目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T37937 | |||
Prostaglandin F2α (PGF2α) drives luteolysis and smooth muscle contraction by activating the FP receptor. Stable, lipophilic analogs of PGF2α are used to modulate luteolysis and treat glaucoma. 16-phenoxy tetranor Prostaglandin F2α (16-phenoxy tetranor PGF2α) is a metabolically stable form of PGF2α containing a 16-phenoxy group at the ω-terminus. It binds to the FP receptor on ovine luteal cells with much greater affinity (440%) than PGF2α. 16-phenoxy tetranor PGF2α methyl ester is a lipophilic analog of 16-phenoxy tetranor PGF2α. Methyl esters of PGs serve as prodrugs, as they are efficiently hydrolyzed in certain tissues to generate the bioactive free acid. | |||
T75837 | |||
Spantide I TFA 是substance P 的类似物,是选择性的神经激肽-1 受体 (NK1receptor) 的拮抗剂,其对NK1和NK2受体的Ki 值分别为 230 nM 和8150 nM。Spantide I 可减少感染角膜的1型细胞因子和增强2型细胞因子IL-10,从而显著减少角膜穿孔。 | |||
T61938 | |||
vibsanin A 类似物 C(VAC)是一种抗癌化合物,对各种癌细胞系显示出抗增殖作用,且抗增殖活性在 vibsanin A 类似物中较强。VAC 使细胞中 HSP90相关蛋白的量波动,并显示出对 HSP90介导的荧光素酶体外蛋白重折叠的抑制作用。 | |||
T5499 | |||
Gardiquimod diTFA,咪唑啉类似物TLR7/8激动剂,可特异性抑制巨噬细胞和活化外周血单个核细胞(PBMCs)的HIV-1感染。在浓度低于10 μM时,该化合物特异性激活TLR7。 | |||
T60341 | |||
Pyruvate Carboxylase-IN-1 (compound 37) 是一种有效的丙酮酸羧化酶(PC) 抑制剂,对于基于细胞裂解物和基于细胞的 PC 活性,IC50s 分别为 0.204 和 0.104 μM。Pyruvate Carboxylase-IN-1 是毛兰素的天然类似物。Pyruvate Carboxylase-IN-1 抑制 PC 的酶活性,介导人肝细胞癌 (HCC) 的抗癌作用。 | |||
T68667 | |||
Oxanosine is an analog of guanosine that has been found in S. capreolus and has diverse biological activities, including antibacterial, antiviral, and anticancer properties. It is active against a variety of bacteria, including S. flexneri, P. mirabilis, and E. coli (MICs = 6.25, 12.5, 25 µg/ml, respectively, on peptone, but not nutrient, agar). Oxanosine inhibits replication of the HIV-1 strain IIIb in infected CEM and U937, but not H9, cells (EC50s = 7, 27, and >500 µg/ml, respectively). It also inhibits the growth of HeLa human cervical cancer cells (IC50 = 32 µg/ml) and reduces tumor growth in a murine L1210 lymphocytic leukemia model. | |||
T36999 | |||
Novel oxylipins, referred to as docosanoids, have been derived from C22polyunsaturated fatty acids 7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic acid (7(S),17(S)-hydroxy DPA) is a DPA-derived analog of the 17(S)-dihydroxy series of docosanoids known as protectins. Protectin D1, a DHA-derived dihydroxy fatty acid, exhibits potent anti-inflammatory activities.1,2,3Potentially, 7(S),17(S)-hydroxy DPA demonstrates similar properties; however, its biological activity has yet to be determined. 1.Serhan, C.N., Gotlinger, K., Hong, S., et al.Anti-inflammatory actions of neuroprotectin D1/protectin D1 and its natural stereoisomers: Assignments of dihydroxy-containing docosatrienesJ. Immunol.176(3)1848-1859(2006) 2.Ariel, A., and Serhan, C.N.Resolvins and protectins in the termination program of acute inflammationTRENDS in Immunology28(4)176-183(2007) 3.Schwab, J.M., Chiang, N., Arita, M., et al.Resolvin E1 and protectin D1 activate inflammation-resolution programmesNature447(7146)869-874(2007) | |||
T36829 | |||
9-deoxy-9-methylene-16,16-dimethyl Prostaglandin E2 (Meteneprost) is a potent analog of prostaglandin E2 with an extended half-life in vivo. In combination with various other prostaglandin derivatives, it results in the termination of first trimester pregnancy in monkeys. A single intramuscular injection containing 0.5 mg of meteneprost and 7.5 mg of 17-phenyl trinor PGF1α is very effective in terminating early pregnancy. This prostaglandin mixture is ineffective on monkeys in their third trimester of pregnancy. Meteneprost, when compared to PGE2 and PGF1α, in monkey and rat, does not result in unwanted side effects such as fever or gastrointestinal problems. | |||
T75804 | |||
K41498 TFA 是一种强选择性的CRF2 receptor 拮抗剂,其对人 CRF2α、CRF2β和 CRF1受体的Ki 值分别为 0.66 nM、0.62 nM 和425 nM。K41498 TFA 是 antisauvagine-30 (aSvg-30) 的类似物,可抑制 sauvagine 刺激的 cAMP 在 hCRF2α/hCRF2β表达细胞中的积累。K41498 可用于低血压研究。 | |||
T61961 | |||
Pyruvate Carboxylase-IN-2 是毛兰素的天然类似物。Pyruvate Carboxylase-IN-2 (compound 29) 是有效的丙酮酸羧化酶(pyruvate carboxylase) 抑制剂。在基于细胞裂解物和基于细胞的 PC 活性中,Pyruvate Carboxylase-IN-2的 IC50s 分别为 0.065 和 0.097 μM。Pyruvate Carboxylase-IN-2介导人肝细胞癌 (HCC) 的抗癌作用。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
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.
|
|||||
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.
|
|||||
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.
|
|||||
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.
|