ml 23

ML 23 is a melatonin analogue in the treatment and management of Parkinson's disease. ML-23 is a potential clinical candidate for the treatment of PD, and the present study has been undertaken to determine the efficacy of ML-23 in the 1-methyl-4-phenyl, 1

ML 2-23是一种有效的PROTAC BCR-ABL降解剂，可在白血病细胞中通过蛋白酶体依赖的途径选择性地降解BCR-ABL。

Mevastatin (ML236B) 是他汀类 HMG-CoA 还原酶抑制剂。它是一种降脂药，可诱导细胞凋亡，将癌细胞阻滞在 G0/G1期。它还可增加内皮型一氧化氮合酶的 mRNA 和蛋白质水平。它有抗肿瘤活性，用于心血管疾病的研究。

ML239 (CID-49843203) 是乳腺癌肿瘤干细胞的选择性抑制剂(C50:1.16 μM)。

ML230 is a selective ATP-binding cassette (ABC) transporter ABCG2 inhibitor. It 36-fold selective for ABCG2 over ABCB1 (EC50s: 0.13 μM and 4.65 μM, respectively).

ML234作为一种针对EZH2/LSD1的双重抑制剂，IC50分别达到0.09和0.12 μM。该化合物对前列腺癌细胞系LNCAP、PC3及22RV1显示出显著的抗增殖效果，并在22RV1异种移植小鼠模型中有效抑制肿瘤生长。因此，ML234具备成为前列腺癌治疗研究中的重要抗癌试剂的潜力。

novel APJ agonist

ML233 is a potent non-peptide apelin receptor agonist (EC50 = 3.7 μM) that exhibits more than 21-fold selectivity over the closely related angiotensin 1 receptor (AT1) (>79 μM) [1].

ML-236A is an inhibitor of cholesterogenesis.

ML-236C is an inhibitor of cholesterogenesis.

(E)-ML233是ML233的E型异构体，后者为一种有效的APJ激动剂。

Calcitriol (1,25-Dihydroxyvitamin D3) 是一种维他命 D 的代谢物，一种维他命 D 受体 (VDR) 的激动剂 (IC50=0.4 nM)。Calcitriol 增加肠道对钙和磷的吸收，并与甲状旁腺激素一起增加了骨吸收。

Myricetin (Cannabiscetin) 属于天然类黄酮，是一种 MEK1 抑制剂。Myricetin 具有降血糖、抗氧化、保肝护肝、抗肿瘤和抗炎活性。

Compound A33 (Antibacterial agent 246) 在治疗23种革兰氏阳性细菌方面表现出色，其最低抑菌浓度范围为0.5 ~ 4 μg/mL。此外，当与Polymyxin E联用时，Compound A33 能有效抑制多种革兰氏阴性菌的生长，表现出的部分抑菌浓度指数为0.066。

DT-23是一种有效的抗真菌药物，其MIC50为15 μg/mL。DT-23抑制重组Arg1和Kcs1，IC50值分别为0.6 μM和0.68 μM。

CYP51-IN-22 是一种强效广谱的 CYP51 抑制剂，是 CYP51-IN-23-d3 的非氘代形式，对烟曲菌的 MIC80 为 1 μg/mL。CYP51-IN-22 具有显著的杀菌作用和抗耐药性能，并对细胞展现出良好的安全性，对小鼠显示出显著的药效学活性。CYP51-IN-22 可用于侵袭性真菌感染 (IFIs) 的研究。

NDM-1-IN-10 (Compound CS-23) 是一种不可逆的共价 NDM-1 抑制剂，其 IC50 值为 36 nM。NDM-1-IN-10 与 Meropenem 对表达 NDM-1 的 E. coli 显示协同效应，对 E. coli BL21/pET15b-blaNDM-1 的 MIC 为 0.25 μg/mL。NDM-1-IN-10 可用于细菌感染的研究。

HT-2 Toxin-13C22 is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active,deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin,HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2,A549,HEp-2,Caco-2,A-204,U937,Jurkat,and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human umbilical vein endothelial cells with an IC50value of 56.4 ng/ml.1It induces oxidative stress,DNA damage,and autophagy in,as well as halts the development of,cultured mouse embryos when used at a concentration of 10 nM.3HT-2 toxin has been found in cereal grains and food products.4,5

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003). 3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4 References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003).

Galbinic acid is a depsidone lichen metabolite that has been found in U. undulata.1,2 It is active against the Gram-positive bacteria B. cereus, B. subtilis, and S. aureus, but not S. epidermidis (MICs = 62.5, 62.5, 250, and >250 μg/ml, respectively), as well as the Gram-negative bacterium E. coli, but not S. sonnei (MICs = 125 and >250 μg/ml, respectively).3 |1. Salgado, F., Albornoz, L., Cortéz, C., et al. Secondary metabolite profiling of species of the genus Usnea by UHPLC-ESI-OT-MS-MS. Molecules 23(1), E54 (2017).|2. Elix, J.A., and Engkaninan, U. The structure of galbinic acid. A depsidone from the lichen Usnea undulata. Aust. J. Chem. 28(8), 1793-1797 (1975).|3. Sultana, N., and Afolayan, A.J. A new depsidone and antibacterial activities of compounds from Usnea undulata Stirton. J. Asian Nat. Prod. Res. 13(12), 1158-1164 (2011).

Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) 属于天然产物，是一种凋亡和自噬诱导剂，通过调节GSK3β/β-catenin和p53通路，具有口服活性及抗病毒、抗肿瘤等多种药理作用。

LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) [1]. LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin[2]. LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin[1].Pharmacokinetic AnalysisLEO 39652 exhibits total clearance (rats 930, minipigs 200 and monkey 300 mL/min/kg) and ratio to total AUC (rats 4, minipigs 6 and monkey 6 %) following intravenous administration (rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg)[1]. [1]. Jens Larsen, et al. Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3 H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5- a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel Dual-Soft" PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis. J Med Chem. 2020 Dec 10;63(23):14502-14521.[2]. Stefan Eirefelt

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)

Antitubercular agent-23 是有效的抗念珠菌及抗结核剂，能够作用于 Candida albicansMTCC 3017 (MIC: 1.1 μg/ml) 和 M. tuberculosis(H37Rv) (MIC: 1 μg/ml)。