T27395
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Furamidine is a cell-permeable, selective inhibitor of protein arginine methyltransferase 1 (PRMT1). Furamidine binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine targets the enzyme active site and is primarily competitive with t |
T16011
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Prostaglandin Receptor
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Manumycin A is an antibiotic. Manumycin A induces apoptosis and exerts antitumor activity. Manumycin A inhibits exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A acts as a selective, competitive inhibitor of |
T75318
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Spectinomycin 是广谱性抗生素,能够抑制多种革兰氏阳性及阴性细菌生长。其机制为特异性靶向细菌核糖体,干扰蛋白质合成。Spectinomycin 同时作为 td 内含子 RNA 的非竞争性抑制剂。 |
T73336
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Ketotifen (HC 20-511)为第二代口服活性非竞争性组胺1(H1)受体阻滞剂兼肥大细胞稳定剂,能体外阻断6-磷酸葡萄糖酸脱氢酶(6-PGD)。其对SARS-CoV-2及流感病毒(Influenza virus)展现出抗病毒活性,适用于自身免疫性脑脊髓炎(EAE)与哮喘发作预防研究。 |
T61891
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SHP2-IN-8 是一种可逆、非竞争性、选择性、高效性的变构SHP2抑制剂(IC50= 23 nM,Ki= 22 nM),在细胞中也有效果。SHP2-IN-8 能引起显著的热位移(ΔTm = 7.01 ℃)。SHP2-IN-8 可抑制AKT 的磷酸化,诱导 Hela 细胞凋亡 (apoptosis)。 |
T78140
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Others
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ELOVL6-IN-1是一种具有高效、口服生物活性和选择性的ELOVL6抑制剂。该化合物针对小鼠ELOVL6展现剂量依赖性抑制,IC50为0.350 μM,并且对丙二酰辅酶a(Ki=994 nM)具有非竞争性抑制ELOVL6的活性,以及对棕榈酰辅酶a同样显示非竞争性抑制作用。 |
T80175
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Adrenergic Receptor
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Conopeptide rho-TIA为从掠食性海螺Conus tulipa毒液中提炼的多肽,对人类α1B-Adrenergic Receptor呈现非竞争性抑制作用,同时对α1A-Adrenergic Receptor和α1D-Adrenergic Receptor表现出竞争性抑制。Conopeptide rho-TIA与这些亚型的结合特性可能对开发针对α1-Adrenergic Receptor亚型的选择性新药具有参考价值。 |
T61454
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α-NETA是一种有效的胆碱乙酰转移酶(ChA)非竞争性抑制剂,IC50值为9μM。同时,它也是ALDH1A1(IC50=0.04μM)和趋化因子样受体1(CMKLR1)的有效拮抗剂。此外,α-NETA对胆碱酯酶(ChE; IC50=84μM)和乙酰胆碱酯酶(AChE; IC50=300μM)的抑制作用较弱。α-NETA亦显示出抗癌活性。 |
T79700
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Glucosidase
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α-Glucosidase-IN-32 (compound f26),是一种口服有效的α-glucosidase抑制剂,具有可逆、非竞争性特点,IC50值为3.07 μM。该化合物通过与α-glucosidase形成氢键和疏水相互作用,以改变其构象和二级结构,从而抑制酶活性。α-Glucosidase-IN-32 主要用于糖尿病研究。 |
T37106
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2'-Deoxyadenosine-5'-triphosphate (dATP) is a purine nucleotide and derivative of the nucleic acid adenosine 5'-triphosphate .1dATP is a substrate for DNA polymerase in the synthesis of DNA.2It is a noncompetitive inhibitor of ribonucleotide reductases, which provides feedback inhibition during DNA synthesis.1dATP has commonly been used in DNA synthesis, sequencing, and labeling in research applications.3,4dATP accumulates in adenosine deaminase deficiency, a disorder characterized by mutations in the gene for adenosine deaminase, the enzyme that catalyzes the deamination of adenosine and deoxyadenosine.5
1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Key steps in nucleotide biosynthesis are regulated by feedback inhibitionBiochemistry(2002) 2.Berg, J.M., Tymoczko, J.L., and Stryer, L.DNA is replicated by polymerases that take instructions from templatesBiochemistry(2002) 3.Cadwell, R.C., and Joyce, G.F.Randomization of genes by PCR mutagenesisPCR Methods Appl.2(1)28-33(1992) 4.Steffens, D.L., Jang, G.Y., Sutter, S.L., et al.An infrared fluorescent dATP for labeling DNAGenome Res.5(4)393-399(1995) 5.Flinn, A.M., and Gennery, A.R.Adenosine deaminase deficiency: A reviewOrphanet J. Rare Dis.13(1)65(2018) |