目录号 | 产品详情 | 靶点 | |
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T14943 | VEGFR CDK PKC | ||
CGP60474 是一种高效的抗内毒素药物,抑制细胞周期蛋白依赖激酶(CDK) ,抑制 CDK1/B、CDK2/E、CDK2/a、CDK4/D、CDK5/p25、CDK7/H 和 CDK9/T 的IC50分别为 26、3、4、216、10、200 和 13 nM。它是选择性和 ATP 竞争性PKC 抑制剂。 | |||
T7304 | GluR iGluR | ||
DNQX (FG 9041) 是喹恶啉衍生物,是一种选择性和强竞争性的非 NMDA 谷氨酸受体拮抗剂,对 AMPA、kainate 和 NMDA 受体的IC50分别为 0.5、2 和 40 μM。 | |||
T2850 | GABA Receptor | ||
Bicuculline ((+)-Bicuculline) 是从东北延胡索中提取的一种生物碱,能阻断 Ca2+激活钾 (SK) 通道。它是一种竞争性的神经递质 GABAA 受体拮抗剂,IC50为 2 μM。 | |||
T38862 | Others | ||
Nandrolone acetate (19-Nortestosterone 17β-acetate) 是一种甾体酮,是异构酶的竞争性抑制剂,对Δ5-3-酮甾体异构酶的 Ki 为 7 μM。 | |||
T7673 | Apoptosis FLT | ||
ATH686 是一种选择性的,ATP 竞争性的FLT3抑制剂,具有抗白血病作用。它靶向突变 FLT3 蛋白激酶活性,并通过诱导凋亡和抑制细胞周期来抑制具有 FLT3 突变的细胞的增殖。 | |||
T7322 | EGFR | ||
Theliatinib 是一种ATP 竞争性、口服活性和高度选择性的EGFR 抑制剂,Ki 为 0.05 nM,IC50为 3 nM。它具有抗肿瘤活性,对EGFR T790M/L858R 突变体的IC50值为 22 nM。它对EGFR 的选择性是其他激酶的 50 倍以上。 | |||
T5125 | TGF-beta/Smad | ||
LY3200882 是一种高度选择性的、口服活性的、具有 ATP 竞争性的 TGF-β 受体 1 型 (ALK5) 抑制剂(IC50:38.2 nM)。它能够抑制多种促肿瘤活性,可用作免疫调节剂。 | |||
T6685 | Antibacterial Antibiotic | ||
Sulbactam sodium (CP-45899-2) 是一种竞争性、不可逆的 β-内酰胺酶抑制剂。它具有抗菌活性,抑制耐多药不动杆菌-鲍曼不动杆菌复合物。 | |||
T23524 | AChR | ||
W-84 dibromide (HDMPPA) 是 M2胆碱受体的强变构调节剂,是一种非竞争性毒蕈碱乙酰胆碱受体拮抗剂,具有变构效应。它联合阿托品时,可有效地防止有机磷中毒。它阻碍 [3H]N-甲基东莨菪碱解离,能稳定胆碱能拮抗剂-受体复合物。 | |||
TN2004 | MAO Monoamine Oxidase | ||
Obtusin 是来自决明子种子,是一种高度选择性和竞争性的人单胺氧化酶-A 抑制剂,IC50=11.12 μM,Ki=6.15 μM。它在神经退行性疾病,尤其是焦虑和抑郁中起预防作用。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-01369 | AGRP Protein, Human, Recombinant (His) | Human | HEK293 | ||
Agouti Related Protein (AGRP, or AGRT), is an endogenous antagonist of the melanocortin receptors MC3R and MC4R found in the hypothalamus and exhibits potent orexigenic activity. AGRP can act as a competitive antagonist to proopiomelanocortin (POMC)-derived peptides at the melanocortin-4 receptor (MC4R), and that this homeostatic mechanism is important as a means of coordinating appetite with perceived metabolic requirement. AGRP is upregulated by fasting while intracerebroventricular injections of synthetic AGRP lead to increased appetite and food intake. Thus, AGRP is a powerful orexigenic peptide that increases food intake when ubiquitously overexpressed or when administered centrally.
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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.
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TMPK-00750 | KLRG1 Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 | ||
Immune homeostasis requires the tight, tissue-specific control of the different CD4 Foxp3 regulatory T (Treg) cell populations. The cadherin-binding inhibitory receptor killer cell lectin-like receptor G1 (KLRG1) is expressed by a subpopulation of Treg cells with GATA3 effector phenotype.Lack of KLRG1 on Treg cells conferred on them a competitive advantage in the gut, but not in lymphoid organs. Hence, although absence of KLRG1 is not enough to increase intestinal Treg cells in KLRG1 knockout mice, KLRG1 ligation reduces T-cell receptor signals and the competitive fitness of individual Treg cells in the intestine.
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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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TMPK-01140 | KLRG1 Protein, Human, Recombinant (hFc) | Human | HEK293 | ||
Immune homeostasis requires the tight, tissue-specific control of the different CD4 Foxp3 regulatory T (Treg) cell populations. The cadherin-binding inhibitory receptor killer cell lectin-like receptor G1 (KLRG1) is expressed by a subpopulation of Treg cells with GATA3 effector phenotype.Lack of KLRG1 on Treg cells conferred on them a competitive advantage in the gut, but not in lymphoid organs. Hence, although absence of KLRG1 is not enough to increase intestinal Treg cells in KLRG1 knockout mice, KLRG1 ligation reduces T-cell receptor signals and the competitive fitness of individual Treg cells in the intestine.
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TMPK-00839 | ITGB6 Protein, Human, Recombinant (His) | Human | HEK293 | ||
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.
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TMPK-01247 | ITGB6 Protein, Mouse, Recombinant (His) | Mouse | HEK293 | ||
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.
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TMPH-02940 | MAFK Protein, Mouse, Recombinant (His & Myc) | Mouse | HEK293 | ||
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.
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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.
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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.
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TMPH-01761 | Neuroglobin Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Involved in oxygen transport in the brain. Hexacoordinate globin, displaying competitive binding of oxygen or the distal His residue to the iron atom. Not capable of penetrating cell membranes. The deoxygenated form exhibits nitrite reductase activity inhibiting cellular respiration via NO-binding to cytochrome c oxidase. Involved in neuroprotection during oxidative stress. May exert its anti-apoptotic activity by acting to reset the trigger level of mitochondrial cytochrome c release necessary to commit the cells to apoptosis.
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TMPY-00630 | AGRP Protein, Rhesus, Recombinant (mFc) | Rhesus | HEK293 | ||
Agouti Related Protein (AGRP, or AGRT), is an endogenous antagonist of the melanocortin receptors MC3R and MC4R found in the hypothalamus and exhibits potent orexigenic activity. AGRP can act as a competitive antagonist to proopiomelanocortin (POMC)-derived peptides at the melanocortin-4 receptor (MC4R), and that this homeostatic mechanism is important as a means of coordinating appetite with perceived metabolic requirement. AGRP is upregulated by fasting while intracerebroventricular injections of synthetic AGRP lead to increased appetite and food intake. Thus, AGRP is a powerful orexigenic peptide that increases food intake when ubiquitously overexpressed or when administered centrally.
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TMPY-00661 | AGRP Protein, Human, Recombinant (hFc) | Human | HEK293 | ||
Agouti Related Protein (AGRP, or AGRT), is an endogenous antagonist of the melanocortin receptors MC3R and MC4R found in the hypothalamus and exhibits potent orexigenic activity. AGRP can act as a competitive antagonist to proopiomelanocortin (POMC)-derived peptides at the melanocortin-4 receptor (MC4R), and that this homeostatic mechanism is important as a means of coordinating appetite with perceived metabolic requirement. AGRP is upregulated by fasting while intracerebroventricular injections of synthetic AGRP lead to increased appetite and food intake. Thus, AGRP is a powerful orexigenic peptide that increases food intake when ubiquitously overexpressed or when administered centrally.
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TMPY-00434 | AGRP Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 | ||
Agouti Related Protein (AGRP, or AGRT), is an endogenous antagonist of the melanocortin receptors MC3R and MC4R found in the hypothalamus and exhibits potent orexigenic activity. AGRP can act as a competitive antagonist to proopiomelanocortin (POMC)-derived peptides at the melanocortin-4 receptor (MC4R), and that this homeostatic mechanism is important as a means of coordinating appetite with perceived metabolic requirement. AGRP is upregulated by fasting while intracerebroventricular injections of synthetic AGRP lead to increased appetite and food intake. Thus, AGRP is a powerful orexigenic peptide that increases food intake when ubiquitously overexpressed or when administered centrally.
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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-02269 | AGRP Protein, Mouse, Recombinant (His) | Mouse | HEK293 | ||
Agouti Related Protein (AGRP, or AGRT), is an endogenous antagonist of the melanocortin receptors MC3R and MC4R found in the hypothalamus and exhibits potent orexigenic activity. AGRP can act as a competitive antagonist to proopiomelanocortin (POMC)-derived peptides at the melanocortin-4 receptor (MC4R), and that this homeostatic mechanism is important as a means of coordinating appetite with perceived metabolic requirement. AGRP is upregulated by fasting while intracerebroventricular injections of synthetic AGRP lead to increased appetite and food intake. Thus, AGRP is a powerful orexigenic peptide that increases food intake when ubiquitously overexpressed or when administered centrally.
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TMPH-01092 | CHGA Protein, Human, Recombinant (His) | Human | Yeast | ||
Strongly inhibits glucose induced insulin release from the pancreas.; Inhibits catecholamine release from chromaffin cells and noradrenergic neurons by acting as a non-competitive nicotinic cholinergic antagonist. Displays antibacterial activity against Gram-positive bacteria S.aureus and M.luteus, and Gram-negative bacteria E.coli and P.aeruginosa. Can induce mast cell migration, degranulation and production of cytokines and chemokines. Acts as a potent scavenger of free radicals in vitro. May play a role in the regulation of cardiac function and blood pressure.; Regulates granule biogenesis in endocrine cells by up-regulating the transcription of protease nexin 1 (SERPINE2) via a cAMP-PKA-SP1 pathway. This leads to inhibition of granule protein degradation in the Golgi complex which in turn promotes granule formation.
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TMPH-01885 | PABPC1 Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Binds the poly(A) tail of mRNA, including that of its own transcript, and regulates processes of mRNA metabolism such as pre-mRNA splicing and mRNA stability. Its function in translational initiation regulation can either be enhanced by PAIP1 or repressed by PAIP2. Can probably bind to cytoplasmic RNA sequences other than poly(A) in vivo. Involved in translationally coupled mRNA turnover. Implicated with other RNA-binding proteins in the cytoplasmic deadenylation/translational and decay interplay of the FOS mRNA mediated by the major coding-region determinant of instability (mCRD) domain. Involved in regulation of nonsense-mediated decay (NMD) of mRNAs containing premature stop codons; for the recognition of premature termination codons (PTC) and initiation of NMD a competitive interaction between UPF1 and PABPC1 with the ribosome-bound release factors is proposed. By binding to long poly(A) tails, may protect them from uridylation by ZCCHC6/ZCCHC11 and hence contribute to mRNA stability.; (Microbial infection) Positively regulates the replication of dengue virus (DENV).
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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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