ml 10

ML 10 is is a [18F] positron emission tomography (PET) radiotracer that accumulates in cells presenting apoptosis-specific membrane alterations. [18F]ML-10 allows for the detection of apoptotic cells located in atherosclerotic plaques.

4-Methoxycinnamyl alcohol showed toxicity to MCF-7, HeLa and DU145 cancer cell lines with IC50 values of 14.24, 7.82 and 22.10 μg mL, respectively. 4-Methoxycinnamyl alcohol was isolated from Foeniculum vulgare. 4-Methoxycinnamyl alcohol did not show apoptotic effects but showed necrosis after 48 h in a 10 μg mL DNA fragmentation study.

ALPHA-PINENE ((-)-Alpha-Pinene) is a bicyclic monoterpene found in pine trees and other plants, including Cannabis with diverse biological activities [1]. It reduces the growth of a panel of seven Gram-positive bacteria, seven Gram-negative bacteria, and eight yeast strains with MIC values of 0.75-1.29, 1.05-1.59, and 0.7-1.17%, respectively [2]. It has insecticidal activity against C. molestus larvae with LC50 values ranging from 47 to 49 mg L.3 ALPHA-PINENE (100 μg ml) induces apoptosis, increases anion superoxide production and DNA fragmentation, and activates caspase-3 in B16 F10 melanoma cells [4]. In a B16 F10 mouse xenograft model, ALPHA-PINENE(100 ml of a 10 mg ml solution) reduces the number of metastatic lung nodules by approximately 7-fold. ALPHA-PINENE(8.6 mg L, aerosol) also increases the time spent in the open arms of the elevated plus maze by approximately 2-fold in mice, indicating anxiolytic-like activity [5].

ML-090 is NOX1-specific inhibitor(IC50 = 90 nM) which is >100 selectivity for NOX1 over NOX2, NOX3, NOX4 (all IC50s >10 μM).

ML-211 is a carbamate-based dual inhibitor of LYPLA1 (IC50 = 17 nM) and LYPLA2 (IC50 = 30 nM).

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. It inhibits DNA relaxation with an IC50 of 2 μM, compared to 120 μM for Etoposide. ARN-21934 exhibits favorable in vivo pharmacokinetic properties and shows promise in anticancer research, displaying affinity for topoIIα with an IC50 of 2 μM and for topoIIβ with an IC50 of 120 μM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 μM, G-361: 8.1 μM), breast (MCF7: 15.8 μM), endometrial (HeLa: 38.2 μM), lung (A549: 17.1 μM), and prostate (DU145: 11.5 μM) cancer cells. Following a single intraperitoneal injection of 10 mg kg, ARN-21934 achieves a peak plasma concentration of 0.68 μg mL in 15 minutes, with a half-life of 149 minutes, and remains detectable in plasma and the brain for up to 360 minutes. [1] Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.

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.

N-acetyltyramine is a metabolite of the biogenic amine tyramine . It enhances cytotoxicity of doxorubicin in resistant P388 murine leukemia cells with an IC50 value of 0.13 μg ml compared with an IC50 value of 0.48 μg ml for doxorubicin alone.

Oleic acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic acid is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma, cell membranes, and adipose tissue.1,2 It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets.1 Oleic acid inhibits collagen-stimulated platelet aggregation by approximately 90% when used at a concentration of 10 μg/ml. It also inhibits fMLF-induced neutrophil aggregation and degranulation by 55 and 68%, respectively, when used at a concentration of 5 μM, similar to arachidonic acid .3 Oleic acid (60 μM) induces release of intracellular calcium in human platelets.4

Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from patients with lung cancer). It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg/ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg/ml, reduces cough induced by citric aci......

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg/ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg/ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg/kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg/kg to 2.5 mg/kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

Urdamycin A is a bacterial metabolite originally isolated fromS. fradiaethat has antibacterial and anticancer activities.1,2It is active against a variety of Gram-positive and Gram-negative bacteria, includingB. subtilisand strains ofArthrobacterandStreptomyces, but not the fungusS. cerevisiae, in a disc assay when used at a concentration of 1 mg/ml.2Urdamycin A is cytotoxic to L1210 and HT-29, but not A549, cancer cells (IC50s = 7.5, 5, and >10 μg/ml, respectively).1

ATP Synthase Inhibitor 2 (Compound 22) TFA is a potent inhibitor of Pseudomonas aeruginosa ATP synthase with an IC50 value of 10 μg/mL. It effectively halts ATP synthesis in Pseudomonas aeruginosa at a concentration of 128 μg/mL [1].

Spirorenone is an androstadienone derivative as a highly effective aldosterone antagonist. Spirorenone is 8.6 times as potent as spironolactone, but showed a lower affinity for the mineralocorticoid receptors. In phase I clinical trials Spirorenone was absorbed with a half-life of 20-30 min, achieving maximum concentrations of about 100 ng/ml (10 mg) and 260 ng/ml (40 mg) after 1-2 h. Disposition of the parent drug was biphasic with half-lives of 50-60 min (distribution) and 5-6 h (elimination). Neither significant accumulation nor enzyme induction was observed after prolonged treatment.

Mabuterol is a selective agonist of β2 adrenoreceptor with no beta 1-stimulation. Mabuterol inhibited the positive inotropic effect of isoprenaline at 10(-7) g/ml and decreased the maximum driving frequency at 3 X 10(-6) g/ml. Mabuterol was 3 times more p

TunR2 is an antibiotic and derivative of tunicamycin .1It is active againstB. subtilis(MIC = 0.3 μg/ml) and increases the efficacy of the β-lactam antibiotics oxacillin , methicillin , and penicillin G againstB. subtiliswhen used at a concentration of 0.4 μg/ml. Unlike tunicamycin, TunR2 is non-toxic toS. cerevisiae(MIC = >10 μg/ml) and does not inhibit glycosylation in a protein N-glycosylation assay. TunR2 also has reduced antiproliferative activity against MDA-MB-231 and CHO cells compared with tunicamycin. 1.Price, N.P., Hartman, T.M., Li, J., et al.Modified tunicamycins with reduced eukaryotic toxicity that enhance the antibacterial activity of β-lactamsJ. Antibiot. (Tokyo)70(11)1070-1077(2017)

10-Norparvulenone is a fungal metabolite originally isolated fromMicrosphaeropsis.1It decreases viral sialidase activity in, and increases survival of, MDCK cells infected with the mouse-adapted influenza virus A/PR/8/34 when used at a concentration of 1 μg/ml. 1.Fukami, A., Nakamura, T., Kim, Y.P., et al.A new anti-influenza virus antibiotic, 10-norparvulenone from Microsphaeropsis sp. FO-5050J. Antibiot. (Tokyo)53(10)1215-1218(2000)

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd < 10 pM). The compound selectively binds to α4β1 (IC50 = 1.8 nM) over various other integrins and results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].

C8 Galactosylceramide is a synthetic C8 short-chain derivative of known membrane microdomain-forming sphingolipids. It increases the amount delivered and toxicity of doxorubicin in cancerous but not non-cancerous cells when incorporated into the nanoliposomal membrane of nanoliposomal-doxorubicin. C8 Galactosylceramide induces proliferation and cytokine production by splenocytes in vitro at concentrations ranging from 100-1,000 ng/ml but has no effect on natural killer T cell production in vivo. It also activates NF-κB production in C6 glioma cells when used at a concentration of 10 μM.

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, exhibits IC50 values of 20.1 μM and 34.1 μM, respectively, and demonstrates significant anti-Helicobacter pylori activity with a minimum inhibitory concentration (MIC) of 10 μg mL [1] [2] [3].

Leucomycin A13 is a macrolide antibiotic and a component of the leucomycin complex originally isolated from S. kitasatoensis. It is active against B. subtilis, S. aureus, M. luteus, and E. coli with MIC values of 0.16, 0.16, 0.08, and >10 μg ml, respectively. It binds to ribosomes with an IC50 value of 1.2 μM in a radioligand binding assay.

Forphenicine is a bacterial metabolite that has been found in S. fulvoviridis and an inhibitor of alkaline phosphatase (IC50 = 0.036 µg/ml for the chicken intestine enzyme). It inhibits the growth of HL-60 leukemia cells when used at a concentration of 10 µM. Forphenicine (50 and 500 µg/animal) increases survival in a guinea pig model of experimental autoimmune encephalomyelitis (EAE).

Papyracillic acid is a fungal metabolite and a derivative of penicillic acid originally isolated fromL. papyraceumand has antibiotic, antifungal, and phytotoxic activities.1,2It is active against the bacteriaX. campestrisandB. subtilisand the fungusC. tropicalisin a disc assay when used at a concentration of 5 μg/disc.2Papyracillic acid (1 mg/ml) induces necrotic lesion formation in a panel of 10 plants. 1.Shan, R., Anke, H., Stadler, M., et al.Papyracillic acid, a new penicillic acid analogue from the Ascomycete Lachnum papyraceumTetrahedron52(30)10249-10254(1996) 2.Evidente, A., Berestetskiy, A., Cimmino, A., et al.Papyracillic acid, a phytotoxic 1,6-dioxaspiro[4,4]nonene produced by Ascochyta agropyrina Var. nana, a potential mycoherbicide for Elytrigia repens biocontrolJ. Agric. Food Chem.57(23)11168-11173(2009)

SP-Chymostatin B is a potent inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases. It weakly inhibits human leucocyte elastase. It is effective at a final concentra

ATP Synthase Inhibitor 2, a compound targeting Pseudomonas aeruginosa (PA) ATP synthase with an IC50 of 10 μg/mL, fully inhibits the ATP synthesis activity of PA at a concentration of 128 μg/mL [1].

5β-Dihydroprogesterone (5β-DHP) is a progesterone receptor agonist and metabolite of progesterone .1,2It is formed from progesterone by 5β-reductase.25β-DHP inhibits spontaneous contractions in isolated rat uterus when used at a concentration of 10 μg/ml, an effect that can be blocked by the progesterone receptor antagonist RU486 but not the GABAAreceptor antagonist picrotoxin .1It is a negative modulator of homooligomeric Ρ1 subunit-containing GABAAreceptors, inhibiting GABA-induced currents inX. laevisoocytes expressing these receptors (IC50= 5.02 μM).3Plasma levels of 5β-DHP decrease at the onset of spontaneous human labor.4

Pyrocoll, a bacterial metabolite originally isolated from Streptomyces, inhibits the growth of A. aurescens, A. globiformis, A. oxydans, A. pascens, and R. erythropolis (MICs = 10, 1, 10, 3, and 10 μg ml, respectively), as well as HMO2, HepG2, and MCF-7 cancer cells (GI50s = 0.28, 0.42, and 2.2 μg ml, respectively) in vitro. Pyrocoll is also active against P. falciparum and T. rhodesiense (IC50s = 1.19 and 1.97 μg ml, respectively).

Evoxanthine is an alkaloid that has been found in O. renieri and has antimalarial and anticancer activities.1,2 It is active against P. falciparum with an IC50 value of 67.6 μg/ml.1 Evoxanthine decreases proliferation of nine sensitive and drug-resistant cancer cell lines (IC50s = 6.11-80.99 μM).2 |1. Khalid, S.A., Farouk, A., Geary, T.G., et al. Potential antimalarial candidates from African plants: And in vitro approach using Plasmodium falciparum. J. Ethnopharmacol. 15(2), 201-209 (1986).|2. Kuete, V., Fouotsa, H., Mbaveng, A.T., et al. Cytotoxicity of a naturally occurring furoquinoline alkaloid and four acridone alkaloids towards multi-factorial drug-resistant cancer cells. Phytomedicine 22(10), 946-951 (2015).

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 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).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 µg/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)

Herquline A is an alkaloid fungal metabolite originally isolated from P. herquei. It inhibits cell death induced by influenza A strain A/PR/8/34 in MDCK cells with an IC50 value of 10 μg/ml and inhibits viral replication in a plaque assay in a concentration-dependent manner. Herquline A also inhibits platelet aggregation induced by ADP and platelet-activating factor (PAF) in vitro (IC50s = 180 and 240 μM, respectively).

Dysolenticin J shows significant vasodilative effects on intact rat aortic rings with a diastolic degree of 87.4% at 10 ug/mL.

12-Bromododecanoic acid, a halogenated derivative of lauric acid, serves in the synthesis of clickable myristic acid derivatives and functions as a model fatty acid ligand for elucidating the X-ray crystal structure of bovine β-lactoglobulin-ligand complexes. This compound, at a concentration of 10 µg/ml, has been shown to diminish virion DNA in the culture supernatant of primary hepatocytes from a duckling model of hepatitis B virus (HBV) infection and exhibits inhibitory activity against HIV replication in CEM-SS T cells with an EC50 value of 38 µM.

Mollicellin I (compound 1), a depsidone, exhibits minimal growth inhibitory activity against human breast cancer (Bre04), human lung (Lu04), and human neuroma (N04) cell lines, with GI50 values exceeding 10 μg/mL [1].

Enrofloxacin-d5 is intended for use as an internal standard for the quantification of enrofloxacin by GC- or LC-MS. Enrofloxacin is a fluoroquinolone antibiotic. It is active against panels of Campylobacter, E. coli, and Salmonella isolates (mean MIC50s = 0.06, 0.5, and 0.03 µg/ml, respectively). It is also active against equine isolates of L. intracellularis (MICs = 0.125-0.5 µg/ml). Enrofloxacin inhibits bacterial DNA gyrase. In vivo, enrofloxacin (10 mg/kg) increases survival in a mouse model of enteropathogenic E. coli-induced sepsis. Formulations containing enrofloxacin have been used in the treatment of veterinary bacterial infections.

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg/kg) decreases serum cholesterol levels and total bod......

Peptide 5g, an antimicrobial peptide, inhibits E. coli, S. aureus, and C. albicans, exhibiting minimum inhibitory concentration (MIC) values of 30, 10, and 12.5 μg/mL, respectively [1].

Hydrochloride salt of dTAGV-1. Suitable for use in vivo. Following ip administration of 10 mg/kg in mice: T = 4.43 h; Cmax = 2123 ng mL-1; AUCinf = 18517 hr*ng mL-1 and CL = 9.05 mL min-1 kg-1 Negative control dTAGV-1-NEG also available. Important: It is recommended that DMSO stock solutions of this compound are made and used on the same day and are not subjected to freeze/thaw.

Aloenin aglycone (compound 13), an inhibitor of NF-κB, can be sourced from aloe exudate. It impedes TNFα-stimulated NF-κB transcriptional activity, showing an IC 50 of 18.7 μM. At a concentration of 10 μM, aloenin aglycone decreases both inducible nitric oxide synthase (iNOS) and intercellular adhesion molecule 1 (ICAM-1) gene expression in HepG2 cells exposed to 10 ng/mL TNFα [1].

16,16-dimethyl PGA2 is a metabolism-resistant analog of PGA2 with a prolonged in vivo half-life. It inhibits the proliferation of Sendai virus in cultured African green monkey kidney cells by >90% at a concentration of 4 μg/ml. Daily infusion of 10 μg of 16,16-dimethyl PGA2 methyl ester into mice infected with influenza A virus increased survival by 40%. Similar treatment of mice inoculated with erythroleukemia cells delayed tumor growth and increased survival time.

IT-143A is a bacterial metabolite originally isolated fromStreptomycessp. IT-143.1It is active against the bacteriumM. luteus(MIC = 6.25 μg/ml) and the fungiA. fumigatusandT. rubrumin vitro(MICs = 12.5-25 μg/ml). 1.Urakawa, A., Sasaki, T., Yoshida, K., et al.IT-143-A and B, novel piericidin-group antibiotics produced by Streptomyces SpJ. Antibiot. (Tokyo)49(10)1052-1055(1996)

Inostamycin A is a bacterial metabolite that has been found inStreptomycesand has anticancer activity.1It is an inhibitor of CDP-diacylglycerol:inositol 3-phosphatidyltransferase (IC50= 0.02 μg/ml in A431 cell membranes) and is selective for CDP-diacylglycerol:inositol 3-phosphatidyltransferase over phospholipase C (PLC) and phosphatidylinositol kinase at 10 μg/ml.2Inostamycin A decreases viability of YCU-T892, KCC-TC873, KB, HSC-4, and YCU-T891 oral squamous cell carcinoma (OSCC) cells in a concentration-dependent manner.3It induces cell cycle arrest in the G1phase in HSC-4 cells when used at a concentration of 250 ng/ml and induces apoptosis in Ms-1 small cell lung cancer cells at 300 ng/ml.3,4Inostamycin A also reduces levels of matrix metalloproteinase-2 (MMP-2) and MMP-9 and inhibits EGF-induced migration of HSC-4 cells.5 1.Imoto, M., Umezawa, K., Takahashi, Y., et al.Isolation and structure determination of inostamycin, a novel inhibitor of phosphatidylinositol turnoverJ. Nat. Prod.53(4)825-829(1990) 2.Imoto, M., Taniguchi, Y., and Umezawa, K.Inhibition of CDP-DG: inositol transferase by inostamycinJ. Biochem.112(2)299-302(1992) 3.Baba, Y., Tsukuda, M., Mochimatsu, I., et al.Cytostatic effect of inostamycin, an inhibitor of cytidine 5'-diphosphate 1,2-diacyl-sn-glycerol (CDP-DG): inositol transferase, on oral squamous cell carcinoma cell linesCell Biol. Int.25(7)613-620(2001) 4.Imoto, M., Tanabe, K., Simizu, S., et al.Inhibition of cyclin D1 expression and induction of apoptosis by inostamycin in small cell lung carcinoma cellsJpn. J. Cancer Res.89(3)315-322(1998) 5.Baba, Y., Tsukuda, M., Mochimatsu, I., et al.Inostamycin, an inhibitor of cytidine 5'-diphosphate 1,2-diacyl-sn-glycerol (CDP-DG): Inositol transferase, suppresses invasion ability by reducing productions of matrix metalloproteinase-2 and -9 and cell motility in HSC-4 tongue carcinoma cell lineClin. Exp. Metastasis18(3)273-279(2000)

Prostaglandin D1 (PGD1) is the theoretical D-series metabolite of dihomo-γ-linolenic acid (DGLA), but to date it has not been isolated as a natural product. It is an inhibitor of ADP-induced platelet aggregation in humans with an IC50 value of 320 ng/ml, about 1/10 as potent as PGD2. 13,14-dihydro-15-keto Prostaglandin D1 (13,14-dihydro-15-keto PGD1) is the theoretical metabolite of PGD1 via the 15-hydroxy PG dehydrogenase metabolic pathway. No biological studies for this compound have been reported.

Insulin-degrading enzyme (IDE) is a thiol-sensitive zinc-metallopeptidase that acts as the major insulin-degrading protease in vivo, mediating the termination of insulin signaling. [1] In addition to regulating insulin action in diabetes pathogenesis, IDE plays a role in Varicella-Zoster virus infection and degradation of amyloid-β, a peptide implicated in Alzheimer's disease. ML-345 is a small molecule inhibitor that selectively targets cysteine819 in IDE with an EC50 value of 188 nM. [2] It demonstrates 10-fold selectivity for IDE over a panel of enzymes with reactive cysteine residues.[2] Reference：[1]. Maianti, J.P., McFedries, A., Foda, Z.H., et al. Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones. Nature 511(7507), 94-98 (2014).[2]. Bannister, T.D., Wang, H., Abdul-Hay, S.O., et al. ML345, a small-molecule inhibitor of the insulin-degrading enzyme (IDE). 1 R03 DA024888-01 (MLSCN cycle 6), 1-41 (2014).

Trypacidin is a fungal metabolite originally isolated fromA. fumigatus.1It is active againstB. subtilisandM. bovis(MICs = 12.5 and 1.25 μg/ml, respectively), as well asT. cruziandT. gondii(MICs = 5-10 and 10-20 μg/ml, respectively).1,2It reduces viability and induces lysis of A549 human lung cancer cells (IC50s = 7.4 μM for both).3Trypacidin increases survival in a mouse model ofT. gondiiinfection when administered in six doses of 12.5 mg/kg each.1 1.Balan, J., Ebringer, L., Nemec, P., et al.Antiprotozoal antibiotics. II. Isolation and characterization of trypacidin, a new antibiotic, active against Trypanosoma cruzi and Toxoplasma gondiiJ. Antibiot. (Tokyo)16157-160(1963) 2.Song, Z., Liu, Y., Gao, J., et al.Antitubercular metabolites from the marine-derived fungus strain Aspergillus fumigatus MF029Nat. Prod. Res.1-8(2019) 3.Gauthier, T., Wang, X., Dos Santos, J.S., et al.Trypacidin, a spore-borne toxin from Aspergillus fumigatus, is cytotoxic to lung cellsPLoS One7(2)e29906(2012)

9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME (1 g animal) enhances the antiviral IgA and IgG antibody responses induced by a nasal influenza hemagglutinin (HA) vaccine by 5.2- and 2-fold, respectively, in mice.4 1.Hamberg, M., and Hamberg, G.Peroxygenase-catalyzed fatty acid epoxidation in cereal seeds: Sequential oxidation of linoleic acid into 9(S),12(S),13(S)-trihydroxy-10(E)-octadecenoic acidPlant Physiol.110(3)807-815(1996) 2.Hong, S.S., and Oh, J.S.Inhibitors of antigen-induced degranulation of RBL-2H3 cells isolated from wheat branJ. Korean Soc. Appl. Biol. Chem.5569-74(2012) 3.Kim, C.S., Kwon, O.W., Kim, S.Y., et al.Five new oxylipins from Chaenomeles sinensisLipids49(11)1151-1159(2014) 4.Shirahata, T., Sunazuka, T., Yoshida, K., et al.Total synthesis, elucidation of absolute stereochemistry, and adjuvant activity of trihydroxy fatty acidsTetrahedron62(40)9483-9496(2006) 5.Fuchs, D., Tang, X., Johnsson, A.-K., et al.Eosinophils synthesize trihydroxyoctadecenoic acids (TriHOMEs) via a 15-lipoxygenase dependent processBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(4)158611(2020)

Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromycin (3.4 nM) reverses bleomycin-induced cell cycle arrest at the G2 phase in Jurkat cells. It inhibits replication of the HIV-1 strains LAV-1 and RF and the HIV-2 strain LAV-2 in MT-4 cells (IC50s = 0.008, 0.11, and 0.007 μM, respectively). It also inhibits replication of a clinical isolate of HIV-1, strain KK-1, in MT-4 cells and peripheral blood mononuclear cells (PBMCs; IC50s = 0.14 and <0.1 μM, respectively).