目录号 | 产品详情 | 靶点 | |
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T71811 | |||
Lobaric acid is a depsidone metabolite that has been isolated from Stereocaulon lichen species with antioxidant, antiproliferative, antiviral, and enzyme inhibitory activites. It scavenges superoxide radicals in a cell-free assay (IC50 = 97.9 μmol) and inhibits proliferation in a panel of leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic, and lung cancer cell lines (EC50s = 15.2-63.9 μg/ml). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC50 = 0.87 μM for the human recombinant enzyme) and production of 12(S)-HETE (Item No. 34570) by 12(S)-lipoxygenase (IC50 = 28.5 μM). In vivo, lobaric acid (250 μM) decreases lesion number, but not lesion diameter, in tobacco leaves infected with tobacco mosaic virus (TMV). | |||
T73471 | |||
YLT-11 是一种有效的选择性和具有口服活性的PLK4抑制剂,对 PLK1、PLK2、PLK3、PLK4的Kd 值分别为 >10000、653、>10000、5.2 nM。YLT-11 显示出抗增殖活性。YLT-11 诱导细胞凋亡 (Apoptosis) 细胞周期停滞在 G2/M 期。YLT-11 具有抗癌活性。 | |||
T79420 | |||
FLT3-IN-22(化合物22f)是一款高效的FLT3抑制剂,具有针对FLT3和FLT3/D835Y极低的IC50值,分别为0.941 nM和0.199 nM。在MV4-11细胞和携带FLT3变异的Ba/F3细胞系中(涵盖FLT3-D835Y及FLT3-F691L),此抑制剂显示出显著的抗增殖能力。 | |||
T79667 | PARP | ||
YCH1899为一种口服活性PARP抑制剂,其对PARP1/2的IC50均低于0.001 nM。该化合物对Olaparib和Talazoparib耐药的Capan-1细胞株(Capan-1/OP及Capan-1/TP细胞)表现出显著抗增殖能力,IC50分别为0.89 nM和1.13 nM。在大鼠体内,YCH1899展现优良的药代动力学属性。 | |||
T74898 | |||
NC-III-49-1 是一种有效的二价 BET(bivalent bromodomain and extraterminal domain (BET))抑制剂。NC-III-49-1 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 0.095、0.32、0.29、0.089 、5.5、0.058 nM。NC-III-49-1 显示出抗增殖活性。NC-III-49-1 降低 c-Myc 的表达。 | |||
T72759 | |||
c-Met/HDAC-IN-2 是一种高效的c-Met 和HDAC 双重抑制剂,对HDAC1与c-Met 的IC50分别为 18.49 nM 和 5.40 nM。c-Met/HDAC-IN-2 对几种癌细胞具有抗增殖活性。c-Met/HDAC-IN-2 能将 HCT-116 细胞周期阻滞在 G2/M 期,诱导细胞凋亡 (apoptosis)。c-Met/HDAC-IN-2 可用于抗癌耐药研究。 | |||
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。 | |||
T62531 | |||
TRK-IN-12 (Compound 9e) 是一种大环衍生的有效TRK抑制剂,具有显著的TRKG595R抑制活性 (IC50= 13.1 nM)。在Ba/F3-LMNA-NTRK1细胞系中具有出色的抗增殖效果 (IC50= 0.080 μM),并且在Ba/F3-LMNA-NTRK1-G595R细胞系中展示了超过对照活性分子LOXO-101的抑制能力 (IC50= 0.646 μM)。 | |||
T68631 | |||
Carbetimer is a partially imidized copolymer of ethylene & maleic anhydride with average MW approx 1,200 daltons; capable of specific stimulation of immune response. Carbetimer is a low molecular weight polymer derived from ethylene and maleic anhydride with potent antineoplastic activity. Preclinical studies have shown antitumor effects against many tumor cell lines including B 16 melanoma. Its antitumor actions are felt to include both reduction of uridine and cytidine nucleoside triphosphate as well as the diminution of pyrimidine salvage by inhibiting uridine, cytidine, and thymidine kinase. Besides direct antiproliferative effects, Carbetimer could act through immunomodulation, as suggested by the induction of cytotoxic T-cells in mice and the discordant in vitro and in vivo activities against the Lewis lung carcinoma model. | |||
T69618 | |||
XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kinase activation and anchorage-independent growth in NIH 3T3 transformed with v12 H-ras. Since the antiproliferative effect of the compound is not related to the ras phenotype, XR3054 may also have effects on other cell signaling mechanisms. |
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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