目录号 | 产品详情 | 靶点 | |
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T75142 | |||
Acid Ceramidase-IN-2(compound 1)是一款针对酸性神经酰胺酶(ceramidase)的抑制剂,显示出抗增殖及细胞活性抑制的潜力。有研究表明,该化合物在前列腺癌细胞中可阻止人酸性神经酰胺酶的过度表达,从而揭示了其潜在的抗肿瘤能力。此外,Acid Ceramidase-IN-2被三种α-酮酰胺:GT85、GT98和GT99在体外有效抑制其水解作用。 | |||
T80750 | PROTACs | ||
YN14是一种高效且选择性的KRASG12C蛋白水解靶向嵌合体(PROTAC)。其能够稳定诱导KRASG12C:YN14:VHL三元复合物,并展现出低结合自由能(ΔG)。YN14对KRASG12C突变型癌细胞的增殖具有抑制作用,显著抑制其生长,并能在MIA PaCa-2异种移植模型中促进肿瘤消退,实现超过100%的肿瘤生长抑制(TGI%)。 | |||
T61017 | |||
Topoisomerase II inhibitor 6 (Compound 5) 是色胺酮的衍生物。它是一种有效的拓扑异构酶的选择性抑制剂。Topoisomerase II inhibitor 6 在 G2 期阻断 CCRF-CEM 的细胞周期并诱导 DNA 双链断裂。Topoisomerase II inhibitor 6 对不同的肿瘤细胞系具有抗增殖活性,在癌症疾病研究中具有潜力。 | |||
T73121 | FGFR | ||
FGFR4-IN-8 (Compound 7v) 是 ATP 竞争性、高选择性的 FGFR4 野生型及其突变体共价抑制剂,对 FGFR4、FGFR4V550L、FGFR4V550M 及 FGFR4C552S 的 IC50 值分别为 0.5、0.25、1.6、931 nM。该化合物能有效抑制 Hep3B 肝细胞癌细胞增殖,显示出显著的抑制效果,具有潜在的临床应用价值。 | |||
T68581 | |||
AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the low nanomolar cellular and biochemical inhibitory properties of AP23464 extend to frequently observed imatinib mesylate-resistant Bcr-Abl mutants, including nucleotide binding P-loop mutants Q252H, Y253F, E255K, C-terminal loop mutant M351T, and activation loop mutant H396P. AP23464 was ineffective against mutant T315I, an imatinib mesylate contact residue. The potency of AP23464 against imatinib mesylate-refractory Bcr-Abl and its distinct binding mode relative to imatinib mesylate warr...... | |||
T81740 | Trk receptor | ||
Multi-kinase-IN-6 (compound 10e) 是一种效能极高的多激酶抑制剂,具有对 TrkA、ALK2、c-KIT、EGFR、PIM1、CK2α、CHK1 和 CDK2 等多种酶的显著抑制作用。在 MCF7、HCT116 和 EKVX 癌细胞系上,其抗增殖活性突出,IC50 值分别达到 3.36 μM、1.40 μM 与 3.49 μM。此外,Multi-kinase-IN-6 能引起 MCF7 与 HCT116 细胞的细胞周期在 G1/S 期及 G1 期停滞,并有效诱导凋亡。 | |||
T79456 | Pim | ||
FD1024是一种PIM抑制剂,对PIM1、PIM2和PIM3的IC50s分别为1.96、38.9及4.17 nM。用于急性髓系白血病研究的FD1024,对AML细胞系显示出显著的抗增殖效果,其对EOL-1、MV-4-11、KG-1和MOLM-16细胞的抑制浓度(IC50s)分别为0.16 μM、0.12 μM、1.05 μM和1.39 μM。此外,FD1024在小鼠模型中也表现出抗肿瘤活性。 | |||
T79274 | Histone Methyltransferase | ||
PRMT5-IN-31(Compound 3m)作为一种高选择性PRMT5抑制剂,其IC50为0.31 μM。它能够通过占据PRMT5的底物位点以及与氨基酸残基形成必要相互作用来上调hnRNP E1蛋白水平。此外,PRMT5-IN-31能有效抑制A549细胞增殖,其机制涉及诱导apoptosis和阻碍细胞迁移。该化合物在人肝微粒体中表现出较高的代谢稳定性,半衰期为132.4分钟。 | |||
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.). | |||
T79587 | VEGFR | ||
hCA/VEGFR-2-IN-2 (compound 8g) 是一种具有吲哚酮基苯磺酰胺结构的化合物,目标是癌症相关的hCA IX/XII 及VEGFR-2 的双重抑制剂。该化合物对VEGFR-2 表现出强效的抑制作用(IC50=204 nM),且对hCAs有高亲和力,Ki 值分别为 hCA IX 3.6 nM、hCA II 16.1 nM、hCA XII 16.7 nM 以及hCA I 75.3 nM。hCA/VEGFR-2-IN-2 还展现出针对过表达VEGFR-2 的乳腺癌细胞的抗增殖活性。 |
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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