ml 18

ML-18是一种非肽铃蟾肽受体亚型-3 拮抗剂，能够抑制肺癌生长。

VU0400195 is a oral effective, positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)).

ML188 enantiomer 是一种针对 HKU4-CoV 3CLpro 的抑制剂，展现出良好的酶抑制及抗病毒效果。

ML-184 (CID2440433) 是一种选择性的GPR55激动剂(EC50: 250 nM)，对 GPR55 的选择性比 GPR35、CB1 和 CB2 的高100 倍以上。它可以激活 GPR55 ，诱导 ERK1 2 磷酸化并促使PKCβII 向质膜移位。它能在体外诱导神经干细胞增殖，并加速进神经元分化。

16-(S)-ML188 是一种有用的有机化合物，可用于生命科学领域的相关研究，其产品编号为 T64738。

ML188是一种选择性非共价 SARS-CoV3CLpro 抑制剂，具有抗病毒活性，IC50为 1.5 μM。

ML-180 (SR1848) 是孤儿核受体肝受体同源物 1 (LRH-1;NR5A2) 的反向激动剂(IC50:3.7 µM)。它不抑制类固醇生成因子 1 (SF-1;NR5A1; IC50>10 µM)。 它具有潜在的抗依赖 LRH-1 癌症作用。

6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg ml).2 |1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity of 6-substituted indoles. J. Antibiot. (Tokyo) 55(11), 1009-1012 (2002).|2. Nkunya, M.H., Makangara, J.J., and Jonker, S.A. Prenylindoles from Tanzanian Monodora and Isolona species. Nat. Prod. Res. 18(3), 253-258 (2004).

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 &#181g ml) and Gram-negative bacteria (MICs = 136-200 &#181g ml), as well as yeasts (MICs = 10-20 &#181g ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 &#181M), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 &#181M).2It reduces tumor growth in a B16 BL6 mouse model of melanoma when administered at a dose of 25 mg kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 &#181g ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg kg.3Ajoene (25 mg kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16 BL6 melanoma cells in C57BL 6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

Anti-MRSA agent 18 (E17)，MRSA和S. aureus的MIC值分别是4 μg mL与2 μg mL，它抑制MRSA的机制主要是与细菌细胞膜中的磷脂酰甘油和心磷脂发生相互作用。这种作用引起细胞膜的通透性及极化状态发生改变，导致细胞内的ROS水平升高，以及DNA与蛋白质的渗漏，从而促进细菌的快速死亡。

Erythromycin 2'-propionate is a macrolide antibiotic and an esterified form of erythromycin .1It is active againstS. aureuswhen used at a concentration of 1 μg/ml. Erythromycin 2'-propionate (1 mM) inhibits protein synthesis in a cell-free assay. 1.Tardrew, P.L., Mao, J.C.H., and Kenney, D.Antibacterial activity of 2'-esters of erythromycinAppl. Microbiol.18(2)159-165(1969)

Flumequine-13C3is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae(MICs = 1-100 μg ml). Flumequine is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3In vivo, flumequine (50 mg kg) increases survival in rat models ofP. vulgaris-induced urinary tract infection andP. mirabilis-induced prostatitis.1Formulations containing flumequine have been used in the treatment of urinary tract infections in veterinary medicine. 1.Rohlfing, S.R., Gerster, J.R., and Kvam, D.C.Bioevaluation of the antibacterial flumequine for urinary tract useAntimicrob. Agents Chemother.10(1)20-24(1976) 2.Aller-Morán, L.M., Martínez-Lobo, F.J., Rubio, P., et al.Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriaeRes. Vet. Sci.10351-53(2015) 3.Smith, J.T.The mode of action of 4-quinolones and possible mechanisms of resistanceJ. Antimicrob. Chemother.18 (Suppl. D)21-29(1986)

Benastatin A is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2,3It inhibits glutathione S-transferase (GST; Ki= 5 μM for the rat liver enzyme).2Benastatin A is active against several bacteria, including methicillin-resistantS. aureus(MRSA; MIC = 3.12 μg ml). It induces apoptosis and cell cycle arrest at the G1 G0phase in Colon 26 mouse colon cancer cells when used at concentrations of 20 and 16 μM, respectively.3 1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyagi, T., Aoyama, T., Kojima, F., et al.Benastatins A and B, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)45(9)1385-1390(1992) 3.Kakizaki, I., Ookawa, K., Ishikawa, T., et al.Induction of apoptosis and cell cycle arrest in mouse colon 26 cells by benastatin AJpn. J. Cancer Res.91(11)1161-1168(2000)

Antitubercular agent-18 (Compound 9a) 为抗结核剂，对M. tuberculosisH37Rv、Spec. 192、Spec 210 及 Spec. 800 的最小抑制浓度(MIC)值依次为2、2、2 及128 μg ml，展现出对分支杆菌的高选择性抗菌活性。

Platycodin D2 是分离自桔梗的皂苷类物质，显示除抗癌活性。

Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities.1,2,3,4,5 It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg ml, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestrin (0.1 μg ml) induces apoptosis in HL-60 cells.4 It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg kg.5 |1. Seya, H., Nakajima, S., Kawai, K.-i., et al. Structure and absolute configuration of emestrin, a new macrocyclic epidithiodioxopiperazine from Emericella striata. J. Chem. Soc. Chem. Commun. 10, 657-658 (1985).|2. Herath, H.M.T.B., Jacob, M., Wilson, A.D., et al. New secondary metabolites from bioactive extracts of the fungus Armillaria tabescens. Nat. Prod. Res. 27(17), 1562-1568 (2013).|3. Herath, K.B., Jayasuriya, H., Ondeyka, J.G., et al. Isolation and structures of novel fungal metabolites as chemokine receptor (CCR2) antagonists. J. Antibiot. (Tokyo) 58(11), 686-694 (2005).|4. Ueno, Y., Umemori, K., Niimi, E.-c., et al. Induction of apoptosis by T-2 toxin and other natural toxins in HL-60 human promyelotic leukemia cells. Nat. Toxins 3(3), 129-137 (1995).|5. Terao, K., Ito, E., Kawai, K.-i., et al. Experimental acute poisoning in mice induced by emestrin, a new mycotoxin isolated from Emericella species. Mycopathologia 112(2), 71-79 (1990).

Benastatin C is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2It inhibits glutathione S-transferase (GST; IC50= 24 μg ml for the rat liver enzyme).2Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50= 10 μg ml). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner. 1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyama, T., Kojima, F., Yamazaki, T., et al.Benastatins C and D, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. Production, isolation, structure determination and biological activitiesJ. Antibiot. (Tokyo)46(5)712-718(1993)

Anticancer agent 37 (compound 18) is a sulfonylurea derivative known for its potent anticancer activity. It efficiently inhibits the growth of HePG2 cells, displaying an IC 50 value of 17.2 μg mL [1].