目录号 | 产品详情 | 靶点 | |
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T36205 | |||
Methylcarbamyl PAF C-16 is a stable analog of PAF C-16 with a half-life greater than 100 minutes in platelet poor plasma due to its resistance to degradation by PAF-AH. It is nearly equipotent with PAF C-16 in its ability to induce platelet aggregation both in isolated platelets and in platelet-rich plasma. In NRK-49 cells overexpressing the PAF receptor, both PAF C-16 and methylcarbamyl PAF C-16 cause the induction of c-myc and c-fos and the activation of mitogen-activated protein kinase. Methylcarbamyl PAF C-16 induces G1 phase cell cycle arrest, suggesting a potential role for PAF in the inhibition of oncogenic transformation. | |||
T36404 | |||
PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM. PRLX-93936 inhibits tumor growth in PANC-1 and HT-1080 xenograft models when administered at a dose of 50 mg/kg and induces tumor regression when administered at a dose of 100 mg/kg. | |||
T37996 | |||
17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to increase lipid solubility, thereby improving uptake into tissues and further lowering the effective concentration. Ethyl amide groups are then removed by amidases, regenerating the active free acid. | |||
T83236 | |||
8-Azido-cAMP作为一种cAMP荧光模拟物,用于作为检测cAMP模式靶点的应用。该化合物是点击化学试剂,拥有Azide基团,能够通过铜催化的叠氮-炔环加成反应(CuAAc)与含Alkyne基团的分子发生反应。此外,它也能通过菌株促进的炔-叠氮环加成反应(SPAAC)与含有DBCO或BCN基团的分子进行反应。 | |||
T69731 | |||
Remdesivir, also known as GS-5734, is a prodrug form of the antiviral nucleoside analog GS-44152. Remdesivir is a broad spectrum anti-viral drug that has shown to inhibit SARS-CoV-2, in vitro and in vivo. Efficacy of remdesivir against Ebola virus has been demonstrated. Remdesivir inhibits SARS-CoV-2 replication, reduces viral load, and exerts protective effects in SARS-CoV-2 infected animals. Remdesivir also reduces the pathological process, alleviates mild symptoms, and improves pulmonary lesions in SARS-CoV-2-infecetd animals. Remdesivir has been used as a compassionate drug for treating COVID-19 patients. *******WARNING****** Our product remdesivir is a pure chemical solid powder which is only for laboratory research use, NOT FOR HUMAN OR PATIENT USE | |||
T8996 | |||
AQX-016A 是一种口服有效的 SHIP1激动剂。AQX-016A 是 Pelorol 的结构类似物,在相同摩尔浓度下,其效力是海洋天然产物 Pelorol 的 3 倍。AQX-016A 可以在体外激活重组 SHIP1酶并刺激 SHIP1活性。AQX-016A 还可抑制 PI3K 通路和 TNFa 的产生,可用于各种炎症疾病的研究。 | |||
T73665 | |||
Bufrolin,作为Cromoglycate(组胺释放抑制剂)的类似物,是一种高效的GPR35激动剂,能够促进β-arrestin-2与人GPR35a或大鼠GPR35之间的相互作用。此外,Bufrolin亦可作为抗过敏性肥大细胞稳定剂,有效抑制内化肽诱导的抗炎反应,并且在内化肽连接药剂的药物递送研究中,被作为抗炎剂使用。 | |||
T36464 | |||
Nutlin-3 is an activator of p53 that functions by inhibiting the interaction of p53 with MDM2, a negative regulator of p53 activity. Caylin-1 is a nutlin-3 analog which contains chlorine substituents at the 3 and 4 positions on two of the phenyl rings rather than a single 4-chloro as seen in nutlin-3. At high concentrations, caylin-1 inhibits the growth of HCT116 cells with an IC50 value of approximately 7 μM, making it about 7-fold less potent than nutlin-3 in the same assay. Interestingly, at concentrations at or below 1 μM, caylin-1 promotes the growth of HCT116 cells approximately 20% compared to untreated cells. The mechanism of the growth promoting properties of caylin-1 have not yet been elucidated. | |||
T37496 | |||
Alamandine can be formed from angiotensin A by action of ACE-2 or directly from angiotensin-(1-7) by decarboxylation of its aspartate residue. The angiotensin A analog produces effects resembling those of Ang II (1-7). However, it acts independently of the two known vasodilators receptors of the RAS (Mas and angiotensin II type 2). To produce its effects, alamandine binds to the Mas-related receptor, MrgD. A novel orally active formulation of alamandine produced a long-term antihypertensive effect in spontaneously hypertensive rats and cardioprotective effects. These novel findings will be helpful for developing a new understanding of the RAS, a key regulator of blood pressure and fluid balance. The heptapeptide could serve as a model peptide, e.g. in the development and evaluation of analytical methods. | |||
T37684 | |||
Anandamide (arachidonoyl ethanolamide; AEA) is an endogenous lipid with cannabinergic activity; along with 2-arachidonoyl glycerol, it forms part of the endocannabinoid system. AEA undergoes reuptake into neurons by a facilitated process. Controversy exists as to whether there is a specific AEA transporter, or instead the uptake process is simply driven by hydrolysis of AEA by intracellular fatty acyl amide hydrolase (FAAH). CAY10412 is an analog of AEA that has no intrinsic binding affinity for either CB1 or CB2 receptors. It is a potent inhibitor of AEA reuptake in U937 lymphoma cells, with an IC50 of 3 μM. CAY10412 could be a useful tool for distinguishing the competing transporter theories. The pharmacology of CAY10412 is largely unexplored; it may enhance endocannabinoid signalling by augmenting endocannabinoid concentrations. |
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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