hirsutum 中发现的倍半萜,具有抗菌、杀虫、抗癌和抗增殖活性。 它对肺炎双球菌的MIC 值为31.25 μg/ml,对 A. stephensi、A. aegypti 和 C. quinquefasciatust 三龄幼虫的LC50s 值分别8.23、9. 2和3。(+)-δ-Cadinene(10、50 和 100 μM)可诱导 OVCAR-3 人类卵巢癌细胞凋亡并抑制其增殖。 | |||
T9644 | |||
Triciferol 作为具有结合了 VDR 激动剂和 HDAC 拮抗剂活性的多重配体发挥作用。Triciferol 直接与 VDR 结合 (IC50=87 nM),在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化,并增强组蛋白乙酰化。Triciferol 在体外癌细胞模型中也表现出有效的抗增殖和细胞毒性活性。 | |||
T72803 | |||
Norartocarpetin 是一种酪氨酸酶抑制剂。Norartocarpetin 具有较强的酪氨酸酶抑制活性,其抑制活性 IC50值为 0.47 μM。Norartocarpetin 作为一种抗褐变剂可用于食品体系的研究。Norartocarpetin 对肺癌细胞 (NCI-H460) 也具有显著的抗癌活性,其 IC50值为 22 μM。Norartocarpetin 的抗增殖作用是通过靶向 Ras/Raf/MAPK 信号通路、线粒体介导的细胞凋亡、S 期细胞周期阻滞和抑制细胞迁移和侵袭实现的。 | |||
T60453 | |||
TrxR-IN-3 (Compound 2c) 是TrxR 的有效抑制剂。TrxR-IN-3 对五种人类癌细胞系表现出强大的抗增殖活性,特别是对乳腺肿瘤细胞。TrxR-IN-3 增加 ROS 水平并通过调节乳腺癌细胞中细胞凋亡相关蛋白的表达导致明显的细胞凋亡。TrxR-IN-3 还通过促进 LC3-II 和 Beclin-1 的表达并减少 LC3-I 和 p62 蛋白的表达,来触发自噬体和自溶酶体的形成。 | |||
T69963 | |||
Birabresib dihydrate was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibitor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and differentiation to energy homeostasis and neurological processes. OTX015 has potent antiproliferative activity accompanied by c-MYC down-regulation in several tumor types, and has demonstrated synergism with the mTOR inhibitor everolimus in different models. Oral administration of OTX-015 markedly inhibited tumor growth and reduced tumor volume. OTX015 is currently in Phase 1b studies for the treatment of hematological malignancies and advanced solid tumors such as Triple Negative Breast ...... | |||
T71230 | |||
VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 , but not purvalanol B, significantly decreased the proportion of cells in S phase and increased the proportion of cells in G(2)/M. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death Receptors DR4 and DR5, Bax and Bad while decreasing the number of viable cells, all supporting apoptosis as a mechanism of cell death. VMY-1-103 possesses unique antiproliferative capabilities and that this compound may form the basis of a new candidate drug to treat medulloblastoma. | |||
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。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
TMPH-01073 | CD81 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
CD81 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 25.8 kDa and the accession number is P60033.
|
|||||
TMPY-06983 | IFN gamma Protein, Human, Recombinant (E. coli) | Human | E. coli | ||
IFN gamma, also known as IFNG, is a secreted protein that belongs to the type II interferon family. IFN gamma is produced predominantly by natural killer and natural killer T cells as part of the innate immune response, and by CD4 and CD8 cytotoxic T lymphocyte effector T cells once antigen-specific immunity develops. IFN gamma has antiviral, immunoregulatory, and anti-tumor properties. IFNG, in addition to having antiviral activity, has important immunoregulatory functions, it is a potent activator of macrophages and has antiproliferative effects on transformed cells and it can potentiate the antiviral and antitumor effects of the type I interferons. The IFNG monomer consists of a core of six α-helices and an extended unfolded sequence in the C-terminal region. IFN gamma is critical for innate and adaptive immunity against viral and intracellular bacterial infections and tumor control. Aberrant IFN gamma expression is associated with some autoinflammatory and autoimmune diseases. The importance of IFN gamma in the immune system stems in part from its ability to inhibit viral replication directly, and most importantly from its immunostimulatory and immunomodulatory effects. IFNG also promotes NK cell activity.
|
|||||
TMPH-02451 | IFN gamma Protein, Marmota monax, Recombinant (His) | Marmota monax | P. pastoris (Yeast) | ||
Produced by lymphocytes activated by specific antigens or mitogens. IFN-gamma, in addition to having antiviral activity, has important immunoregulatory functions. It is a potent activator of macrophages, it has antiproliferative effects on transformed cells and it can potentiate the antiviral and antitumor effects of the type I interferons. IFN gamma Protein, Marmota monax, Recombinant (His) is expressed in yeast with N-6xHis tag. The predicted molecular weight is 18.6 kDa and the accession number is O35735.
|
|||||
TMPK-00637 | IFNAR2 Protein, Cynomolgus, Recombinant (aa 27-243, His) | Cynomolgus | HEK293 Cells | ||
Although interferon (IFN)-α is known to exert immunomodulatory and antiproliferative effects on dendritic cells (DCs) through induction of protein-coding IFN-stimulated genes (ISGs), little is known about IFN-α-regulated miRNAs in DCs. Since several miRNAs are involved in regulating DC functions, it is important to investigate whether IFN-α's effects on DCs are mediated through miRNAs as well. IFNAR2 Protein, Cynomolgus, Recombinant (aa 27-243, His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 25.93 kDa and the accession number is G7P6B3.
|
|||||
TMPH-00373 | IFN gamma Protein, Chicken, Recombinant (GST) | Chicken | E. coli | ||
Produced by lymphocytes activated by specific antigens or mitogens. IFN-gamma, in addition to having antiviral activity, has important immunoregulatory functions. It is a potent activator of macrophages, it has antiproliferative effects on transformed cells and it can potentiate the antiviral and antitumor effects of the type I interferons. IFN gamma Protein, Chicken, Recombinant (GST) is expressed in E. coli expression system with N-GST tag. The predicted molecular weight is 43.7 kDa and the accession number is P49708.
|
|||||
TMPK-00889 | IFNAR2 Protein, Human, Recombinant (aa 27-243, His) | Human | HEK293 Cells | ||
Although interferon (IFN)-α is known to exert immunomodulatory and antiproliferative effects on dendritic cells (DCs) through induction of protein-coding IFN-stimulated genes (ISGs), little is known about IFN-α-regulated miRNAs in DCs. Since several miRNAs are involved in regulating DC functions, it is important to investigate whether IFN-α's effects on DCs are mediated through miRNAs as well. IFNAR2 Protein, Human, Recombinant (aa 27-243, His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 25.8 kDa and the accession number is P48551-2.
|
|||||
TMPJ-01371 | Limitin Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Limitin, also called IFN-ζ, is a secreted interferon (IFN)-like glycoprotein. Limitin has approximately 30% sequence homology with IFN-α, IFN-β, and IFN-ω and binds to the IFN-α/β receptors. Like IFN-α and IFN-β, limitin has antiproliferative, immunomodulatory, and antiviral properties, it is unique in lacking influence on myeloid and erythroid progenitors. Similar dose requirement between limitin and IFN-α was observed for the enhancement of cytotoxic T lymphocyte activity, the augmentation of MHC class I expression, and the growth inhibition of a myelomonocytic leukemia cell line.
|
|||||
TMPY-02122 | IFNGR2 Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Interferon-gamma receptor beta chain (IFNgammaR2), also known as IFNGR2, belongs to the type II cytokine receptor family, whose deficiency is a cause of autosomal recessive mendelian susceptibility to mycobacterial disease (MSMD), also known as familial disseminated atypical mycobacterial infection. This accessory factor is an integral part of the IFN-gamma signal transduction pathway and is likely to interact with GAF, JAK1, and/or JAK2. IFNGR2 is a component of the IFNgamma receptor complex along with the IFNgammaR alpha chain (IFNGR1) and is a new Bax suppressor. The C-terminal fragment (cytoplasmic domain) of IFNgammaR2 is expressed in human cancer cell lines of megakaryocytic cancer (DAMI), breast cancer (MDA-MD-468), and prostate cancer (PC3 cells). The Th1 cytokine IFNgamma, acting through its heterodimeric receptors, IFNgammaR1 and IFNgammaR2, in the induction/proliferation of Th1 cells, might suppress the Th2 responses that may underlie atopic asthma. IFNGR2 has always been seen as a key mechanism for shielding T lymphocytes from the antiproliferative effects of the IFNgamma-signal transducer and activator of the transcription 1 (STAT1) pathway.
|