mt-2

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).

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].

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].

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

AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.

RS-127445 hydrochloride (MT 500) is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist(pKi : 9.5).

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.

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. It effectively induces apoptosis in MYD88 MT DLBCL and has demonstrated efficacy in inducing in vivo tumor regressions in a lymphoma model [1] [2] [3].

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)

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

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

HIV-1 Integrase Inhibitor 10, an orally active allosteric integrase inhibitor (ALLINI), effectively inhibits the NLRepRluc virus's viral outgrowth in MT-2 cells, exhibiting EC50 values of 3-5 nM. This compound is utilized in the research of Human Immunodeficiency Virus-1 (HIV-1).

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).

F9170, an antiviral peptide derived from the HIV-1 envelope glycoprotein (amino acids 789-803), targets the LLP1 domain in the virus's envelope protein cytoplasmic tail. This interaction inhibits HIV-1 IIIB infection in MT-2 cells, evidenced by an EC50 value of 0.19 µM. Additionally, at a dosage of 3 mg/kg, F9170 significantly lowers plasma viral load in rhesus macaques infected with simian HIV (SHIV).

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.

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

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].

Quinine hemisulfate hydrate, an alkaloid extracted from the cinchona tree bark, serves as an anti-malarial agent and potassium channel inhibitor. It specifically targets and inhibits WT mouse Slo3 (K Ca 5.1) channel currents induced by voltage pulses to +100 mV, having an IC 50 value of 169 μM [1] [2].

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)

3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50 = 13.4 µM). It is also active against L. donovani amastigotes when used at a concentration of 50 µM.

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.

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.

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

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.