T74934
|
|
|
|
Trypanothione synthetase-IN-3是一种针对Trypanothione synthetase (TryS)的非竞争性混合双曲线抑制剂,其Ki值为0.8 μM。该化合物主要用于研究寄生虫,例如L. infantum。 |
TP1490
|
|
|
|
Endogenous peptide agonist of Mas related GPR X2 (MRGPRX2, EC50 = 251 nM). Also a noncompetitive nicotinic cholinergic antagonist. Inhibits nicotine-stimulated catecholamine secretion from PC12 cells in vitro, and from sympathetic nerve endings and adrena |
T79217
|
|
|
RSV
|
RSVL-protein-IN-2 (Compound A)为一种RSV聚合酶的非竞争性抑制剂,其IC50值为4.5 μM。此化合物对长RSV株表现出抗病毒活性,EC50值达1.3 μM。 |
T79220
|
|
|
RSV
|
RSVL-Protein-IN-4 (Compound C)为非竞争性RSV聚合酶抑制剂,IC50为0.88 μM。该化合物对RSV株显示出抗病毒活性,其EC50为0.25 μM。 |
T68457
|
|
|
|
GSK812397 is a potent entry inhibitor of X4-tropic strains of HIV-1, as demonstrated in multiple in vitro cellular assays. GSK812397 is a noncompetitive antagonist of the CXCR4 receptor, with GSK812397 producing a concentration-dependent decrease in both an SDF-1-mediated chemotaxis and intracellular calcium release (IC50s were 0.34+/-0.01 nM and 2.41+/-0.50 nM, respectively). GSK812397 is effective against a broad range of X4- and X4R5-utilizing clinical isolates. The potency and efficacy of GSK812397 are dependent on the individual isolate, with complete inhibition of infection observed with 24 of 30 isolates. GSK812397 does not show any detectable in vitro cytotoxicity and was highly selective for CXCR4. GSK812397 shows acceptable pharmacokinetic properties and bioavailability across species. GSK812397 has antiviral activity against a broad range of X4-utilizing strains of HIV-1 via a noncompetitive antagonism of the CXCR4 receptor. |
T69024
|
|
|
|
Homidium Chloride is the chloride salt of ethidium (a fluorochrome), Ethidium Chloride intercalates within double-stranded nucleic acids, particularly DNA. In molecular biology, the bromide salt of ethidium is used to detect and visualize DNA after electrophoresis or in cytochemical preparations. In veterinary pharmacology, it is used as a trypanosomicide. Ethidium bromide and chloride are toxic substances and potent noncompetitive antagonists of the nicotinic acetylcholine receptor. |
T82241
|
|
|
|
Halichondrin B,源自海绵 Halichondria okadai,为非竞争性Vinca-alkaloid 微管蛋白结合抑制剂,微管蛋白聚合 IC50 值为1.2-1.4 μM,表现出抗肿瘤活性。 |
T69019
|
|
|
|
Mecamylamine 是一种具有口服活性,非选择性,非竞争性的nAChR 拮抗剂。Mecamylamine 也是一种神经节阻滞剂,可穿过血脑屏障。Mecamylamine 可用于神经疾病,高血压,抗抑郁的研究。 |
T72746
|
|
|
|
'(R)-eIF4A3-IN-2'为eIF4A3-IN-2的一种活性较弱异构体。eIF4A3-IN-2是一款具高度选择性且为非竞争性的真核起始因子4A-3(eIF4A3)抑制剂,其半抑制浓度(IC50)为110 nM。 |
T69826
|
|
|
|
U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. It was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase and mammalian target of rapamycin pathways. |