a-395

A-395 是一种多梳抑制复合物 2 (PRC2) 蛋白质-蛋白质相互作用的拮抗剂，可有效抑制三聚体 PRC2 复合物 (EZH2-EED-SUZ12)，IC50为 18 nM。

(1S,2R)-Alicapistat ((1S,2R)-ABT-957)是一种高效的口服活性化合物，专门抑制人类calpains 1和2，对阿尔茨海默病(AD)治疗具有前景的应用[1]。该化合物有效应对与羰基还原相关的代谢负担，同时展示出对calpain 1的强效抑制作用，其IC50值为395 nM[2]。

Dimethoate (L-395) 是一种系统性和接触性杀虫剂，用于控制牛蛴螬和农场动物的某些其他害虫。

GX-395 is a novel Nav1.7 inhibitor.

VX-11e (TCS ERK 11e) 是可口服的ERK 高效选择性抑制剂，Ki 值小于 2 nM。

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)

10-Pyrene-PC is a substrate for all PLA2s with the exception of cPLA2 and PAF-AH. Upon phospholipid hydrolysis, 10-pyrenyldecanoic acid is produced from 10-pyrene-PC. The monomeric 10-pyrenyldecanoic acid exhibits fluorescence (excitation 345 nm, emission 395 nm), allowing quantitation of phospholipase activity.

N-p-Tosyl-Gly-Pro-Lys-pNA is a colorimetric substrate for plasmin.1,2,3Plasmin binds and hydrolyzes N-p-tosyl-Gly-Pro-Lys-pNA to releasep-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of plasmin activity. 1.Jespersen, J., Gram, J., and Astrup, T.The autodigestion of human plasmin follows a bimolecular mode of reaction subject to product inhibitionThromb. Res.41(3)395-404(1986) 2.Kim, S.H., and Choi, N.S.Electrophoretic analysis of protease inhibitors in fibrin zymographyAnal. Biochem.270(1)179-181(1999) 3.Chen, T., and Rael, E.D.Purification of M5, a fibrinolytic proteinase from Crotalus molossus molossus venom that attacks complementInt. J. Biochem. Cell Biol.29(5)789-799(1997)

γ-Fibrinogen377-395 TFA 是纤维蛋白原衍生抑制肽，具有纤维蛋白原表位特性。该化合物能在体外抑制小胶质细胞激活、阻断纤维蛋白与Mac-1相互作用，并在小鼠体内抑制实验性自身免疫性脑脊髓炎(EAE)。该肽适用于多发性硬化症(MS)及其他血脑屏障损伤和小胶质细胞激活相关的神经炎症疾病研究。

γ-Fibrinogen377-395是一种衍自纤维蛋白原的抑制性肽段，也被认为是纤维蛋白原的表位之一。它能在体外抑制小胶质细胞的激活并阻断纤维蛋白与Mac-1的交互作用；此外，在小鼠体内能够抑制实验性自身免疫性脑脊髓炎(EAE)的发展。因此，γ-Fibrinogen377-395对于多发性硬化症(MS)以及其他与血脑屏障损伤和小胶质细胞活化相关的神经炎症性疾病的研究具有潜在的应用价值。