mt 2

Mt KARI-IN-2 (compound 5b) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki value of 2.02 μM. It also inhibits Mtb H37Rv with a MIC value of 0.78 μM and demonstrates low cytotoxicity, as indicated by a HEK IC50 greater than 86 μg mL [1].

2-MT 63 is a novel TIE-2 kinase inhibitor that demonstrates unique and improved kinase selectivity compared to other inhibitors known to interact with TIE-2. 2-MT 63 has a good kinase selectivity profile in enzyme assays with >30-fold selectivity (typically much greater) against the tested kinases. Importantly, the profile includes selectivity against other targets of relevance for angiogenesis (KDR, PDGFR, EPHB4).

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.

4-P-PDOT (4-phenyl-2- propionamidotetralin) is a potent, selective and affinity Melatonin receptor (MT2) antagonist.

1,2-Bis(2-iodoethoxy)ethane is a PEG-based PROTAC linker used in the synthesis of MT802 and SJF620, which are potent PROTAC BTK degraders with DC50s of 1 nM and 7.9 nM, respectively [1].

glycine (2-Aminoacetic acid) is a non-essential amino acid. It is found primarily in gelatin and silk fibroin and used therapeutically as a nutrient. It is also a fast inhibitory neurotransmitter.

TJ191 is a selective anti-cancer agent, targeting low TβRIII-expressing malignant T-cell leukemia lymphoma cells.

4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, demonstrates potent activity against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.

8-M-PDOT (AH-002) is a selective and potent melatonin MT2 receptor agonist that also inhibits MT1 receptors. 8-M-PDOT exhibits anxiolytic activity and can be used to study MT2-induced neuropathic pain.

AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC

Roluperidone (CYR-101), a novel cyclic amide derivative, exhibits high equipotent affinities for 5-HT2A and σ2 receptors with Ki values of 7.53 nM and 8.19 nM, respectively.

Loviride is a non-nucleoside reverse transcriptase inhibitor (IC50: 0.3 µM). Loviride inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells. It is used for reverse transcriptase from HIV-1.

S26131 (N-[2-[7-[3-[8-(2-acetamidoethyl)naphthalen-2-yl]oxypropoxy]naphthalen-1-yl]ethyl]acetamide) behaves as an antagonist on MT1 and MT2 receptors with Ki of 0.5 and 112 nM respectively.

UCM 765 is a partial agonist of melatonin MT(2) receptor.

3'-Deoxy-4-thiothymidine can moderately active in protecting HIV-induced cytopathogenicity of MT-2 and CEM cells.

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).

C18 D-threoCeramide (d18:1 18:0) is a synthetic ceramide and stereoisomer of C18 ceramide .1It inhibits rat brain mitochondrial ceramidase (mt-CDase) with an IC50value of 16.6 μM.2[Matreya, LLC. Catalog No. 1855] 1.Koolath, S., Murai, Y., Suga, Y., et al.Chiral combinatorial preparation and biological evaluation of unique ceramides for inhibition of sphingomyelin synthaseChirality32(3)308-313(2019) 2.Usta, J., El Bawab, S., Roddy, P., et al.Structural requirements of ceramide and sphingosine based inhibitors of mitochondrial ceramidaseBiochemistry40(32)9657-9668(2001)

Benanomicin A is a microbial metabolite found in Actinomycetes with antifungal, fungicidal, and antiviral activities. It is effective against various mammalian and plant pathogenic fungi, including C. albicans, T. mentagrophytes, C. neoformans, P. oryzae, and A. niger (MICs = 3.13-50 μg ml). Benanomicin A also inhibits HIV-1 viral infection in MT-4 cells in a concentration-dependent manner.

Benanomicin B is a microbial metabolite that has been found inActinomycetesand has antifungal, fungicidal, and antiviral activities.1,2It is active against a variety of mammalian and plant pathogenic fungi, includingC. albicans,T. mentagrophytes,C. neoformans, andP. oryzae(MICs = 1.56-50 μg/ml).1Benanomicin B inhibits HIV-1 viral infection in MT-4 cells in a concentration-dependent manner.2 1.Takeuchi, T., Hara, T., Naganawa, H., et al.New antifungal antibiotics, benanomicins A and B from an actinomyceteJ. Antibiot. (Tokyo)41(6)807-811(1987) 2.Kondo, S., Gomi, S., Ikeda, D., et al.Antifungal and antiviral activities of benanomicins and their analoguesJ. Antibiot. (Tokyo)44(11)1228-1236(1990)

1,4-Dicaffeoylquinic acid has antioxidant activity.1,4-Dicaffeoylquinic acid is a potent and highly selective class of HIV-1 integrase inhibitors, inhibitsHIV-1 replication in MT-2 cell culture at non-toxic concentrations.

MtTMPK-IN-2 (compound 15), a potent inhibitor of Mycobacterium tuberculosis thymidylate kinase (Mt TMPK), demonstrates an IC50 value of 1.1 μM. This compound effectively inhibits Mtb H37Rv with a minimum inhibitory concentration (MIC) of 12.5 μM and exhibits cytotoxicity in MRC-5 human fibroblast cells with an EC50 of 6.1 μM. MtTMPK-IN-2 is valuable for tuberculosis research [1].

HIV-1 inhibitor-24 (compound S-12a) is a potent inhibitor of HIV-1 reverse transcription (HIV-1 RT) with an IC50 of 9.5 nM. It exhibits a high antiviral effect on wild-type HIV-1, showing an EC50 value of 1.6 nM and low cytotoxicity (CC50 on MT-4 cells). HIV-1 inhibitor-24 was well tolerated in mice at a dose of 2 g kg and demonstrated a significant cardiovascular safety profile.

Dp2mT is an iron chelator which inhibits HIV-1 transcription.