ml-18

ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 [mu]M.

ML-180 (SR1848) is a potent inverse agonist of the orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) with an IC50 of 3.7 μM.

ML-184 (CID2440433) is a potent synthetic agonist of GPR55 with an EC50 of 0.26 μM.

Anti-MRSA agent 18 (E17) is an inhibitor of MRSA, exhibiting MIC values of 2 μg mL for S. aureus and 4 μg mL for MRSA. This compound accelerates bacterial death by interacting with the bacterial cell membrane constituents, phosphatidylglycerol and cardiolipin, leading to changes in membrane permeability and polarization. Additionally, it increases intracellular ROS, along with leakage of DNA and proteins.

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)

Emestrin, a mycotoxin originally isolated from *E. striata*, exhibits antimicrobial, immunomodulatory, and cytotoxic activities. It is effective against fungi *C. albicans* and *C. neoformans*, and 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). Emestrin acts as a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes). At 0.1 μg ml, it induces apoptosis in HL-60 cells and causes necrosis in heart, thymus, and liver tissues in mice at doses of 18-30 mg kg.

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)

Benastatin C is a polyketide synthase-derived benastatin found in [Streptomyces] with diverse biological activities. It inhibits glutathione S-transferase (GST; IC50 = 24 μg ml for the rat liver enzyme) and the esterase activity of isolated porcine pancreatic lipase (IC50 = 10 μg ml). Benastatin C also increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner.

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)

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)

Antitubercular agent-18 (Compound 9a) is an antitubercular agent that exhibits highly selective antimycobacterial effects, with minimum inhibitory concentration (MIC) values of 2 μg ml against M. tuberculosis H37Rv, Spec. 192, and Spec. 210, and 128 μg ml against Spec. 800, demonstrating its efficacy in inhibiting the growth of these mycobacterial strains [1].

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].

Platycodin D2 , a less hemolytic saponin, can improve specific cellular and humoral responses to hepatitis B surface antigen in mice, it could be safely used as adjuvant eliciting Th1 and Th2 immune responses. Polygalacin D2 has anti-cancer activity, it e