目录号 | 产品详情 | 靶点 | |
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T70049 | |||
Ro 04-5595 is a selective antagonist of NMDA receptors NR2B subunits. Ro 04-5595 had an EC 50 of 186 ± 32 nmol/L. Ro 04-5595 was predicted to bind the EVT-101 binding site, not the ifenprodil-binding site. Specific binding, defined with a new NR2B-specific antagonist Ro 04-5595 at 10 microM was fully inhibited by several compounds with the following rank order of affinities--Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol > spermine > spermidine > MgCl2 > CaCl2--and partially inhibited by competitive glutamate recognition site antagonists. Complementary high-resolution autoradiographic images using [3H]Ro04-5595 demonstrated strong binding in NR2B receptor-rich regions and low binding in cerebellum where NR2B concentration is low. | |||
T71227 | |||
LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor). LGB321 is unique relative to previously described PIM inhibitors, in that it is active in PIM2 dependent cell lines. , a kinase that has proven difficult to inhibit in the cellular context. Consistent with its activity on all three PIM kinases, LGB321 inhibits proliferation of a number of cell lines derived from diverse hematological malignancies, including MM, AML, CML and B-Cell NHL. In vivo, LGB-321 is orally available, demonstrates efficacy in tumor xenografts and is well-tolerated within the therapeutic exposure range in mice. (source: Clin Cancer Res. 2014 Apr 1;20(7):1834-45 ) | |||
T78753 | Aurora Kinase | ||
Aurora Kinases-IN-4(Compound 11c)是共价ATP竞争型aurora kinaseA抑制剂,具有IC50为1.7 nM。该化合物对SJSA-1、MDA-MB-231、A549和HeLa细胞系的增殖抑制效果显著,其IC50分别为4.27、1.54、3.08和6.99 μM。Aurora Kinases-IN-4适用于三阴性乳腺癌(TNBC)的相关研究。 | |||
T75714 | |||
Decapeptide-12,一个小型寡肽,作为tyrosinase的抑制剂,通过与tyrosinase的C末端残基相互作用(Kd: 61.1 μM)发挥作用。作为mushroom tyrosinase的竞争性抑制剂(IC50: 40 µM),Decapeptide-12有效上调SIRT的转录水平,并能减少黑色素细胞中的黑色素含量,适用于黑色素生成、衰老和炎症的研究。 | |||
T83935 | |||
eIF4A i28是一种真核起始因子-4A(eIF4A)抑制剂,其在eIF4A ATP酶实验中的IC50为8.60 μM。它能降低BJAB Burkitt淋巴瘤细胞的活性,其在CellTiter-Glo (CTG) 发光细胞活性测试中的EC50为0.46 μM。eIF4A i28作为一种与RNA竞争性、与ATP非竞争性的eIF4A抑制剂发挥作用。 | |||
T60837 | |||
AChE/BuChE-IN-2 (Compound 5f) 具有血脑屏障通透性,它是口服有效的 AChE 和BuChE 抑制剂,IC50值分别为 0.72 μM 和 0.16 μM。AChE/BuChE-IN-2 抑制显示出对自诱导的β-淀粉样蛋白(Aβ)聚集的有效抑制,IC50为 62.52 μM,并且与 AChE 具有非竞争性抑制作用。 | |||
T63152 | |||
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) 是一种 ATP 竞争性的、选择性的第二代细胞周期检测点激酶 1 (CHK1) 抑制剂 (IC50<1 nM, Ki: 0.9 nM)。Prexasertib Mesylate Hydrate 对 CHK2 (IC50: 8 nM) 和 RSK1 (IC50: 9 nM) 表现出抑制作用。Prexasertib Mesylate Hydrate 能够导致双链 DNA 断裂和复制突变,诱导细胞凋亡,并表现出有效的抗肿瘤作用。 | |||
T73436 | |||
AK-IN-1(化合物 4072-2732)是针对腺苷(Ado)具有竞争性抑制作用而对 ATP 不产生竞争性抑制作用的腺苷激酶(AK)抑制剂。在浓度为 2, 4, 10 µM 的条件下,AK-IN-1 能够分别抑制 86%、87% 和 89% 的 AK 活性。该化合物在包括缺血、炎症和癫痫发作在内的多种疾病研究领域展示出了良好的潜力。 | |||
T80253 | |||
S3 Fragment 是具有生物活性的肽,含有 ADF/cofilin 的特异性 N-端磷酸化位点,即 LIM 激酶(LIMK)的靶点。LIMK1 通过在 ADF/cofilin 的丝氨酸 3 位磷酸化来失活该蛋白,是肌动蛋白细胞骨架重要调控因子。该肽段包含 ADF/cofilin 丝氨酸 3 位点,作为 LIMK1 的有效竞争性抑制剂而被广泛研究。 | |||
T76565 | |||
PDC31 (THG113.31; ILGHXDYK) 是FPProstaglandin Receptor 的变构和非竞争性抑制剂。PDC31是基于D-氨基酸的寡肽,用作平滑肌收缩剂。PDC31 在体内降低子宫收缩的强度和持续时间,可用于早产和原发性痛经 (PD) 的研究。PDC31 还增强人子宫肌层细胞中 Ca2+依赖性大电导 K+通道。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPJ-00473 | QPRTase Protein, Human, Recombinant (His) | Human | E. coli | ||
Nicotinate-Nucleotide Pyrophosphorylase (QPRT) belongs to the nadC/modD family. QPRT plays an improtant role in catabolism of quinolinate which acts as a potent endogenous exitotoxin to neurons. In addition, QPRT serves as an an intermediate in the Tryptophan-Nicotinamide Adenine Dinucleotide pathway. QPRT participates in some pathways including Cofactor biosynthesis, NAD(+) biosynthesis and the Nicotinate D-Ribonucleotide from Quinolinate. In addition, QPRT is involved in the catabolism of Quinolinic Acid (QA). The activity toward QA is slightly repressed by phosphoribosylpyrophosphate (PRPP) in both a competitive and a non-competitive manner.
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TMPH-00893 | AHCY Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Adenosylhomocysteine is a competitive inhibitor of S-adenosyl-L-methionine-dependent methyl transferase reactions; therefore adenosylhomocysteinase may play a key role in the control of methylations via regulation of the intracellular concentration of adenosylhomocysteine. AHCY Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 63.6 kDa and the accession number is P23526.
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TMPK-00839 | ITGB6 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
ITGB6 is known to be one of the major receptor components involved in host tropism of foot-and-mouth disease (FMD) virus in cattle. A competitive PCR technique called ARMS PCR was adapted to identify a single-nucleotide polymorphism (SNP), G29A, db SNP Id: rs109075046, in the 5' untranslated region (5'UTR) of the bovine ITGB6 gene. ITGB6 Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 75.4 kDa and the accession number is P18564-1.
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TMPK-01247 | ITGB6 Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
ITGB6 is known to be one of the major receptor components involved in host tropism of foot-and-mouth disease (FMD) virus in cattle. A competitive PCR technique called ARMS PCR was adapted to identify a single-nucleotide polymorphism (SNP), G29A, db SNP Id: rs109075046, in the 5' untranslated region (5'UTR) of the bovine ITGB6 gene. ITGB6 Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 75.7 kDa and the accession number is Q9Z0T9.
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TMPH-00227 | Beta-casein Protein, Bovine, Recombinant (His & Myc) | Bovine | E. coli | ||
Important role in determination of the surface properties of the casein micelles.; Casoparan acts as a macrophage activator, increasing the phagocytic activity of macrophages and peroxide release from macrophages. It also acts as a bradykinin-potentiating peptide.; Casohypotensin acts as a bradykinin-potentiating peptide. Induces hypotension in rats. Acts as a strong competitive inhibitor of endo-oligopeptidase A.; Antioxidant peptide has antioxidant activity. Beta-casein Protein, Bovine, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 28.6 kDa and the accession number is P02666.
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TMPH-02941 | MAFK Protein, Mouse, Recombinant (His & Myc & SUMO) | Mouse | E. coli | ||
Since they lack a putative transactivation domain, the small Mafs behave as transcriptional repressors when they dimerize among themselves. However, they act as transcriptional activators by dimerizing with other (usually larger) basic-zipper proteins, such as NFE2, NFE2L1/NRF1, NFE2L2/NRF2 and NFE2L3/NRF3, and recruiting them to specific DNA-binding sites. Small Maf proteins heterodimerize with Fos and may act as competitive repressors of the NF-E2 transcription factor. MAFK Protein, Mouse, Recombinant (His & Myc & SUMO) is expressed in E. coli expression system with N-10xHis-SUMO and C-Myc tag. The predicted molecular weight is 37.5 kDa and the accession number is Q61827.
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TMPH-02940 | MAFK Protein, Mouse, Recombinant (His & Myc) | Mouse | HEK293 Cells | ||
Since they lack a putative transactivation domain, the small Mafs behave as transcriptional repressors when they dimerize among themselves. However, they act as transcriptional activators by dimerizing with other (usually larger) basic-zipper proteins, such as NFE2, NFE2L1/NRF1, NFE2L2/NRF2 and NFE2L3/NRF3, and recruiting them to specific DNA-binding sites. Small Maf proteins heterodimerize with Fos and may act as competitive repressors of the NF-E2 transcription factor. MAFK Protein, Mouse, Recombinant (His & Myc) is expressed in HEK293 mammalian cells with N-10xHis and C-Myc tag. The predicted molecular weight is 21.5 kDa and the accession number is Q61827.
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TMPJ-01309 | PKI-Beta Protein, Human, Recombinant (His) | Human | E. coli | ||
cAMP-Dependent Protein Kinase Inhibitor β (PKI-β) is a member of the PKI family. As a member of the cAMP-dependent protein kinase inhibitor family,It has been shown that PKI-β is an extremely potent competitive inhibitor of cAMP-dependent protein kinase activity; this protein interacts with the catalytic subunit of the enzyme after the cAMP-induced dissociation of its regulatory chains. It may play a role in the protein kinase A (PKA) pathway by interacting with the catalytic subunit of PKA, and overexpression of this gene may play a role in prostate cancer.
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TMPY-01769 | 4EBP1 Protein, Human, Recombinant (His) | Human | E. coli | ||
The translational suppressor eIF4E binding protein-1, 4E-BP1 functions as a key regulator in cellular growth, differentiation, apoptosis and survival. The Eif4ebp1 gene, encoding 4E-BP1, is a direct target of a transcription factor activating transcription factor-4 (ATF4), a master regulator of gene expression in stress responses. 4E-BP1 is characterized by its capacity to bind specifically to eIF4E and inhibit its interaction with eIF4G. Phosphorylation of 4E-BP1 regulates eIF4E availability, and therefore, cap-dependent translation, in cell stress. Binding of eIF4E to eIF4G is inhibited in a competitive manner by 4E-BP1. Phosphorylation of 4E-BP1 decreases the affinity of this protein for eIF4E, thus favouring the binding of eIF4G and enhancing translation. 4E-BP1 is important for beta-cell survival under endoplasmic reticulum (ER) stress. 4E-BP1 mediates the regulation of protein translation by hormones, growth factors and other stimuli that signal through the MAP kinase and mTORC1 pathways. Recently, 4E-BP1 was found to be a key factor, which converges several oncogenic signals, phosphorylates the molecules, and drives the downstream proliferative signals. Recent studies showed that high expression of phosphorylated 4E-BP-1 (p-4E-BP1) is associated with poor prognosis, tumor progression, or nodal metastasis in different human cancers.
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