目录号 | 产品详情 | 靶点 | |
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T71230 | |||
VMY-1-103 is a potent CDK inhibitor, is also a novel dansylated analog of purvalanol B, was shown to inhibit cell cycle progression and proliferation in prostate and breast cancer cells more effectively than purvalanol B. VMY-1-103 , but not purvalanol B, significantly decreased the proportion of cells in S phase and increased the proportion of cells in G(2)/M. VMY-1-103 increased the sub G(1) fraction of apoptotic cells, induced PARP and caspase-3 cleavage and increased the levels of the Death Receptors DR4 and DR5, Bax and Bad while decreasing the number of viable cells, all supporting apoptosis as a mechanism of cell death. VMY-1-103 possesses unique antiproliferative capabilities and that this compound may form the basis of a new candidate drug to treat medulloblastoma. | |||
T36015 | |||
PDMP is a ceramide analog first prepared in a search for inhibitors of glucosylceramide synthase. PDMP has two adjacent chiral centers (C1 and C2) allowing for the formation of four possible isomers. PDMP contains all four of these stereoisomers. PDMP inhibits glucosylceramide synthase by 90% when used at a concentration of 0.8 μM in MDCK cell homogenates, however, the ability to inhibit glucosylceramide synthase has been found to reside in the D-threo (1R,2R) enantiomer. The D-threo PDMP enantiomer is also responsible for inhibition of β-1,4-galactosyltransferase 6 and prevention of lactosylceramide synthesis, which is a promotor of neuroinflammation in mice during chronic experimental autoimmune encephalomyelitis (EAE), a model of multiple sclerosis. PDMP enhances curcumin-induced inhibition of proliferation, JNK activation, and Akt inhibition, as well as induction of apoptosis in WM-115 melanoma cells in vitro. | |||
T38156 | |||
N-Acetyl-DL-penicillamine is a chelating agent.1,2,3It inhibits the binding of methyl mercury to isolated human erythrocytes by 50% and removes 50% of methyl mercury ions from methyl mercury-loaded blood cells when used at a concentration of 1 mM.1,2N-Acetyl-DL-penicillamine (3 mmol/kg per day, p.o.) reduces the biological half-life of mercury and decreases liver, kidney, brain, and blood mercury levels, as well as increases urinary excretion of mercury in a concentration-dependent manner, in mice when administered following injection of methyl mercuric chloride. It decreases mercuric chloride-induced mortality in mice when administered orally at a dose of 1.6 mmol/kg.3N-Acetyl-DL-penicillamine is also an analog of SNAP that does not generate nitric oxide and has been used as a negative control in experiments using SNAP.4,5 | |||
T74467 | |||
Remdesivir de(ethylbutyl 2-aminopropanoate) 是 Remdesivir 的一种杂质,后者为一种具有抗病毒活性的核苷类似物。在 HAE 细胞针对 SARS-CoV 和 MERS-CoV 的实验中,Remdesivir 的 EC50 值为 74 nM;在针对鼠肝炎病毒的延迟脑肿瘤细胞实验中,其 EC50 值为 30 nM。此外,Remdesivir 亦被认为具有针对 2019-nCoV (COVID-19) 的研究潜力。 | |||
T36947 | |||
Pyrithiamine is the pyridine analog of thiamine that prevents growth of organisms that require intact thiamine. [1] It inhibits the growth of bacterial and fungal species at a pyrithiamine:thiamine ratio of 10:1 in growth media and induces symptoms of thiamine deficiency in mice at a dietary ratio of 3:1. These effects are reversible with addition of sufficient thiamine in all species. Pyrithiamine inhibits the formation of cocarboxylase from thiamine in chicken blood in a dose-dependent manner. [2] It has been used to induce thiamine deficiency in various disease models, including rat models of alcoholism and diencephalic amnesia, to study the effects of thiamine deficiency on disease pathology.[3] [4] Reference:[1]. Woolley, D.W., and White, A.G.C. Selective reversible inhibition of microbial growth with pyrithiamine. J. Exp. Med. 78(6), 489-497 (1943).[2]. Woolley, D.W. An enzymatic study of the mode of action of pyrithiamine (neopyrithiamine). J. Biol. Chem. 191(1), 43-54 (1951).[3]. Vetreno, R.P., Anzalone, S.J., and Savage, L.M. Impaired, spared, and enhanced ACh efflux across the hippocampus and striatum in diencephalic amnesia is dependent on task demands. Neurobiol. Learn Mem. 90(1), 237-244 (2008).[4]. Zahr, N.M., Sullivan, E.V., Rohlfing, T., et al. Concomitants of alcoholism: Differential effects of thiamine deficiency, liver damage, and food deprivation on the rat brain in vivo. Psychopharmacology (Berl) 233(14), 2675-2686 (2016). | |||
T76047 | |||
TAK-683 TFA是一种高效的全KISS1R激动剂(IC50=170 pM),拥有较好的代谢稳定性,是九肽metastin的类似物,对KISS1R有激动效应,其对人和大鼠EC50值分别为0.96 nM和1.6 nM。TAK-683 TFA能够降低下丘脑GnRH水平,进而减少血浆FSH、LH、睾酮的浓度,显示出对激素依赖性前列腺癌研究的可能性。 | |||
T62582 | |||
WEHI-150是一种米托蒽醌类似物,作为DNA链间交联剂,具有12.5小时的半衰期。该化合物能够在CpG序列上形成共价加合物,对甲基化CpG位点表现出选择性。甲醛激活的WEHI-150能够诱导DNA链间交联,并表现出浓度依赖性的转录阻断作用。此外,WEHI-150还能在新的DNA序列中形成加合物,这不涉及与鸟嘌呤N-2的相互作用。 | |||
T69994 | |||
BIM-46050 is a potent and specific inhibitor of human farnesyltransferase. BIM-46050 is free acidic form of BIM-46068. The IC50 values for in vitro inhibition of human brain FTase indicate that BIM-46050 and the ester form BIM-46068 are potent inhibitors of farnesyltransferase. Their potencies are in the nanomolar range and compare favorably with the compounds B581, FTI-277 and L745,631. B581 is an analog of the tetrapeptide Cys-Val-Phe-Met obtained by replacement of the amino-terminal amide bonds inhibiting processing of farnesylated proteins specifically. FTI-277 is a methyl ester of FTI-276, reported as a preferential inhibitor of FTase over GGTase I (100-fold). L745,631 is a 2-substituted piperazine reported to be a highly selective inhibitor of FTase over GGTase (2,000-fold). The selectivity of BIM-46050 and BIM-46068 for FTase over GGTase is very similar for both compounds (3,000-fold). | |||
T35491 | |||
PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K/Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB/c mice with a dose of 1 mg/kg of 3,5-dimethyl PIT-1 per day. | |||
T75074 | |||
6-Methoxypurine-9-β-D-5’(R)-C-methylriboside 是一种嘌呤碱基,属于次黄嘌呤似物,主要在肌肉组织中发现。作为黄嘌呤在嘌呤氧化酶作用下的代谢产物,次黄嘌呤具备显著的抗炎性质,并可作为内源性 poly(ADP-ribose) polymerase (PARP) 的抑制剂。其通过抑制 PARP 活性,防止过氧亚硝酸盐引起的线粒体去极化及次级超氧化物的产生,展现出细胞保护作用。同时,次黄嘌呤也被用作缺氧的生物标志物。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-03036 | Cytotoxin 2 Protein, Naja atra, Recombinant (His & Myc) | Naja atra | E. coli | ||
Basic protein that binds to cell membrane and depolarizes cardiomyocytes. It also shows lytic activities, but 2-fold less important than that of CTX-A4. It binds to the integrin alpha-V/beta-3 (ITGAV/ITGB3) with a moderate affinity. It may interact with sulfatides in the cell membrane which induces pore formation and cell internalization and is responsible for cytotoxicity in cardiomyocytes. It also may target the mitochondrial membrane and induce mitochondrial swelling and fragmentation.
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TMPH-00645 | Lactose permease Protein, E. coli, Recombinant (His) | E. coli | E. coli | ||
Responsible for transport of beta-galactosides into the cell, with the concomitant import of a proton (symport system). Can transport lactose, melibiose, lactulose or the analog methyl-1-thio-beta,D-galactopyranoside (TMG), but not sucrose or fructose. The substrate specificity is directed toward the galactopyranosyl moiety of the substrate. Lactose permease Protein, E. coli, Recombinant (His) is expressed in E. coli expression system with N-10xHis tag. The predicted molecular weight is 34.4 kDa and the accession number is P02920.
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TMPJ-00871 | BAR Protein, S. hygroscopicus, Recombinant | Streptomyces hygroscopicus | E. coli | ||
Phosphinothricin N-acetyltransferase (PAT) is an enzyme that acetylates the free NH2 group of L-phosphinothricin (L-PPT) in the presence of acetyl-CoA as a co-substrate. It is highly specific for L-PPT and does not acetylate other L-amino acids or structurally similar molecules. L-PPT is a glutamate analog that can inhibit glutamine synthetase activity in plants, resulting in the accumulation of ammonia to toxic levels and impairment of photosynthesis. The introduction of a PAT gene into a plant genome can confer resistance to glufosinate herbicide during post-emergent applications.
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TMPH-03038 | Cobra venom factor Protein, Naja kaouthia, Recombinant (His & SUMO) | Naja kaouthia | E. coli | ||
Complement-activating protein in cobra venom. It is a structural and functional analog of complement component C3b, the activated form of C3. It binds factor B (CFB), which is subsequently cleaved by factor D (CFD) to form the bimolecular complex CVF/Bb. CVF/Bb is a C3/C5 convertase that cleaves both complement components C3 and C5. Structurally, it resembles the C3b degradation product C3c, which is not able to form a C3/C5 convertase. Unlike C3b/Bb, CVF/Bb is a stable complex and completely resistant to the actions of complement regulatory factors H (CFH) and I (CFI). Therefore, CVF continuously activates complement resulting in the depletion of complement activity.
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