目录号 | 产品详情 | 靶点 | |
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T74899 | |||
GXH-II-052 是一种有效的二价 BET(bivalent bromodomain and extraterminal domain (BET))抑制剂。GXH-II-052 显示与 BRD4-1、BRD4-2、BRD4-T、BRDT-1、BRDT-2、BRDT-T 的结合潜力,Kd 值分别为 28、9.1、4.8、0.6、8.4、2.6 nM。GXH-II-052 显示出抗增殖活性。GXH-II-052 降低 c-Myc 的表达。 | |||
T78773 | |||
Tubulin inhibitor 38(化合物14)是一款强效的四唑基微管蛋白抑制剂,能够显著抑制细胞增殖。以100 nM浓度作用24小时后,该抑制剂能够引起有丝分裂停滞,特别是在G2/M期细胞周期阶段,进而诱导细胞凋亡。在HeLa、MCF7和U87 MG细胞系中,Tubulin inhibitor 38展现了较高的细胞毒性及选择性。 | |||
T63879 | |||
microRNA-21-IN-1(compound 7A)是一种高效microRNA抑制剂,对Hela和HCT-116细胞显示出抗增殖活性,IC50值分别为5.5 μM和2.8 μM,并能促进Hela细胞凋亡(apoptosis)。该化合物通过上调microRNA-21下游功能靶点(PTEN、EGR1、SLIT2)的表达,有助于抗癌研究。 | |||
T81922 | |||
LM2I是一种多杀菌素(SPA)衍生物,兼具精氨酸琥珀酸合成酶(ASS1)激活剂和针对ASS1的直接作用的肿瘤抑制剂功能。在7种结直肠癌细胞系和结直肠癌异种移植肿瘤中,LM2I展现出明显的抗增殖活性,并且通过EGFR途径阻断结直肠癌细胞增长。 | |||
T72164 | |||
Enpp/Carbonic anhydrase-IN-2 是一种有效的 Enpp 和 carbonic anhydrase 抑制剂,对 NPP1、NPP2、NPP3、CA-IX, CA-XII 的 IC50值分别 1.13、 1.07、 0.74、 0.33、 0.68。Enpp/Carbonic anhydrase-IN-2 对癌细胞具有抗增殖活性,对正常细胞具有低细胞毒性。Enpp/Carbonic anhydrase-IN-2 诱导细胞凋亡 (Apoptosis)。 | |||
T80074 | Others | ||
Biphalin TFA 是能穿透血脑屏障的阿片类肽,具有双活性脑啡肽效应团。该化合物对阿片受体有高亲和力,并在急性、神经性及慢性疼痛动物模型中展现了显著的镇痛活性。此外,Biphalin TFA 还具有抗病毒、抗增殖、抗炎以及神经保护的特性。 | |||
T36671 | |||
C2 Phytoceramide is a bioactive semisynthetic sphingolipid that inhibits formyl peptide-induced oxidant release (IC50 = 0.38 μM) in suspended polymorphonuclear cells. It increases COX-2 protein levels 15-fold through ERK signaling. It induces death of keratinocytes (20% viability) with an ED50 value of 30 μM, the same concentration at which 35% of cells in a TUNEL assay are apoptotic. C2 Phytoceramide also has antiproliferative effects in CHO cells, with greater than 80% cytotoxicity achieved at a concentration of 20 μM, and induces internucleosomal DNA fragmentation. In addition, it inhibits the activation of phospholipase D (PLD) mediated by muscarinic acetylcholine receptors in vitro. | |||
T69197 | |||
AG-012986 HCl is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 HCl showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 HCl was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 HCl also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity. | |||
T70906 | |||
EHT-6706 is a novel microtubule-disrupting agent that targets the colchicine-binding site to inhibit tubulin polymerization. At low nM concentrations, EHT 6706 exhibits highly potent antiproliferative activity on more than 60 human tumor cell lines, even those described as being drug resistant. EHT 6706 also shows strong efficacy as a vascular-disrupting agent, since it prevents endothelial cell tube formation and disrupts pre-established vessels, changes the permeability of endothelial cell monolayers and inhibits endothelial cell migration. Genome-wide transcriptomic analysis of EHT 6706 effects on human endothelial cells shows that the antiangiogenic activity elicits gene deregulations of antiangiogenic pathways. These findings indicate that EHT 6706 is a promising tubulin-binding compound with potentially broad clinical antitumor efficacy. | |||
T79662 | STAT | ||
STAT3-IN-20(Compound 40)是一种选择性地靶向STAT3的SH2结构域,展现了在DU145和MDA-MB-231癌细胞中的抗增殖效果(IC50分别为2.97 μM和3.26 μM),并诱导细胞周期停滞与细胞凋亡。该抑制剂有效抑制了STAT3的磷酸化、核内易位及其下游基因的转录活性(IC50: 0.65 μM)。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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