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Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacteriumtuberculosis and Mycobacterium lepraeInhA. Prothionamide can effectively inhibit the growth of Mycobacteriumtuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
MycobacteriumTuberculosis-IN-2 (Compound 29) is a bacterial inhibitor that effectively inhibits MycobacteriumTuberculosis. MycobacteriumTuberculosis-IN-2 can be used in tuberculosis research (MIC = 0.07-0.16 μM) .
MycobacteriumTuberculosis-IN-5 (Compound 11) is the HCl salt form of 5-Fluoroindole (HY-40156). MycobacteriumTuberculosis-IN-5 is an antibacterial agent, that inhibits Mycobacteriumtuberculosis with a MIC of 29.1 μM. MycobacteriumTuberculosis-IN-5 exhibits metabolic stability in rat liver microsomes. MycobacteriumTuberculosis-IN-5 exhibits anti-tuberculosis efficacy in mice .
MycobacteriumTuberculosis-IN-7 (Compound 4c) inhibits M. tuberculosis H37Ra with MIC of 5.34 μg/mL. MycobacteriumTuberculosis-IN-7 exhibits slight cytotoxicity in cancer cell Vero, A549, and HepG2 (IC50s >50 μM) .
MycobacteriumTuberculosis-IN-6 (compound b1) is an inhibitor of Mycobacteriumtuberculosis enoyl reductase InhA, with IC50 of 7.74 μM. MycobacteriumTuberculosis-IN-6 can be used for antibacterial research .
MycobacteriumTuberculosis-IN-8 (Compound 6g) is a selective inhibitor of Mycobacteriumtuberculosis (MTB) with an MIC value of 6.25 µg/mL against MTB H37Rv. MycobacteriumTuberculosis-IN-8 shows potent antitubercular activities, inhibiting mycolic acid biosynthesis critical for bacterial cell wall integrity. MycobacteriumTuberculosis-IN-8 is promising for research of antitubercular agents .
Mycobacterium bovis bacterial protein is a member of the Mycobacteriumtuberculosis complex. Mycobacterium bovis bacterial protein causes tuberculosis in bovines .
Mtb-cyt-bd oxidase-IN-3 (compound 1u) is a Mycobacteriumtuberculosis cytochrome bd oxidase (Mtb cyt-bd oxidase) inhibitor with an IC50 value of 0.36 μM. Mtb-cyt-bd oxidase-IN-3 inhibits the growth of Mycobacteriumtuberculosis (MIC=32 μM). Mtb-cyt-bd oxidase-IN-3 can be used in tuberculosis research .
TBAJ-876 is the inhibitor of mycobacteriumtuberculosis. TBAJ-876 is the analogue of the anti-tuberculosis agent Bedaquiline. TBAJ-876 has the potential for the research of tuberculosis .
(Rac)-TBAJ-876 is a racemate of TBAJ-876. TBAJ-876 is the inhibitor of mycobacteriumtuberculosis. TBAJ-876 is the analogue of the anti-tuberculosis agent Bedaquiline (HY-14881). TBAJ-876 has the potential for the research of tuberculosis .
Mtb-cyt-bd oxidase-IN-1 (compound 1x) is a Mycobacteriumtuberculosis cytochrome bd oxidase (Mtb cyt-bd oxidase) inhibitor with an IC50 value of 0.13 μM. Mtb-cyt-bd oxidase-IN-1 can be used in tuberculosis research .
JSF-4898 is an orally active inhibitor of the MenG enzyme in Mycobacteriumtuberculosis. JSF-4898 has MIC of 0.78 μM against MycobacteriumtuberculosisH37Rv. JSF-4898 can enhance the efficacy of Rifampicin (HY-B0272) in a subacute model of Mycobacteriumtuberculosis infection in mice .
KSK-104 has potent antibacterial activity against Mycobacteriumtuberculosis (MIC=0.78 μM). The role of KSK-104 is mainly involved in the synthesis and recovery pathways of pyridoxal 5'-phosphate (PLP), PLP-dependent enzymes and oxidative stress networks. KSK-104, as a candidate molecule for novel anti-tuberculosis drugs, can be used to develop research against drug-resistant mycobacteriumtuberculosis .
Tuberculosis inhibitor 6 (compound 2c) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacteriumtuberculosis (MIC90 of ≤1.66 μM) and Mycobacterium marinum (MIC90 of 2.65 μM) .
Tuberculosis inhibitor 7 (compound 2d) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacteriumtuberculosis (MIC90 of 0.63 μM) and Mycobacterium marinum (MIC90 of 0.63 μM) .
Tuberculosis inhibitor 9 (compound 3d) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacteriumtuberculosis (MIC90 of 0.64 μM) and Mycobacterium marinum (MIC90 of 0.64 μM) .
Tuberculosis inhibitor 8 (compound 3b) is a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative that shows highly active against Mycobacteriumtuberculosis (MIC90 of 0.69 μM) and Mycobacterium marinum (MIC90 of 0.69 μM) .
JNJ-6640 is an inhibitor targeting mycobacterial PurF (the first enzyme in the de novo purine biosynthesis pathway) with potent anti-tuberculosis activity. JNJ-6640 exhibits bactericidal activity against Mycobacteriumtuberculosis in vitro, with an MIC90 of 8.6 nM. JNJ-6640 disrupts de novo purine biosynthesis, inhibits M. tuberculosis DNA replication in vivo. JNJ-6640 exhibits anti-tuberculosis efficacy in acutely infected mice. JNJ-6640 can be used for the study of tuberculosis .
Mtb-cyt-bd oxidase-IN-4 (compound 1g) is a Mycobacteriumtuberculosis cytochrome bd oxidase (Mtb cyt-bd oxidase) inhibitor with an IC50 value of 0.25 μM. Mtb-cyt-bd oxidase-IN-4 inhibits the growth of Mycobacteriumtuberculosis (MIC=8 μM). Mtb-cyt-bd oxidase-IN-4 can be used in tuberculosis research .
Zamanic acid is a potent inhibitor of glutathione reductase. Zamanic acid inhibits the growth of Mycobacteriumtuberculosis in culture and has also been shown to have anti-inflammatory activity .
DNA Gyrase-IN-1 (compound 42) is a potent and selective DNA gyrase inhibitor with an IC50 value of 2.6 µM. DNA Gyrase-IN-1 has high inhibitory activity against Mycobacteriumtuberculosis (Mtb) with MIC of 0.49 µM. DNA Gyrase-IN-1 can be used for researching tuberculosis .
InhA-IN-7 (Compound 11) is a Triclocan (HY-B1119) derivative with inhibitory activity towards enoyl-acyl carrier protein reductase (InhA) with an IC50 of 96 nM. InhA-IN-7 inhibits proliferations of Mycobacteriumtuberculosis wildtype and mutant strains with MICs ranging from 19 to 75 μM .
GSK2556286 (GSK286) is an orally active and cholesterol-dependent Mycobacteriumtuberculosis inhibitor. GSK2556286 inhibits Mycobacteriumtuberculosis inside infected macrophages (IC50 = 0.07 μM in THP-1 cells), in the presence of cholesterol. GSK2556286 acts via Rv1625c, a membrane-bound adenylyl cyclase in Mycobacteriumtuberculosis. GSK2556286 is an Rv1625 agonist leading to increased cAMP and reduced cholesterol metabolism. GSK2556286 can be studied in research for antitubercular purposes .
MenA IN-1 is an effective inhibitor of 1,4-dihydroxy-2-naphthoate isoprenyltransferase (MenA) from Mycobacteriumtuberculosis (MTB) with an IC50 value of 13 µM and an GIC50 value of 8 µM. MenA IN-1 can be used to curb the continuous spread of tuberculosis .
(2E)-Eicosenoic acid is an inhibitor of Mycobacteriumtuberculosisprotein tyrosine phosphatase A (PtpA). (2E)-Eicosenoic acid exhibits strong inhibitory activity against PtpA with an IC50 value in the low micromolar range. (2E)-Eicosenoic acid can be used for research on Mycobacteriumtuberculosis infection .
Mtb-cyt-bd oxidase-IN-2 is an inhibitor of Mycobacteriumtuberculosis cytochrome bd oxidase (Mtb cyt-bd oxidase) with an IC50 value of 0.67 μM. Mtb-cyt-bd oxidase-IN-2 inhibits the growth of Mycobacteriumtuberculosis with a MIC value of 256 μM. Mtb-cyt-bd oxidase-IN-2 can be used for the research of infection .
Mtb-IN-11 (Compound 1e) is an inhibitor of Mycobacteriumtuberculosis salicylate synthase (MbtI), with an IC50 of 11.2 μM. Mtb-IN-11 exhibits good in vitro anti-tuberculosis activity, with a MIC99 of 32 μM against M. bovis BCG. Mtb-IN-11 can be used for the research of tuberculosis .
Mtb-cyt-bd oxidase-IN-6 is a potent Mycobacteriumtuberculosis (Mtb) cytochrome bd (cyt-bd) oxidase (MtbCyt-bd Oxidase) inhibitor with an IC50 value of 0.35 μM. Mtb-cyt-bd oxidase-IN-6 can effectively inhibit the growth of Mtb (MIC= 4 μM). Mtb-cyt-bd oxidase-IN-6 can be used in the study of tuberculosis .
MenA-IN-2 (Compound 11) is an inhibitor of 1,4-dihydroxy-2-naphthoate prenyltransferase (MenA). MenA-IN-2 inhibits MenA with an IC50 value of 22 µM and inhibits Mycobacteriumtuberculosis (Mtb) with an GIC50 value of 10 µM. MenA-IN-2 can curb the continuous transmission of Mtb .
MSU-43085 is an orally active MmpL3 inhibitor of Mycobacteriumtuberculosis (Mtb). MSU-43085 effectively inhibits Mtb in an acute murine tuberculosis infection model. MSU-43085 can be used in tuberculosis research .
Amycolatopsin C is a glycosylated macrolactone with antibacterial activity. Amycolatopsin C selectively inhibits the growth of Mycobacterium bovis (BCG) and Mycobacteriumtuberculosis (H37Rv) compared to other Gram-positive and Gram-negative bacteria. Amycolatopsin C demonstrates low levels of cytotoxicity toward mammalian cells and can be utilized in antibacterial research .
HadAB-IN-1 is a potent HadAB inhibitor. HadAB-IN-1 inhibits HadAB enzyme complexes activity with an IC50 value of 0.03 μM. HadAB-IN-1 also affects mycolic acid biosynthesis in Mycobacteriumtuberculosis (Mtb). HadAB-IN-1 can be used for the research of tuberculosis (TB) .
TCA1 is a small molecule with activity against agent-susceptible and -resistant Mycobacteriumtuberculosis (Mtb). TCA1 inhibits enzymes involved in cell wall and molybdenum cofactor biosynthesis, such as DprE1 and MoeW .
TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacteriumtuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacteriumtuberculosis .
Tetrahydroxysqualene is a triterpene, possessing antimycobacterial activity against Mycobacteriumtuberculosis with an MIC of 10.0 μg/mL. Tetrahydroxysqualene can be isolated from the methanolic extracts of Rhus taitensis Guill .
UH-NIP-16 exhibits antimicrobial activity against Mycobacteriumtuberculosis, with MIC50 of 1.86 and 3.05 μM, for pathogenic mycobacterial strains H37Rv and CDC1551. UH-NIP-16 synergizes with Streptomycin (HY-B1906), Isoniazid (HY-B0329), Ethambutol (HY-B0535) and Bedaquiline (HY-14881), potentiates their anti-tuberculosis activities .
Bio-AMS is a potent bacterial biotin protein ligase inhibitor. Bio-AMS possesses selective activity against Mycobacteriumtuberculosis (Mtb) and arrests fatty acid and lipid biosynthesis .
Tuberculosis inhibitor 4 (compound 16), a mandelic acid-based spirothiazolidinone, has potent antimycobacterial activity against Mycobacteriumtuberculosis strain H37Rv with the high inhibition value 98% at lower than 6.25 µg/mL concentration .
Bio-AMS (TFA) is a potent bacterial biotin protein ligase inhibitor. Bio-AMS (TFA) possesses selective activity against Mycobacteriumtuberculosis (Mtb) and arrests fatty acid and lipid biosynthesis .
VEGFR-2/InhA-IN-1 is a pyrazole-based dual inhibitor of InhA-VEGFR with anti-tuberculosis and anti-angiogenic activities. VEGFR-2/InhA-IN-1 has good antibacterial activity against Mycobacteriumtuberculosis H37Rv strain (MIC=6.25 μg/mL) and significantly inhibits VEGFR-2 (IC50=15.27 nM) .
MptpB-IN-1 (Compound 13) is a potent and orally active inhibitor of MptpB. Mycobacteriumtuberculosis protein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. MptpB-IN-1 reduces multidrug-resistant mycobacteriumtuberculosis survival and infection burden .
DQn-1 is a potent antifolate with activity against Mycobacteriumtuberculosis (Mtb) (MIC90=0.03 µM). DQn-1 directly inhibits DHFR enzyme activity, with IC50s of 8.7 and 7.6 nM for Mtb and human DHFR enzyme, respectively .
PptT-IN-1 (compound 5j) is a potent inhibitor of with phosphopantetheinyl phosphoryl transferase (PptT) an IC50 of 2.8 μM. Phosphopantetheinyl transferase, an essential enzyme that plays a critical role in the biosynthesis of cellular lipids and virulence factors in Mycobacteriumtuberculosis. PptT-IN-1 has the potential for the research of tuberculosis .
PptT-IN-2 (compound 5k) is a potent inhibitor of with phosphopantetheinyl phosphoryl transferase (PptT) an IC50 of 2.5 μM. Phosphopantetheinyl transferase, an essential enzyme that plays a critical role in the biosynthesis of cellular lipids and virulence factors in Mycobacteriumtuberculosis. PptT-IN-2 has the potential for the research of tuberculosis .
PptT-IN-3 (compound 5p) is a potent inhibitor of with phosphopantetheinyl phosphoryl transferase (PptT) an IC50 of 3.5 μM. Phosphopantetheinyl transferase, an essential enzyme that plays a critical role in the biosynthesis of cellular lipids and virulence factors in Mycobacteriumtuberculosis. PptT-IN-3 has the potential for the research of tuberculosis .
Mtb-IN-12 (Compound 5m) is a dual-target inhibitor that can target the CYP125 (KD: 40 nM; KI: 0.1 μM) and CYP142 (KD: 160 nM; KI: 0.05 μM) enzymes of Mycobacteriumtuberculosis. Mtb-IN-12 exhibits good inhibitory activity against both drug-sensitive strains and multidrug-resistant tuberculosis strains, with low toxicity to macrophages. Mtb-IN-12 can be used in the research of anti-tuberculosis drugs .
MtInhA-IN-1 is a selective and orally active Mycobacteriumtuberculosis NADH-dependent enoyl-acyl carrier protein reductase (MtInhA) inhibitor with an IC50 of 0.23 μM. MtInhA-IN-1 potently against M. tuberculosis H37Rv strain with a MIC value of 0.4 μM .
LK-60 is a potent DprE1 inhibitor. LK-60 effectively inhibits the proliferation of Mycobacteriumtuberculosis. LK-60 has good safety profiles to gut microbiota and human cells .
Pks13-IN-1 (Compound 44) is an orally active inhibitor for MycobacteriumtuberculosisPolyketide synthase 13 (Pks13). Pks13-IN-1 inhibits M. tuberculosis strain H37Rv with a MIC of 0.07 μM. Pks13-IN-1 exhibits antibacterial efficacy in mouse model .
BRD-4592 is an allosteric inhibitor targeting Mycobacteriumtuberculosistryptophan synthase (TrpAB). BRD-4592 binds at the α-β-subunit interface of TrpAB, with an IC50 of 70.9 nM for the α-subunit and 22.6 nM for the β-subunit .
BioA-IN-1 (Compound 15) is an inhibitor of BioA, a key enzyme in the biotin synthesis pathway of Mycobacteriumtuberculosis, with an IC50 value of 0.195 μM. BioA-IN-1 exhibits antibacterial activity but has no cytotoxicity .
Antibacterial agent 228 (Compound 8) inhibits the mycobacterial ribosome (IC50 for Mycobacterium smegmatis is 2.31 μM) and exhibits antibacterial activity against M. tuberculosis H37Rv (MIC=2 and 0.25 μg/mL for wildtype and Δ1258c mutant), M. abscessus ATCC 19977 (MIC=8 and 8 μg/mL for wildtype and Δ2780c mutant) and M. smegmatis (MIC=8 μg/mL) .
PPM1A-IN-1 (Compound IV-4) is an inhibitor for PP2C Ser/Thr phosphatase protein phosphatase Mg2+/Mn2+-dependent 1A. PPM1A-IN-1 exhibits antibacterial activity against Mycobacteriumtuberculosis .
Antimycobacterial agent-8 (Compound 49) is an inhibitor for DNA gyrase. Antimycobacterial agent-8 exhibits antibacterial activity against Mycobacteriumtuberculosis and M. abscessus with MIC90 of 2.5 μM and 0.63 μM. Antimycobacterial agent-8 exhibits good plasma protein binding ability in mice .
CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacteriumtuberculosis (H37Rv MIC90∼6.25 μM, ∼2.2 μg/mL). CYP121A1-IN-1 can markedly reduce the production of mycocyclosin via inhibiting the CYP121A1 mediated turnover of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin .
TBI-223 is an orally active oxazolidinone antibiotic and an antimicrobial. TBI-223 shows activity against Mycobacteriumtuberculosis (Mtb). TBI-223 exhibits an IC50 of 68 μg/mL for inhibiting mitochondrial protein synthesis (MPS) in HepG2 cells. TBI-223 is effective in three mouse models (bloodstream infection, skin infection, and bone infection) of methicillin-resistant staphylococcus aureus infection. TBI-223 can be used for the study of tuberculosis .
(24S)-Cycloartane-3β,24,25-triol, a cycloartane, has antitubercular activity against Mycobacteriumtuberculosis H37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium .
AU1235, an adamantyl urea, is a potent MmpL3 inhibitor. The Mycobacteriumtuberculosis protein MmpL3 performs an essential role in cell wall synthesis, since it effects the transport of trehalose monomycolates across the inner membrane .
SMIP-031 is a potent and orally active PPM1A inhibitor with an IC50 value of 180 nM. SMIP-031 induces autophagy. SMIP-031 inhibits Mycobacteriumtuberculosis infect in mice .
Calpinactam (FKI-4905), a fungal metabolite, is a new anti-mycobacterial agent.Calpinactam is active only against Mycobacteria among various microorganisms, including Gram-positive and Gram-negative bacteria, fungi and yeasts. Calpinactam inhibits the growth of Mycobacterium smegmatis and Mycobacteriumtuberculosis with MIC values of 0.78 and 12.5 μg/ml, respectively .
MTC420 (compound 42a) is a heterocyclic quinolone compound that targets the respiratory chain of Mycobacteriumtuberculosis and exhibits antituberculosis activity (Rep Mtb: IC50=525 nM, Wayne Mtb: IC50=76 nM, MDR Mtb: IC50=140 nM) .
RVG TFA is a peptide derived from Rabies Virus Glycoprotein that binds to the α-7 subunit of nicotinic acetylcholine receptors (AchR) of neuronal cells. RVG enhances delivery of Mycobacteriumtuberculosis antigens to antigen-presenting cells .
RVG (RVG29) is a peptide derived from Rabies Virus Glycoprotein that binds to the α-7 subunit of nicotinic acetylcholine receptors (AchR) of neuronal cells. RVG enhances delivery of Mycobacteriumtuberculosis antigens to antigen-presenting cells .
MtTMPK-IN-4 (compound 2), a para-piperidine, is a potent mycobacteriumtuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 of 6.1 μM. MtTMPK-IN-4 is a potent tyrosinase inhibitor. MtTMPK-IN-4 is a potent antibacterial agent .
Mtb ATP synthase-IN-1 (compound 6ab) is a potent Mycobacteriumtuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb. Mtb ATP synthase-IN-1 has good metabolic stability, low cytotoxicity (Vero IC50 > 64 μg/mL), and acceptable oral bioavailability. Mtb ATP synthase-IN-1 can be used for researching anti-mycobacterium .
4-Hydroxyoxyphenbutazone kills both replicating and nonreplicating (NR) Mycobacteriumtuberculosis (Mtb), including Mtb resistant to standard agents. 4-Hydroxyoxyphenbutazone is a potent inhibitor of cytokine production. 4-Hydroxyoxyphenbutazone is an immunosuppressive agent and has the potential for rheumatoid arthritis research .
ESAT6 Epitope is a known CD4+ T cell epitope in early secretory antigen target gene 6 (ESAT6) that binds to major histocompatibility complex MHC class I with nanometer affinity (IC50=180 nM). ESAT6 Epitope can be used to enhance BCG-induced anti-Mycobacteriumtuberculosis cellular immunity .
5-Fluoroindole is an orally active fluorinated indole derivative and antibacterial agent. 5-Fluoroindole induces ROS accumulation and triggers Apoptosis. 5-Fluoroindole inhibits the growth of pan-susceptible Mycobacteriumtuberculosis (Mtb) H37Rv strains. 5-Fluoroindole has significant bactericidal activity against Pseudomonas syringae pv. actinidiae (Psa) with an EC50 of 15.34 μg/mL. 5-Fluoroindole introduces fluorine labeling for protein research. 5-Fluoroindole can be used in the study of tuberculosis and kiwifruit bacterial canker .
Selenosemicarbazide (Hydrazinecarboselenoamide) exhibits antimicrobial activity, that inhibits B. subtilis, S. aureus, Klebsiella pneumoniae, Sarcina lutea and Mycobacteriumtuberculosis. Selenosemicarbazide forms complex with metal ions, and exhibits antitumor efficacy against cancer cells
Mt KARI-IN-2 (compound 5b) is a potent Mycobacteriumtuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 2.02 μM. Mt KARI-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 86 μg/mL) .
Mt KARI-IN-4 (compound 5c) is a potent Mycobacteriumtuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 5.48 μM. Mt KARI-IN-4 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 72 μg/mL) .
Mt KARI-IN-5 (compound 6c) is a potent Mycobacteriumtuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a Ki value of 4.72 μM. Mt KARI-IN-5 has inhibitory activity against Mtb H37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)
Antitubercular agent-29 (compound 6xa) is a potent agent resistant (DR) Mycobacteriumtuberculosis (Mtb) inhibitor with MIC of 0.03 μg/mL against agent-susceptible (DS)-Mtb strains, MIC of 0.03-0.06 μg/mL against DR-Mtb strains, and favourable selectivity (SI>40) against Vero cells .
Carbazomycin D exhibits antituberculosis and antimalarial activities, that inhibits Plasmodium falciparum with an IC50 > 10 μg/mL, inhibits Mycobacteriumtuberculosis with MIC of 25 μg/mL. Carbazomycin D exhibits cytotoxicity in cell MCF-7, KB, NCI-H187 and Vero, with IC50s of 21.3, 33.2, 12.9, and 34.3 μg/mL, respectively .
L-Cycloserine ((S)-4-Amino-3-isoxazolidone) is an oral inhibitor of the enzyme gamma-aminobutyric acid (GABA) transaminase (GABA-t) and branched-chain transaminases in Mycobacteriumtuberculosis. L-Cycloserine has anticonvulsant properties and inhibits the synthesis of neurotensin in mouse brains .
Antitubercular agent-27 (compound 1) is a potent antitubercular agent with an IC50 value of 3.2 µM, an MIC value of 7.8 µM, an IC90 value of 7.0 µM. Antitubercular agent-27 shows antimycobacterial activity for resistant isolates of Mycobacteriumtuberculosis H37Rv. Antitubercular agent-27 shows effective intracellular antimycobacterial activity and low cytotoxicity .
Antitubercular agent-28 (compound 2) is a potent antitubercular agent with an IC50 value of 1.5 µM, an MIC value of 4.5 µM, an IC90 value of 2.5 µM. Antitubercular agent-28 shows antimycobacterial activity for resistant isolates of Mycobacteriumtuberculosis H37Rv. Antitubercular agent-28 shows effective intracellular antimycobacterial activity and low cytotoxicity .
PXYC1 is a ribosomal protein S1 (RpsA) antagonist with Kds of 0.81 and 0.31 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of MycobacteriumTuberculosis (Mtb) .
PXYC12 is a ribosomal protein S1 (RpsA) antagonist with Kds of 2.67 and 4.67 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of MycobacteriumTuberculosis (Mtb) .
PXYC2 is a ribosomal protein S1 (RpsA) antagonist with Kds of 6.35 and 5.11 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of MycobacteriumTuberculosis (Mtb) .
PXYC13 is a ribosomal protein S1 (RpsA) antagonist with Kds of 7.61 and 8.50 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of MycobacteriumTuberculosis (Mtb) .
PXYD4 is a ribosomal protein S1 (RpsA) antagonist with Kds of 3.24 and 1.64 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of MycobacteriumTuberculosis (Mtb) .
Antimycobacterial agent-2 (compound 58) is a potent antimycobacterial agent. Antimycobacterial agent-2 shows anti-mycobacterial activities with an MIC99 of 0.8 µM for Mycobacteriumtuberculosis (M.tb) H37Rv. Antimycobacterial agent-2 shows cytotoxic activities with an IC50 of48.1 µM for CHO cells .
MptpB-IN-2 (compound 20) is a selective mycobacteriumtuberculosis protein tyrosine phosphatase B (MptpB) inhibitor with IC50s of 0.64 μM, 4.06 μM and 4.14 μM for MptpB, MptpA and PTP1B, respectively. MptpB-IN-2 shows weak antituberculosis activity with a MIC of 64.9 μM for Mtb H37Rv .
L-Cycloserine (Standard) is the analytical standard of L-Cycloserine. This product is intended for research and analytical applications. L-Cycloserine ((S)-4-Amino-3-isoxazolidone) is an oral inhibitor of the enzyme gamma-aminobutyric acid (GABA) transaminase (GABA-t) and branched-chain transaminases in Mycobacteriumtuberculosis. L-Cycloserine has anticonvulsant properties and inhibits the synthesis of neurotensin in mouse brains[1][2][3][4].
Phomoxanthone A is a xanthone dimer, which can be isolated from Phomopsis. Phomoxanthone A exhibits antimalarial and antitubercular activities against Plasmodium falciparum (K1, multidrug-resistant strain, IC50 is 0.11 µg/mL) and Mycobacteriumtuberculosis (H37Ra strain, MIC is 0.50 µg/mL). Phomoxanthone A exhibits cytotoxicity in cells KB, BC-1 and Vero, IC50 is 0.99, 0.51 and 1.4 µg/mL, respectively .
Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacteriumtuberculosis, with an IC50 value of 16 μM .
DL-Syringaresinol ((±)-Syringaresinol), a lignin, inhibits UVA-induced upregulation of MMP-1 by suppressing MAPK/AP-1 signaling in human HaCaT keratinocytes and dermal fibroblasts (HDFs). DL-Syringaresinol has antiphotoaging properties against UVA-induced skin aging. DL-Syringaresinol exhibits weak antimycobacterial activity against Mycobacteriumtuberculosis H37Rv .
Amycolatopsin A is a 20-membered macrolide, that can be isolated from a strain of the rare actinomycete Amycolatopsis sp. MST‐108494. Amycolatopsin A shows antimycobacterial activity against Mycobacterium bovis (BCG) and M. tuberculosis (H37Rv) with IC50 values of 0.4 µM and 4.4 µM, respectively .
CdnP-IN-1 (compound c82) is a potent and selective non-nucleotide MTB CDN PDE (CdnP; Mycobacteriumtuberculosis cyclic dinucleotide phosphodiesterase) inhibitor with an IC50 of 18 μM. CdnP-IN-1 does not inhibit the enzymatic activities of three other bacterial CDN PDEs (Yybt, RocR, and GBS-CdnP), a viral CDN PDE (poxin) or mammalian ENPP1 .
RCB18350 is an antituberculosis agent that belongs to the class of isoxazole derivatives. RCB18350 has bacteriostatic activity and inhibits the growth of Mycobacteriumtuberculosis with an MIC of 1.25 μg/mL. RCB18350 is effective against multidrug-resistant Mycobacteriumtuberculosis (MDR-TB) clinical isolates, slow-growing mycobacteria such as Mycobacterium bovis BCG and Mycobacterium avium .
The minimum inhibitory concentration (MIC) of a new 2- (quinoline-4-methoxy) acetamide antituberculotic agent against the reference strain of Mycobacteriumtuberculosis H37Rv was as low as 0.3 μ M. It also inhibited the growth of Mycobacteriumtuberculosis in the macrophage model of tuberculosis infection.
Cefsulodin (sodium) (Standard) is the analytical standard of Cefsulodin (sodium). This product is intended for research and analytical applications. Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacteriumtuberculosis, with an IC50 value of 16 μM .
HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacteriumtuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacteriumtuberculosis infection .
GSK729 is a THPP inhibitor with the activity of inhibiting EchA6 and inhibiting Mycobacteriumtuberculosis. GSK729 can selectively pull down EchA6 in a stereospecific manner, inhibit its activity, inhibit fatty acid synthesis of Mycobacteriumtuberculosis, and has a bactericidal effect in a mouse chronic tuberculosis infection model.
CGI-17341 is a 5-nitroimidazole antibacterial agent that has the activity of inhibiting sensitive and multidrug-resistant strains of Mycobacteriumtuberculosis in vitro and prolonging the survival time of mice infected with Mycobacteriumtuberculosis in vivo in a dose-dependent manner.
Trehalose 6,6'-dimycolate (Cord Factor) is trehalose 6,6'-dimycolate, a cell wall glycolipid of Mycobacteriumtuberculosis, which can be used to simulate inflammation and granuloma induced by Mycobacteriumtuberculosis (MTB) form. Trehalose 6,6′-dimycolate also protects Mycobacteriumtuberculosis from macrophage-mediated killing, inhibits efficient antigen presentation, and reduces the development of protective T cell responses .
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacteriumtuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
DG70 (GSK1733953A), a biphenyl amide, is a respiration inhibitor in Mycobacteriumtuberculosis, inhibits MenG activity with an IC50 value of 2.6 ± 0.6 μM. DG70 inhibits the catalytic methylation of Mycobacteriumtuberculosis demethylmenaquinone methyltransferase enzymes. DG70 can be used for Tuberculosis (TB) research .
Prothionamide-d5 is deuterium labeled Prothionamide (HY-B0306). Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacteriumtuberculosis and Mycobacterium lepraeInhA. Prothionamide can effectively inhibit the growth of Mycobacteriumtuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
Thiocarlide is a potent antibacterial agent. Thiocarlide inhibits Mycobacteriumtuberculosis H37Rv, Mycobacterium bovisBCG, Mycobacterium avium, and Mycobacterium aurum A+ with MICs of 2.5, 0.5, 2.0 and 2.0 μg/mL, respectively .
Prothionamide (Standard) is the analytical standard of Prothionamide (HY-B0306). This product is intended for research and analytical applications. Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacteriumtuberculosis and Mycobacterium lepraeInhA. Prothionamide can effectively inhibit the growth of Mycobacteriumtuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
3,5,4'-Tribromosalicylanilide is a compound with antituberculosis and anti-Mycobacterium abscessus activities, which was found to inhibit the growth of Mycobacteriumtuberculosis and Mycobacterium abscessus and affect gene expression by computational compound repositioning approach.
LysRS-IN-4 (Compound 49) is an orally active Mycobacteriumtuberculosis LysRS (lysyl-tRNA synthetase) inhibitor. LysRS-IN-4 is promising for research of tuberculosis .
α-Mycolic acid, keto cis is a structural lipid component of mycobacterial cell wall. α-Mycolic acid, keto cis can be isolated from Mycobacteriumtuberculosis Canetti. α-Mycolic acid, keto cis significantly modulates membrane permeability and stability, promising for mycobacteriumtuberculosis infection research .
α-Mycolic acid (C80) is a structural lipid component of mycobacterial cell wall. α-Mycolic acid (C80) can be isolated from Mycobacteriumtuberculosis Canetti. α-Mycolic acid (C80) significantly modulates membrane permeability and stability, promising for mycobacteriumtuberculosis infection research .
HT1171 is a potent and selective inhibitor of mycobacteriumtuberculosis proteasome. HT1171 shows strong anti-tuberculosis activity against Mycobacteriumtuberculosis H37Rv with an MIC90 of 2 μg/mL and an MIC of 4 μg/mL. When HT1171 concentration is 100 μM, the inhibition rate of human normal hepatocytes L02 is 53.8%. HT1171 can be used in the research of antitubercular agent .
Cholesterol oxidase, Rhodococcus sp. is a key enzyme in the cholesterol degradation process. It catalyzes the isomerization and oxidation of cholesterol mediated by the coenzyme FAD. Research indicates that cholesterol oxidase plays a crucial role in the pathogenicity of Mycobacteriumtuberculosis by modulating the host macrophage immune response through inhibition of the Toll-like receptor 2 (TLR2) signaling pathway, thereby enhancing the survival of Mycobacteriumtuberculosis. Cholesterol oxidase, from Rhodococcus sp., shows potential for research in the field of tuberculosis .
Quabodepistat (OPC-167832) is a potent and orally active dprE1 inhibitor with an IC50 of 0.258 μM. Quabodepistat has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacteriumtuberculosis .
2-Isopropyl-5-methylanisole is an inhibitor of Mycobacteriumtuberculosis chorismate mutase (CM) with an IC50 of 21.58 μM. The MIC of 2-Isopropyl-5-methylanisole for Mycobacteriumtuberculosis is 152.22 µM. 2-Isopropyl-5-methylanisole holds potential for research in the field of anti-infective studies .
Antimycobacterial agent - 11 (Compound QM7) is a bacteriostatic agent with anti-tuberculosis activity. Its minimum inhibitory concentration (MIC) against Mycobacteriumtuberculosis (Mtb) is 5.58 μg/mL. Antimycobacterial agent - 11 can be used in the research of the anti - infection field, especially in the field of tuberculosis .
NITD-304, an indolcarboxamide, is a MycobacteriumtuberculosisMmpL3 inhibitor. NITD-304 potently inhibits bacterial growth with antitubercular and bactericidal activities. NITD-304 can be used for tuberculosis infections research .
Mycolic acid IIa is a structural lipid component of mycobacterial cell wall. Mycolic acid IIa can be isolated from Mycobacterium bovis BCG. Mycolic acid IIa significantly modulates membrane permeability and stability, promising for mycobacteriumtuberculosis infection research .
MMV688845 is a nontuberculous mycobacteria (NTM) RNA polymerase inhibitor with bactericidal activity against Mycobacterium abscessus and anti-tuberculosis efficacy .
Pyridomycin (Erizomycin) is a selective and low cytotoxic inhibitor of Mycobacteriumtuberculosis that effectively targets InhA. Pyrdomycin is also an antibiotic that can be obtained from metabolites of Dactylosporangium fulvum. Pyrdomycin can be used in the study of bacterial infections such as tuberculosis .
Tuberculosis inhibitor 12 (compound 12) is an oxadiazole derivative and an inhibitor of Mycobacteriumtuberculosis. The inhibition rates of Tuberculosis inhibitor 12 (20 μM) on 7H9-Tw-OADC and 7H9-Tw-OADC reached 82% and 78% respectively .
ZTB23(R) is a potent and selective Mycobacteriumtuberculosis zinc metalloproteinase-1 (Zmp1) inhibitor with Ki value of 0.054 μM. ZTB23(R) can be used for tuberculosis (TB) research .
Ganfeborole hydrochloride (GSK656) is a potent antitubercular agent, acting as an inhibitor of Mycobacteriumtuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM.
Mtb-IN-3 (compound 10c) is an inhibitor of Mycobacteriumtuberculosis (Mtb). Mtb-IN-3 shows selective, potent in vitro antimycobacterial activity without cytotoxicity. Mtb-IN-3 inhibits colony-forming in spleen in the murine tuberculosis model .
SRG-II-19F (dCym-JQ1) is a bromodomain1 of BRDT (BRDTBD1) PROTAC degrader. SRG-II-19F can be used for testing the regulatory effect of ClpC2 on the ClpC1P1P2 protease .
sCNH240 (Compound P1) is an oral active and selective Rv1625c/Cya activator. sCNH240 has significant anti-tuberculosis activity with a MIC90 of 1.24 μM for Mycobacteriumtuberculosis (Mtb) H37Rv strain on cholesterol. sCNH240 can be used for tuberculosis treatment research .
(R,R)-Ethambutol is an antituberculosis compound with tuberculosis inhibitory activity. (R,R)-Ethambutol is often used in combination with other antituberculosis compounds to enhance the efficacy. (R,R)-Ethambutol can also be used to inhibit Mycobacterium avium complex infection and Mycobacterium kansasii infection .
Griselimycin is a compound with antituberculosis activity that exhibits good in vitro and in vivo activity against sensitive and resistant Mycobacteriumtuberculosis, and its cyclohexyl derivative has high transformative potential.
Telacebec ditosylate is a midazopyridine amide compound. Telacebec ditosylate is active against Mycobacteriumtuberculosis H37Rv with an MIC50 of 2.7 nM in culture broth medium.
Faropenem sodium (Standard) is the analytical standard of Faropenem sodium. This product is intended for research and analytical applications. Faropenem sodium is an orally bioavailable penem antibiotic which can efficiently kill Mycobacteriumtuberculosis.
BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.
Telacebec (Q203) is a midazopyridine amide compound. Telacebec is active against Mycobacteriumtuberculosis H37Rv with an MIC50 of 2.7 nM in culture broth medium.
Bedaquiline (fumarate) (Standard) is the analytical standard of Bedaquiline (fumarate). This product is intended for research and analytical applications. Bedaquiline fumarate, a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacteriumtuberculosis infections.
ML338 is a selective small molecule inhibitor probe of non-replicating Mycobacteriumtuberculosis bacilli and is against the non-replicating M. tuberculosis with IC90 and IC99 values of 1 μM and 4 μM, respectively by CFU. ML338 is a invaluable tool for identifying both essential functions and vulnerabilities of the M. tuberculosis bacilli in the nutrient deprivation states. ML338 can be used for the study of M. tuberculosis chemotherapy .
Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacteriumtuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research .
Antitubercular agent-37 is an antibacterial agent. Antitubercular agent-37 has antimycobacterial activity with an MIC values of 0.16 μg/mL. Antitubercular agent-37 can be used for the research of tuberculosis .
NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacteriumtuberculosis H37Rv.
Propioxatin B is a tricyclic sesquiterpenoid compound isolated from the root of vetiver grass. It has anti-tuberculosis activity and inhibitory effects on a variety of drug-resistant mutants of Mycobacteriumtuberculosis. In computer simulation docking studies, it showed binding affinity with bacterial DNA gyrase and has a certain safety in vivo.
S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacteriumtuberculosis lumazine synthases, respectively .
2-Mercaptopyridine N-oxide sodium has bactericidal effect and is against a standard strain of Mycobacteriumtuberculosis H37Rv (ATCC 27294) with MIC90 of 7.20 μM. 2-Mercaptopyridine N-oxide sodium and its complex with iron, gallium, and bismuth have good anti-M. tuberculosis activity. 2-Mercaptopyridine N-oxide sodium has potential for the treatment of tuberculosis .
Rifamycin (Rifamycin SV) is an orally active ansamycin antibiotic. Rifamycin inhibits DNA-dependent RNA synthesis. Rifamycin has antibacterial activity against Mycobacteriumtuberculosis. Rifamycin interferes with hepatic bile acid metabolism. Rifamycin has anti-inflammatory effects. Rifamycin can be used in the study of Mycobacteriumtuberculosis, Bacteroides fragilis infection, and Lipopolysaccharide (HY-D1056B3)-induced inflammation .
Rifamycin sodium (Rifamycin SV monosodium) is an orally active ansamycin antibiotic. Rifamycin sodium inhibits DNA-dependent RNA synthesis. Rifamycin sodium has antibacterial activity against Mycobacteriumtuberculosis. Rifamycin sodium interferes with hepatic bile acid metabolism. Rifamycin sodium has anti-inflammatory effects. Rifamycin sodium can be used in the study of Mycobacteriumtuberculosis, Bacteroides fragilis infection, and Lipopolysaccharide (HY-D1056B3)-induced inflammation .
ABT-255 free base is an orally active anti-bacterial agent. ABT-255 free base exhibits potent in vitro potency (MIC = 0.016-0.031 μg/mL) against drug-susceptible and Rifampin (HY-B0272)- or Ethambutol (HY-B0535)-resistant Mycobacteriumtuberculosis. ABT-255 free base shows efficacy against S. aureus, S. pneumoniae and E. coli and reduces viable counts of drug-resistant Mycobacteriumtuberculosis in CF-1 mice. ABT-255 free base can be used for the study of pulmonary tuberculosis .
Steviolbioside is a sweetener and also an important pharmaceutical intermediate. Steviolbioside can inhibit the proliferation of various tumor cells. Steviolbioside has an MIC of 3.8 µg/mL for Mycobacteriumtuberculosis. Steviolbioside also has antidiabetic activity. Steviolbioside can be used in the research of tuberculosis, diabetes and tumors such as breast cancer .
(Rac)-Bedaquiline is the racemate of Bedaquiline. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacteriumtuberculosis (Mtb) F1FO-ATP synthase through targeting both the c- and the ε-subunit. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
Evybactin is a DNA gyrase inhibitor. Evybactin is a selective inhibitor of Mycobacteriumtuberculosis with a MIC value of 0.25 µg/mL. Evybactin is the first antimicrobial compound found to employ this unusual mechanism of selectivity .
7-Oxo-ganoderic acid Z, a terpenoid, is a nature product that could be isolated from Resina Commiphora. 7-Oxo-ganoderic acid Z has Anti-Mycobacteriumtuberculosis activity .
Antimycobacterial agent-1 (compound 33) has selectively antimycobacterial activity against Mycobacteriumtuberculosis(M. tuberculosis) H37Ra with a MIC value of 1 μg/ml. Antimycobacterial agent-1 has relatively low cytotoxicity in normal cells (Vero cells IC50 = 143.2 μg/ml) .
MmpL3-IN-5 (Compound 3G) is a MmpL3 inhibitor. MmpL3-IN-5 has an antitubercular activity with a pMIC of 7.0 μM for Mycobacteriumtuberculosis H37Rv strain. MmpL3-IN-5 can be used for tuberculosis research .
Thiophene-2 (TP2) is a specific polyketide synthase 13 (Pks13) inhibitor. Thiophene-2 inhibits mycolic acid biosynthesis and rapidly leads to mycobacterial cell death. Thiophene-2 is active against Mycobacteriumtuberculosis with a MIC value of 1 μM, and has potent anti-tuberculosis activity .
InhA-IN-8 (compound 6c) is an orally active inhibitor of MycobacteriumtuberculosisInhA (enoyl ACP reductase). InhA-IN-8 has good inhibitory activity against Mtb UalRv (MIC = 0.5-1 μg/mL). InhA-IN-8 can be used in research on acute tuberculosis model mice .
Mtb-IN-13 (Compound 5f) is an inhibitor of Mycobacteriumtuberculosis (Mtb), with a MIC of 0.25 μg/mL. The Ki values of MTTB-in-13 for MtCA1, MtCA2, MtC, and 3 are 0.6023, 0.0780, and 0.1994 μM, respectively. Mtb-IN-13 can be used in the research of tuberculosis .
UGM-IN-3 (compound 10a) is a UDP-galactopyranose mutase (UGM) inhibitor with a Kd of 66 μM. UGM-IN-3 inhibits the growth of Mycobacteriumtuberculosis with a MIC value of 6.2 μg/mL .
Enzyme-IN-3 disodium (compound 7) is a selective inhibitor of Mycobacteriumtuberculosisshikimate kinase with an IC50 of 1.6 μM. Enzyme-IN-3 disodium has antibacterial activity .
HC2210 has an antibacterial effect against Mycobacterium abscessus (Mab) (EC50: 0.72 µM). HC2210 modulates the expression of Mab genes related to oxidative stress and lipid metabolism. HC2210 can be used in the study of Mab infection .
Quabodepistat-d7 (OPC-167832-d7) is deuterium labeled Quabodepistat. Quabodepistat (OPC-167832) is a potent and orally active dprE1 inhibitor with?an IC50 of 0.258 μM. Quabodepistat has antituberculosis activity and can be used for the research of tuberculosis?caused by?Mycobacteriumtuberculosis .
BM212 (Standard) is the analytical standard of BM212. This product is intended for research and analytical applications. BM212 is a potent Mycobacterial membrane protein Large 3 (MmpL3) inhibitor. BM212 has strong bactericidal activity against both M. tuberculosis and some nontuberculosis mycobacteria. BM212 exhibits antimycobacterial activity against M. tuberculosis H37Rv with an MIC of 5 µM .
BM212 is a potent Mycobacterial membrane protein Large 3 (MmpL3) inhibitor. BM212 has strong bactericidal activity against both M. tuberculosis and some nontuberculosis mycobacteria. BM212 exhibits antimycobacterial activity against M. tuberculosis H37Rv with an MIC of 5 µM .
PptT-IN-4 (Compound 3a) is a PptT inhibitor (IC50: 0.71 μM). PptT-IN-4 inhibits Mtb H37Rv with a MIC value of 42 μM. PptT-IN-4 also inhibits hERG, hCav1.2, and hNav1.5 channels with IC50s of 11 μM, 8.1 μM, 6.9 μM respectively .
Capreomycin is a macrocyclic peptide antibiotic. Capreomycin can be used for anti-multidrug-resistant-tuberculosis research. Capreomycin can inhibit phenylalanine synthesis in in mycobacterial ribosomes translation
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacteriumtuberculosis H37Rv with a MIC value of 0.1 μg/mL .
Mtb against-1 (compound 17af) is an inhibitor of Mycobacteriumtuberculosis, with IC90 values of 1.2 μM and 0.9 μM for the wild-type and LepB low-deformation strains, respectively .
MtTMPK-IN-1 (compound 3) is a potent Mycobacteriumtuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 2.5 μM. MtTMPK-IN-1 has moderate to weak activity against Mtb H37Rv and low cytotoxicity in human fibroblast cells MRC-5. MtTMPK-IN-1 can be used for researching tuberculosis .
Bedaquiline (Standard) is the analytical standard of Bedaquiline. This product is intended for research and analytical applications. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacteriumtuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
Bedaquiline impurity 2-d6 is deuterium labeled Bedaquiline. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacteriumtuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
Caprazene is an antimycobacterial compound and precursor molecule for semi-synthetic antibacterial antibiotics, used for studies on tuberculosis and Mycobacterium avium complex infections, which can be isolated from the acid-treated caprazamycin (CPZ) A-G mixture .
(Rac)-Sativan is an isoflavanoid with a broad spectrum of antimicrobial activity against bacteria and phytopathogenic fungi. (Rac)-Sativan exhibits antituberculosis activity against Mycobacteriumtuberculosis H37Rv, with MIC values of 50 µg/mL .
Mtb-IN-8 (compound 5jb) is an orally active inhibitor of Mycobacteriumtuberculosis (Mtb) with MIC values of 0.03 μg/mL for H37Rv and 0.125-0.06 μg/mL for MDR-Mtb, respectively .
InhA-IN-9 (compound 7h) is a MycobacteriumtuberculosisInhA (an enoyl ACP-reductase) inhibitor. InhA-IN-9 could bind to InhA. InhA-IN-9 shows a antituberculosis activity at MIC value of 2 μg/mL .
(Rac)-Bedaquiline-d6 is the deuterium labeled Bedaquiline (HY-14881) . Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacteriumtuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
Mtb-IN-2 (compound 10c) is an antimicrobial agent against Mycobacteriumtuberculosis (Mtb), without cytotoxicity. Mtb-IN-2 significantly decreases colony-forming units (CFU) in spleen of murine tuberculosis models, and distinguishes both drug-sensitive and drug-resistant Mtb H37Rv strains. Mtb-IN-2 affects methionine metabolism but not folate pathway directly.
Rifamycin (sodium) (Standard) is the analytical standard of Rifamycin (sodium). This product is intended for research and analytical applications. Rifamycin sodium (Rifamycin SV sodium) is an orally active ansamycin antibiotic. Rifamycin sodium inhibits DNA-dependent RNA synthesis. Rifamycin sodium has antibacterial activity against Mycobacteriumtuberculosis. Rifamycin sodium interferes with hepatic bile acid metabolism. Rifamycin sodium has anti-inflammatory effects. Rifamycin sodium can be used in the study of Mycobacteriumtuberculosis, Bacteroides fragilis infection, and Lipopolysaccharide (HY-D1056B3)-induced inflammation .
4-Nitrobenzoic acid is a nitroaromatic compound that can be used in the synthesis of other active compounds. 4-Nitrobenzoic acid is also an inhibitor agent, which can be used for the recognition of the Mycobacteriumtuberculosis complex and differentiation from non-tuberculous mycobacteria .
FolB-IN-1 (Compound 3e) is an inhibitor of FolB that can suppress the activity of FolB enzyme from Mycobacteriumtuberculosis (MtFolB). FolB-IN-1 exhibits antimycobacterial activity with an MIC value of 40 µg/mL (108 µM) .
Ganorbiformin B is a lanostane triterpenoid. Ganorbiformin B shares the same lanostane skeleton with known ganoderic acids. The C-3 epimer of ganoderic acid T exhibits potent antimycobacterial activity against Mycobacteriumtuberculosis H37Ra .
Antitubercular agent-30 is an antibacterial agent against Mycobacteriumtuberculosis (MIC=50 μg/mL). Antitubercular agent-30 has little cytotoxic effect on murine macrophage cells (LD85=~100 μg/mL) .
Steviolbioside (Standard) is the analytical standard of Steviolbioside (HY-N2547). This product is intended for research and analytical applications. Steviolbioside is a sweetener and also an important pharmaceutical intermediate. Steviolbioside can inhibit the proliferation of various tumor cells. Steviolbioside has an MIC of 3.8 µg/mL for Mycobacteriumtuberculosis. Steviolbioside also has antidiabetic activity. Steviolbioside can be used in the research of tuberculosis, diabetes and tumors such as breast cancer .
Pasiniazid is a chemical complex formed by Isoniazid (HY-B0329) and Para-aminosalicylic acid in a 1:1 molar ratio. Pasiniazid is an antibacterial agent. Pasiniazid is rapidly decomposed into isoniazid and para-aminosalicylic acid in the gastrointestinal tract. Isoniazid exerts a bactericidal effect, while para-aminosalicylic acid delays the acetylation process of isoniazid. Pasiniazid has antibacterial activity against Mycobacteriumtuberculosis. Pasiniazid can be used in tuberculosis research .
Mtb-cyt-bd oxidase-IN-5 (compound 1k) is a Mycobacteriumtuberculosis (Mtb) cytochrome bd (cyt-bd) oxidase (MtbCyt-bd Oxidase) inhibitor with an IC50 value of 0.37 μM. Mtb-cyt-bd oxidase-IN-5 can effectively inhibit the growth of Mtb (MIC= 256 μM). Mtb-cyt-bd oxidase-IN-5 can be used in the study of tuberculosis .
TBA-7371 is an orally active and non-covalent inhibitor of Decaprenylphosphoryl-β-D-ribose oxidase (DprE1) of Mycobacteriumtuberculosis (MIC=0.64 μg/mL). TBA-7371 can block the synthesis of arabinose in the bacterial cell wall, resulting in cell wall structural defects, thereby exerting an anti-tuberculosis effect. TBA-7371 can be used in the research of anti-tuberculosis drugs and has a synergistic bactericidal effect with Bedaquiline (HY-14881) and other drugs .
Antitubercular agent-18 (Compound 9a) is an antitubercular agent with MIC values of 2, 2, 2 and 128 µg/ml against M. tuberculosis H37Rv, Spec. 192, Spec 210 and Spec. 800, respectively. Antitubercular agent-18 shows highly selective antimycobacterial effects .
Antitubercular agent-17 (Compound 8a) is an antitubercular agent with MIC values of 2, 2, 2 and 128 µg/ml against M. tuberculosis H37Rv, Spec. 192, Spec 210 and Spec. 800, respectively. Antitubercular agent-17 shows highly selective antimycobacterial effects .
Mtb-IN-5 (compound (-)17j) is an isoxazole, with anti-Mycobacteriumtuberculosis (Mtb) activity. Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant .
PXYD3 is a ribosomal protein S1 (RpsA) antagonist with Kds of 5.66 and 6.91 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of MycobacteriumTuberculosis (Mtb) .
BTZ043 (Standard) is the analytical standard of BTZ043. This product is intended for research and analytical applications. BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosis H37Rv and Mycobacterium smegmatis, respectively.
4-Allylcatechol (4-Allylpyrocatechol) is a xylan which has oral activity and can be isolated from the root of Piper taiwanense. 4-Allylcatechol has a strong inhibitory activity against collagen-induced platelet aggregation (IC50 = 5.3 μM). In addition, 4-Allylcatechol has anti-tuberculosis activity against Mycobacteriumtuberculosis H37Rv (MIC = 27.6 μg/mL) .
GWP-042 is a potent inhibitor of mycobacterial alanine dehydrogenase (Ald) Rv2780, with the IC50 of 0.21 μM. GWP-042 has antimicrobial activity against M. tuberculosis infection in vivo .
BRD-9327 is an inhibitor of EfpA. BRD-9327 binds in the outer vestibule without complete blockade of the substrate path to the outside, suggesting its possible inhibition of the movement necessary for alternate access of the transporter. BRD-9327 can be used for anti-tuberculosis study .
Antibacterial agent 122 (compound 15) is a thiourea derivative with anti-mycobacterial activity and low cytotoxicity. Antibacterial agent 122 can be used for tuberculosis-related studies .
Mtb-IN-6 (Compound C10) is a Mycobacteriumtuberculosis(Mtb) respiration inhibitor. Mtb-IN-6 can enhance the bactericidal activity of isoniazid (INH, HY-B0329). Mtb-IN-6 inhibits WT Mtb with an IC50 of 25 µM .
Pks13-IN-2 (Compound 43) is an orally active inhibitor of Pks13. Pks13-IN-2 exhibits inhibitory activity against Mycobacteriumtuberculosis H37Rv, with a MIC of 0.8-1.8 μM. Pks13-IN-2 shows good metabolic stability in mouse liver microsomes and hepatocytes. Pks13-IN-2 can be used for tuberculosis research .
Antituberculosis agent-13 (Compound 11) inhibits Mycobacteriumtuberculosis, that inhibits Mtb wildtype and mutated strains with IC50 of 4-62.5 nM. Antituberculosis agent-13 exhibits anti-leukemia activity that inhibits MOLM-13 with IC50 of 3.8 μM .
3-(1-Carboxyvinyloxy)benzoic acid is an inhibitor of MbtI(Mycobacteriumtuberculosis salicylate synthase) and AS (Serratia marcescens arginine synthase), with Ki values of 500 and 3.2 µM, respectively. 3-(1-Carboxyvinyloxy)benzoic acid has antibacterial activity and can be used in anti-infection research .
PNU-101603 is a sulfoxide metabolite of Sutezolid (HY-10392). PNU-101603 alone or combined with SQ109 (HY-14989) shows excellent activity against Mycobacteriumtuberculosis (MTB), as well as against agent-susceptible and multidrug-resistant TB .
Mab Aspartate Decarboxylase-IN-1 is a potent aspartate decarboxylase (PanD) inhibitor with an IC50 value of 56.3 μM. Mab Aspartate Decarboxylase-IN-1 shows antibacterial activity .
MtTMPK-IN-2 (compound 15) is a potent Mycobacteriumtuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 1.1 μM. MtTMPK-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-2 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 6.1 μM). MtTMPK-IN-2 can be used for researching tuberculosis .
Antitubercular agent-52 (Compound 7k) is an antitubercular agent targeting Mycobacteriumtuberculosis (Mtb). Antitubercular agent-52 selectively inhibits the cytochrome bcc (cyt-bcc) electron transport chain of Mtb and also acts on cytochrome bd (cyt-bd). Antitubercular agent-52 blocks electron transfer and ATP production by interfering with the key energy metabolism pathway of Mtb. Antitubercular agent-52 is promising for research of tuberculosis .
MtTMPK-IN-3 (compound 25) is a potent Mycobacteriumtuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 value of 0.12 μM. MtTMPK-IN-3 has inhibitory activity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-3 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 12.5 μM). MtTMPK-IN-3 can be used for researching tuberculosis .
TAM-16 is a potent and orally active polyketide synthase 13 (Pks13) inhibitor with an IC50 value of 0.32 μM. TAM-16 has promising activity against Mycobacteriumtuberculosis. TAM-16 inhibits hERG cardiac ion channel .
Anti-infective agent 8 (compound 9d) is an antibacterial agent with an MIC of 0.5 μg/mL against Staphylococcus aureus and Mycobacteriumtuberculosis H37Rv. Anti-infective agent 8 has anti-biofilm activity and significantly reduces Staphylococcus aureus biofilm formation .
Lansoprazole sulfide-d4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole. Lansoprazole Sulfide is an orally active anti-TB (Mycobacteriumtuberculosis) agent with IC50 values of 0.59 μM intracellularly and 0.46 μM in broth .
DprE1-IN-13 (Compound 42) is the inhibitor for decaprenyl-phosphoryl-β-d-ribose oxidase (DprE1) with IC50 of 12.72 μM. DprE1-IN-13 inhibits Mycobacteriumtuberculosis H37Ra with MIC50 of 1.071 μM .
Thiacetazone (Standard) is the analytical standard of Thiacetazone. This product is intended for research and analytical applications. Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacteriumtuberculosis H37Rv with a MIC value of 0.1 μg/mL[1].
Mtb-IN-4 (compound 17h) is a nontoxic isoxazole, with anti-Mycobacteriumtuberculosis (Mtb) activity (IC50=0.70 μM). Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant .
Cordycepin (3'-Deoxyadenosine) is a nucleoside derivative and inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner . Cordycepin kills Mycobacteriumtuberculosis through hijacking the bacterial adenosine kinase .
Miaosporone A, an angucyclic quinone, exhibits antimalarial activity against Plasmodium falciparum K1 and antibacterial activity against Mycobacteriumtuberculosis with respective IC50 values of 2.5 and 2.4 μM and displays cytotoxic activities against both cancerous (MCF-7 and NCI-H187) and nonmalignant (Vero) cells .
Biotin protein ligase-IN-1 (Compound Bio-9) is an inhibitor of biotin protein ligase (BPL) with a Kd value of 7 nM. Biotin protein ligase-IN-1 exhibits antibacterial activity, with MIC values of 0.2 and 20 μM against Staphylococcus aureus (including MRSA and MSSA) and Mycobacteriumtuberculosis, respectively .
SEQ-9 is an orally active Mycobacteriumtuberculosis (Mtb) 23S bacterial ribosome inhibitor with an IC50 of approximately 170 nM for unmethylated Mtb ribosomes. SEQ-9 also potently inhibits A2296 methylated ribosomes. SEQ-9 can be used to study bacterial infection and drug resistance .
Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue without noticeable cytotoxicity. Tuberculosis inhibitor 5 is an anti-tuberculosis agent .
Transketolase-IN-4 is a potent transketolase inhibitor (IC50=3.9 μM). Transketolase-IN-4 inhibits tumor cell proliferation of SW620, LS174T, and MIA PaCa-2. Transketolase-IN-4 is a possible Mycobacteriumtuberculosis DXS inhibitor, with an IC50 value of 114.1 μM .
Antituberculosis agent-10 (Compound 9) has excellent antibacterial activity against Mycobacteriumtuberculosis (MIC = 0.3 μM). Antituberculosis agent-10 inhibits protein synthesis by targeting the 50S ribosomal subunit of the bacterium, thus exerting its antibacterial effect. Antituberculosis agent-10 is orally active .
Cy3-NO2-Tre is a nitroreductase-responsive cyanine-based fluorescent probe that specifically labels Mycobacteriumtuberculosis (Mtb). Cy3-NO2-tre generated fluorescence after activation by a specific nitroreductase, Rv3368c, which is conserved in the Mycobacteriaceae. Cy3-NO2-tre effectively imaged mycobacteria within infected host cells, tracked the infection process, and visualized Mycobacterium smegmatis being endocytosed by macrophages (Ex/Em= 540-550/575-625 nm) .
ATP synthase inhibitor 3 (compound PT6) is an orally active inhibitor of mycobacterial F-ATP synthase (IC50=0.788 μM). ATP synthase inhibitor 3 inhibits the growth of Mycobacteriumtuberculosis H37Rv strain (ATCC-27294) in vitro and depletes intracellular ATP levels at an IC50 value of 30μM .
4-Nitrobenzoic acid-d2 is the deuterium labeled 4-Nitrobenzoic acid (HY-Y0607). 4-Nitrobenzoic acid is a nitroaromatic compound that can be used in the synthesis of other active compounds. 4-Nitrobenzoic acid is also an inhibitor agent, which can be used for the recognition of the Mycobacteriumtuberculosis complex and differentiation from non-tuberculous mycobacteria .
4-Nitrobenzoic acid-d4 is the deuterium labeled 4-Nitrobenzoic acid (HY-Y0607). 4-Nitrobenzoic acid is a nitroaromatic compound that can be used in the synthesis of other active compounds. 4-Nitrobenzoic acid is also an inhibitor agent, which can be used for the recognition of the Mycobacteriumtuberculosis complex and differentiation from non-tuberculous mycobacteria .
Celiprolol (hydrochloride) (Standard) is the analytical standard of Celiprolol (hydrochloride). This product is intended for research and analytical applications. Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure .
Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
Pyrazinamide- 13C, 15N is 15N and 13C labeled Pyrazinamide (HY-B0271). Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
Pyrazinamide (Standard) is the analytical standard of Pyrazinamide. This product is intended for research and analytical applications. Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
DuP-721 is a broad spectrum and orally active antibacterial agent against a variety of clinically susceptible and resistant bacteria, especially M. tuberculosis .
Cordycepin (Standard) is the analytical standard of Cordycepin. This product is intended for research and analytical applications. Cordycepin (3'-Deoxyadenosine) is a nucleoside derivative and inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner . Cordycepin kills Mycobacteriumtuberculosis through hijacking the bacterial adenosine kinase .
Cefsulodin (SCE-129) sodium is a third generation β lactam antibiotic and member of the cephems subgroup of antibiotics. Cefsulodin sodium inhibits cell wall synthesis by competitively inhibiting penicillin binding protein (PBP) cross-linking and transpeptidation of peptidogly. Cefsulodin sodium is a potent tyrosine phosphatase inhibitor against mPTPB, a virulent phosphatase from Mycobacteriumtuberculosis, with an IC50 value of 16 μM .
4-Nitrobenzoic acid (Standard) is the analytical standard of 4-Nitrobenzoic acid (HY-Y0607). This product is intended for research and analytical applications. 4-Nitrobenzoic acid is a nitroaromatic compound that can be used in the synthesis of other active compounds. 4-Nitrobenzoic acid is also an inhibitor agent, which can be used for the recognition of the Mycobacteriumtuberculosis complex and differentiation from non-tuberculous mycobacteria .
Antimycobacterial agent-7 (compound 4) is a 1,2,4-triazole anti-tuberculosis agent (MIC: 2 μg/mL). Antimycobacterial agent-7 inhibits Mtb KatG and causes the accumulation of ROS in Mtb cells. ROS produces oxidative damage, leading to the death of Mtb .
CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo .
ML406 (Standard) is the analytical standard of ML406. This product is intended for research and analytical applications. ML406 is a small molecule probe that shows anti-tubercular activity via M.tuberculosis BioA (DAPA synthase) enzyme inhibition with an IC50 of 30 nM. M.tuberculosis BioA is an enzyme involved in biotin biosynthesis in M.tuberculosis[1].
ML406 is a small molecule probe that shows anti-tubercular activity via M.tuberculosis BioA (DAPA synthase) enzyme inhibition with an IC50 of 30 nM. M.tuberculosis BioA is an enzyme involved in biotin biosynthesis in M.tuberculosis .
Mtb-cyt-bd oxidase-IN-7 is a cytochrome bd terminal oxidase (Cyt-bd) inhibitor with a Kd value of 4.17 μM. Mtb-cyt-bd oxidase-IN-7 shows anti-tuberculosis activities .
Mtb-IN-10 (Compound P15) is a Rv1625c/Cya activator that regulates cAMP metabolism to influence the growth of Mycobacteriumtuberculosis (Mtb). Mtb-IN-10 exhibits an EC50 of 1.96 µM in an Mtb-infected macrophage model and demonstrates 58.0% oral bioavailability in mice at a 20 mg/kg dose. It may regulate intracellular signaling and disrupt cholesterol metabolism in Mtb, thereby inhibiting bacterial proliferation. Mtb-IN-10 holds potential for tuberculosis (TB) research, particularly for combating multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) Mtb strains .
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines .
Dehydrocostus Lactone ((-)-Dehydrocostus lactone) is a natural sesquiterpene that can be isolated from Saussurea lappa. Dehydrocostus Lactone has multiple activities such as anti-inflammatory, antibacterial, anti-tumor, and immunomodulatory effects. Dehydrocostus Lactone has an MIC of 2 µg/mL against Mycobacteriumtuberculosis. Dehydrocostus Lactone can also inhibit the killing activity of cytotoxic T lymphocytes and induce apoptosis in tumor cells .
Saringosterol is found in Sargassum muticum. Saringosterol is a LXR agonist that lowers cholesterol. saringosterol inhibits the mRNA and protein expression of peroxisome proliferator-activated receptor γ and CCAAT enhancer-binding protein α in 3T3-L1 cells. Saringosterol has anti-Mycobacteriumtuberculosis activity. Saringosterol can be used in anti-obesity and anti-atherosclerosis research .
GaMF1.39 is an antimycobacterial compound, targeting the F-ATP synthase subunit γ. GaMF1.39 displays enhanced anti-tuberculosis activity in combination with ETC inhibitors .
SPR719 (VXc-486) is an orally active gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple agent-sensitive isolates and drug-resistant isolates of Mycobacteriumtuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively. SPR719 is promising for research of lung disease caused by non-tuberculous mycobacteria (NTM) .
Celastramycin A isomer is an isomer of Celastramycin A (HY-122292), an antibiotic against Gram-negative bacteria and Mycobacteriumtuberculosis with an MIC of 0.05-3.1 μg/mL. Celastramycin A exerts immunosuppressive effects in Drosophila ex vivo via the immunodeficiency pathway (IC50 of 8 ng/mL), inhibits human innate immune responses via the TNF-α pathway, and inhibits IL-8 production in HUEVC with an IC50 of 60 ng/mL .
VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacteriumtuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
Antibacterial agent 96 (compound 4k) is a potent antibacterial agent. Antibacterial agent 96 shows antitubercular activity against agent-susceptible and multidrug-resistantMycobacterium tuberculosis (M. tuberculosis) strains. Antibacterial agent 96 shows toxicity to HepG2 and Vero cells .
SMARt751 targets the transcriptional regulatory factor VirS, inhibits its DNA binding ability, upregulates the mymA operon expression, thereby activating Ethionamide (HY-B0276), enhancing the antimicrobial activity of Ethionamide. SMARt751 enhances the antibacterial activity of Ethionamide against M. tuberculosis, reverses the Ethionamide resistance. SMARt751 improves the antibacterial effect of Ethionamide and reduces its effective dose in mouse models. SMARt751 can cross blood brain barrier .
SufS-IN-1, a (2R,3R)-3-ethoxycarbonylaziridine-2-carboxylic acid (EAC), is a selective Cysteine desulfurase type II (SufS) inhibitor. SufS-IN-1 significantly inhibits the SufS activity by covalently binding to the cofactor PLP to form a stable PLP-ligand conjugates. SufS-IN-1 can be used for pathogenic microorganisms research, such as Plasmodium falciparum, Staphylococcus aureus and Mycobacteriumtuberculosis .
(+)-(3R,8S)-Falcarindiol is a polyacetylene found in carrots, has antimycobacterial activity, with an IC50 of 6 μM and MIC of 24 μM against Mycobacteriumtuberculosis H37Ra . Antineoplastic and anti-inflammatory activity . (+)-(3R,8S)-Falcarindiol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacteriumtuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic) .
Dehydrocostus Lactone (Standard) ((-)-Dehydrocostus lactone (Standard)) is the analytical standard of Dehydrocostus Lactone (HY-N0591). This product is intended for research and analytical applications. Dehydrocostus Lactone is a natural sesquiterpene that can be isolated from Saussurea lappa. Dehydrocostus Lactone has multiple activities such as anti-inflammatory, antibacterial, anti-tumor, and immunomodulatory effects. Dehydrocostus Lactone has an MIC of 2 µg/mL against Mycobacteriumtuberculosis. Dehydrocostus Lactone can also inhibit the killing activity of cytotoxic T lymphocytes and induce apoptosis in tumor cells.
DXR-IN-4 (Compound 12a) is the inhibitor for 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR). DXR-IN-4 inhibits DXR in Plasmodium falciparum Pf DXR, Escherichia coli Ec DXR, and Mycobacteriumtuberculosis Mt DXR with IC50s of 18, 4.9 and 89 nM, respectively. DXR-IN-4 exhibits antimalarial activity that inhibits P. falciparum strains 3D7 and Dd2 with IC50 of 11 μM and 12 μM .
ND-011992 is a reversible, selective quinazoline-type inhibitor targeting quinone reductases and quinol oxidases. ND-011992 inhibits respiratory complex I and bo3 oxidase in addition to bd-I and bd-II oxidases in E. coli strain BL21*Δcyo with the IC50 of 0.12, 2.47, 0.63 and 1.3 μM, respectively. ND-011992 can be used for tuberculosis study .
Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells . Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitory activity against Mycobacteriumtuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia .
Tin(IV) mesoporphyrin IX dichloride (Stannsoporfin) is an orally active heme oxygenase (HO) inhibitor. Tin(IV) mesoporphyrin IX dichloride increases DENV RNA replication. Tin(IV) mesoporphyrin IX dichloride enhances the bactericidal activity of the SPaO regimen against chronic Mycobacteriumtuberculosis (Mtb)-infected mice. Tin(IV) mesoporphyrin IX dichloride exhibits antitumor effects. Tin(IV) mesoporphyrin IX dichloride is being developed to prevent the development of jaundice in infants with hyperbilirubinemia .
BB2-50F is an antimicrobial agent and succinate dehydrogenase and F1Fo-ATP synthase inhibitor. BB2-50F induces ROS. BB2-50F inhibits succinate oxidation and reduces tricarboxylic acid (TCA) cycle activity. BB2-50F inhibits the growth of Mycobacteriumtuberculosis H37Rv and its auxotrophic, attenuated derivative mc2 6230 (ΔRD1, ΔpanCD) with an MIC of 8 μM .
NADH-IN-3 (Compound C4-1) is a NADH inhibitor with a MIC of 4 μg/mL (13.042 μM) for type II NADH dehydrogenase of Mycobacteriumtuberculosis (Mtb). NADH-IN-3 significantly interrupts ATP synthesis, shows potent inhibitory effects against mono (Rifampicin (HY-B0272) and Isoniazid (HY-B0329)) and multi drug-resistant (Mtb) strains and an anti-bactericidal activity against HepG2 cells with low cytotoxicity (SI: 16.52) .
Antimycobacterial agent-6 (compound 25) is a potent inhibitor of Mycobacteriumtuberculosis (Mtb)，targeting to both wild-type and fluoroquinolone-resistant Mtb strains. Antimycobacterial agent-6 inhibits Mtb DprE1-C387S mutant with MIC90s of 0.9 μM (H37Rv)，0.9 μM (MoxR)，0.5 μM (DprE1-P116S)，respectively .
Antimycobacterial agent-12 (Compound Ec42), a derivative of Platensimycin (HY-127146), is a dual-functional inhibitor KasA and KasB. Antimycobacterial agent-12 has antibacterial activity with a MICs of 2, 2 and 4 μg/mL against Staphylococcus aureus ATCC 29213, Mycobacterium smegmatis and its Isoniazid (HY-B0329)-resistant strain, respectively. Antimycobacterial agent-12 has a superior antimycobacterial activity in M. smegmatis-infected mouse models. Antimycobacterial agent-12 can be used for tuberculosis research .
Fudapirine, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. Fudapirine exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for agent susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. Fudapirine also inhibits hERG channel with the IC50 of 1.89 μM.
(22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid (compound 15) is an antitubercular agent with MIC value of 12.5 μg/mL for Mycobacteriumtuberculosis H37Ra. (22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid shows cytotoxicity with IC50 value of 32 μM for Vero cells .
beta-Mangostin (Standard) is the analytical standard of beta-Mangostin. This product is intended for research and analytical applications. beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacteriumtuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic) .
LMP-420 is a selective tumor necrosis factor-α (TNF-α) inhibitor. LMP-420 reduces the release of pro-inflammatory cytokines (e.g., IL-1β, IL-2), inducing the expression of anti-inflammatory cytokine IL-10 and anti-apoptotic molecules SOCS-1 and Mn-SOD. LMP-420 also downregulates chemokines (e.g., IP-10, MCP-1) to reduce immune cell infiltration. LMP-420 is promising for research of type 1 diabetes mellitus, inflammatory diseases (e.g., colitis), and HIV-Mycobacteriumtuberculosis coinfection .
Eperezolid (PNU-100592) is an orally active protein synthesis inhibitor that targets the bacterial 50S ribosomal subunit. Eperezolid competitively binds to a specific site on the ribosomal 50S subunit (overlapping with the binding sites of chloramphenicol (HY-B0239) and lincomycin (HY-117660)) to inhibit the translation initiation stage and exert antibacterial activity. Eperezolid can induce host cell autophagy to enhance the clearance of intracellular mycobacteria, and its MIC90 for Staphylococcus aureus and Enterococcus is 1-4 μg/mL. Eperezolid is mainly used for antibacterial research on infections with Gram-positive bacteria such as methicillin-resistant (HY-121544) Staphylococci and vancomycin-resistant (HY-B0671) Enterococci, as well as infections with intracellular bacteria such as Mycobacteriumtuberculosis .
TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 has immunomodulatory effects and can be used in the study of tuberculosis and cancer immunotherapy .
TL8-506 (GMP) is TL8-506 (HY-20457) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 has immunomodulatory effects and can be used in the study of tuberculosis and cancer immunotherapy .
Eriochrome black T, Indicator is a complexing agent for metal ions (e.g., Ca 2+, Mg 2+) and is used as an indicator in complexometric titrations. Eriochrome black T, Indicator forms colored complexes with metal ions through covalent coordination bonds, and indicates the endpoint of the titration by color change. Eriochrome black T, Indicator can be used as an anionic azo dye in photocatalytic degradation studies to evaluate the performance of photocatalysts. The reaction solution of Eriochrome black T, Indicator combined with Mg 2+ is initially purple. During loop-mediated isothermal amplification (LAMP), the color changes from purple to sky blue due to the consumption of Mg 2+ by the formation of magnesium pyrophosphate, indicating a positive reaction. The optimal concentration of Eriochrome black T, Indicator in LAMP is 60 μM, and the detection limit for Mycobacteriumtuberculosis is 1 pg DNA/reaction .
Mebeverine alcohol (Standard) is an analytical standard for Mebeverine alcohol. This product is intended for research and analytical applications. Eperezolid (PNU-100592) is an orally active protein synthesis inhibitor that targets the bacterial 50S ribosomal subunit. Eperezolid competitively binds to a specific site on the ribosomal 50S subunit (overlapping with the binding sites of Chloramphenicol (HY-B0239) and Lincomycin (HY-117660)) to inhibit the translation initiation stage and exert antibacterial activity. Eperezolid can induce host cell autophagy to enhance the clearance of intracellular mycobacteria, and its MIC90 for Staphylococcus aureus and Enterococcus is 1-4 μg/mL. Eperezolid is mainly used for antibacterial research on infections with Gram-positive bacteria such as methicillin-resistant (HY-121544) Staphylococci and vancomycin-resistant (HY-B0671) Enterococci, as well as infections with intracellular bacteria such as Mycobacteriumtuberculosis .
5-Nitro-1,10-phenanthroline (5-NP), is a o-Phenanthroline (HY-W004544) derivative, as a mediator of glucose oxidase (GOX) with antituberculous activity. 5-Nitro-1,10-phenanthroline can be applied as redox mediators for oxidases and is suitable for the development of reagent-less biosensors and biofuel cells .
Anti-inflammatory agent 15 (compound 29) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 15 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 2.3 and 7.8 μM, respectively. Anti-inflammatory agent 15 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 15 can be used for tuberculosis (TB) research .
Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research .
L-Ornithine (hydrochloride) (Standard) is the analytical standard of L-Ornithine (hydrochloride). This product is intended for research and analytical applications. L-Ornithine hydrochloride is a non-proteinogenic amino acid, is mainly used in urea cycle removing excess nitrogen in vivo. L-Ornithine hydrochloride shows nephroprotective .
Maltopentaose (Standard) is the analytical standard of Maltopentaose. This product is intended for research and analytical applications. Maltopentaose is the shortest chain oligosaccharide that can be classified as maltodextrin and is also used in a study to investigate glycation and phosphorylation of α-lactalbumin.
I-A09 and its derivatives, specifically 1,2,3-triazole-adamantylacetamide hybrids (5a–u), exhibit significant antitubercular activity. These hybrids were synthesized using copper-catalyzed click chemistry, combining bioactive fragments from antitubercular I-A09 and substituted adamantyl urea. The compound N-(1-adamantyl)-2-azido acetamide was reacted with various alkyl/aryl acetylenes to produce new analogues. Among them, N-(1-adamantan-1-yl)-2-(4-(phenanthren-2-yl)-1H-1,2,3-triazol-1-yl)acetamide (5t) showed the most promise with a minimum inhibitory concentration (MIC) of 3.12 μg/mL against Mycobacteriumtuberculosis H37Rv, and a selectivity index greater than 15 .
Tuberculosis (TB), usually caused by bacteria (Mycobacteriumtuberculosis), is an infectious disease that mainly affects the lungs. According to the statistics of the World Health Organization (WHO), 10 million people suffer from tuberculosis every year, and 1.5 million people die of tuberculosis every year, which makes tuberculosis the number one killer of infectious diseases.
Tuberculosis can be cured through the standard 6-month course of treatment of four kinds of antibiotics. Common drugs include rifampicin and isoniazid. In some cases, TB bacteria do not respond to standard drugs, that is, patients with drug-resistant tuberculosis. The treatment of drug-resistant tuberculosis takes longer and is more complex. In the face of the resurgence of tuberculosis in the world and the rapid emergence of multi drug resistant tuberculosis, it is very important to develop new anti-tuberculosis drugs or new clinical treatment schemes for existing anti mycobacterium drugs.
MCE supplies a unique collection of 134 compounds with clear anti-tuberculosis activity. MCE Anti-tuberculosis Compound Library is a useful tool for anti-tuberculosis related research and anti-tuberculosis drug development
Cy3-NO2-Tre is a nitroreductase-responsive cyanine-based fluorescent probe that specifically labels Mycobacteriumtuberculosis (Mtb). Cy3-NO2-tre generated fluorescence after activation by a specific nitroreductase, Rv3368c, which is conserved in the Mycobacteriaceae. Cy3-NO2-tre effectively imaged mycobacteria within infected host cells, tracked the infection process, and visualized Mycobacterium smegmatis being endocytosed by macrophages (Ex/Em= 540-550/575-625 nm) .
TL8-506 (GMP) is TL8-506 (HY-20457) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 has immunomodulatory effects and can be used in the study of tuberculosis and cancer immunotherapy .
5-Fluoroindole is an orally active fluorinated indole derivative and antibacterial agent. 5-Fluoroindole induces ROS accumulation and triggers Apoptosis. 5-Fluoroindole inhibits the growth of pan-susceptible Mycobacteriumtuberculosis (Mtb) H37Rv strains. 5-Fluoroindole has significant bactericidal activity against Pseudomonas syringae pv. actinidiae (Psa) with an EC50 of 15.34 μg/mL. 5-Fluoroindole introduces fluorine labeling for protein research. 5-Fluoroindole can be used in the study of tuberculosis and kiwifruit bacterial canker .
Trehalose 6,6'-dimycolate (Cord Factor) is trehalose 6,6'-dimycolate, a cell wall glycolipid of Mycobacteriumtuberculosis, which can be used to simulate inflammation and granuloma induced by Mycobacteriumtuberculosis (MTB) form. Trehalose 6,6′-dimycolate also protects Mycobacteriumtuberculosis from macrophage-mediated killing, inhibits efficient antigen presentation, and reduces the development of protective T cell responses .
4-Nitrobenzoic acid is a nitroaromatic compound that can be used in the synthesis of other active compounds. 4-Nitrobenzoic acid is also an inhibitor agent, which can be used for the recognition of the Mycobacteriumtuberculosis complex and differentiation from non-tuberculous mycobacteria .
Eriochrome black T, Indicator is a complexing agent for metal ions (e.g., Ca 2+, Mg 2+) and is used as an indicator in complexometric titrations. Eriochrome black T, Indicator forms colored complexes with metal ions through covalent coordination bonds, and indicates the endpoint of the titration by color change. Eriochrome black T, Indicator can be used as an anionic azo dye in photocatalytic degradation studies to evaluate the performance of photocatalysts. The reaction solution of Eriochrome black T, Indicator combined with Mg 2+ is initially purple. During loop-mediated isothermal amplification (LAMP), the color changes from purple to sky blue due to the consumption of Mg 2+ by the formation of magnesium pyrophosphate, indicating a positive reaction. The optimal concentration of Eriochrome black T, Indicator in LAMP is 60 μM, and the detection limit for Mycobacteriumtuberculosis is 1 pg DNA/reaction .
Mycobacterium bovis bacterial protein is a member of the Mycobacteriumtuberculosis complex. Mycobacterium bovis bacterial protein causes tuberculosis in bovines .
4-Nitrobenzoic acid (Standard) is the analytical standard of 4-Nitrobenzoic acid (HY-Y0607). This product is intended for research and analytical applications. 4-Nitrobenzoic acid is a nitroaromatic compound that can be used in the synthesis of other active compounds. 4-Nitrobenzoic acid is also an inhibitor agent, which can be used for the recognition of the Mycobacteriumtuberculosis complex and differentiation from non-tuberculous mycobacteria .
TL8-506 (GMP) is TL8-506 (HY-20457) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 has immunomodulatory effects and can be used in the study of tuberculosis and cancer immunotherapy .
RVG TFA is a peptide derived from Rabies Virus Glycoprotein that binds to the α-7 subunit of nicotinic acetylcholine receptors (AchR) of neuronal cells. RVG enhances delivery of Mycobacteriumtuberculosis antigens to antigen-presenting cells .
RVG (RVG29) is a peptide derived from Rabies Virus Glycoprotein that binds to the α-7 subunit of nicotinic acetylcholine receptors (AchR) of neuronal cells. RVG enhances delivery of Mycobacteriumtuberculosis antigens to antigen-presenting cells .
ESAT6 Epitope is a known CD4+ T cell epitope in early secretory antigen target gene 6 (ESAT6) that binds to major histocompatibility complex MHC class I with nanometer affinity (IC50=180 nM). ESAT6 Epitope can be used to enhance BCG-induced anti-Mycobacteriumtuberculosis cellular immunity .
Griselimycin is a compound with antituberculosis activity that exhibits good in vitro and in vivo activity against sensitive and resistant Mycobacteriumtuberculosis, and its cyclohexyl derivative has high transformative potential.
Evybactin is a DNA gyrase inhibitor. Evybactin is a selective inhibitor of Mycobacteriumtuberculosis with a MIC value of 0.25 µg/mL. Evybactin is the first antimicrobial compound found to employ this unusual mechanism of selectivity .
Capreomycin is a macrocyclic peptide antibiotic. Capreomycin can be used for anti-multidrug-resistant-tuberculosis research. Capreomycin can inhibit phenylalanine synthesis in in mycobacterial ribosomes translation
L-Cycloserine ((S)-4-Amino-3-isoxazolidone) is an oral inhibitor of the enzyme gamma-aminobutyric acid (GABA) transaminase (GABA-t) and branched-chain transaminases in Mycobacteriumtuberculosis. L-Cycloserine has anticonvulsant properties and inhibits the synthesis of neurotensin in mouse brains .
Zamanic acid is a potent inhibitor of glutathione reductase. Zamanic acid inhibits the growth of Mycobacteriumtuberculosis in culture and has also been shown to have anti-inflammatory activity .
Amycolatopsin C is a glycosylated macrolactone with antibacterial activity. Amycolatopsin C selectively inhibits the growth of Mycobacterium bovis (BCG) and Mycobacteriumtuberculosis (H37Rv) compared to other Gram-positive and Gram-negative bacteria. Amycolatopsin C demonstrates low levels of cytotoxicity toward mammalian cells and can be utilized in antibacterial research .
Tetrahydroxysqualene is a triterpene, possessing antimycobacterial activity against Mycobacteriumtuberculosis with an MIC of 10.0 μg/mL. Tetrahydroxysqualene can be isolated from the methanolic extracts of Rhus taitensis Guill .
(24S)-Cycloartane-3β,24,25-triol, a cycloartane, has antitubercular activity against Mycobacteriumtuberculosis H37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium .
Calpinactam (FKI-4905), a fungal metabolite, is a new anti-mycobacterial agent.Calpinactam is active only against Mycobacteria among various microorganisms, including Gram-positive and Gram-negative bacteria, fungi and yeasts. Calpinactam inhibits the growth of Mycobacterium smegmatis and Mycobacteriumtuberculosis with MIC values of 0.78 and 12.5 μg/ml, respectively .
Carbazomycin D exhibits antituberculosis and antimalarial activities, that inhibits Plasmodium falciparum with an IC50 > 10 μg/mL, inhibits Mycobacteriumtuberculosis with MIC of 25 μg/mL. Carbazomycin D exhibits cytotoxicity in cell MCF-7, KB, NCI-H187 and Vero, with IC50s of 21.3, 33.2, 12.9, and 34.3 μg/mL, respectively .
L-Cycloserine (Standard) is the analytical standard of L-Cycloserine. This product is intended for research and analytical applications. L-Cycloserine ((S)-4-Amino-3-isoxazolidone) is an oral inhibitor of the enzyme gamma-aminobutyric acid (GABA) transaminase (GABA-t) and branched-chain transaminases in Mycobacteriumtuberculosis. L-Cycloserine has anticonvulsant properties and inhibits the synthesis of neurotensin in mouse brains[1][2][3][4].
Phomoxanthone A is a xanthone dimer, which can be isolated from Phomopsis. Phomoxanthone A exhibits antimalarial and antitubercular activities against Plasmodium falciparum (K1, multidrug-resistant strain, IC50 is 0.11 µg/mL) and Mycobacteriumtuberculosis (H37Ra strain, MIC is 0.50 µg/mL). Phomoxanthone A exhibits cytotoxicity in cells KB, BC-1 and Vero, IC50 is 0.99, 0.51 and 1.4 µg/mL, respectively .
DL-Syringaresinol ((±)-Syringaresinol), a lignin, inhibits UVA-induced upregulation of MMP-1 by suppressing MAPK/AP-1 signaling in human HaCaT keratinocytes and dermal fibroblasts (HDFs). DL-Syringaresinol has antiphotoaging properties against UVA-induced skin aging. DL-Syringaresinol exhibits weak antimycobacterial activity against Mycobacteriumtuberculosis H37Rv .
Amycolatopsin A is a 20-membered macrolide, that can be isolated from a strain of the rare actinomycete Amycolatopsis sp. MST‐108494. Amycolatopsin A shows antimycobacterial activity against Mycobacterium bovis (BCG) and M. tuberculosis (H37Rv) with IC50 values of 0.4 µM and 4.4 µM, respectively .
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacteriumtuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
α-Mycolic acid, keto cis is a structural lipid component of mycobacterial cell wall. α-Mycolic acid, keto cis can be isolated from Mycobacteriumtuberculosis Canetti. α-Mycolic acid, keto cis significantly modulates membrane permeability and stability, promising for mycobacteriumtuberculosis infection research .
α-Mycolic acid (C80) is a structural lipid component of mycobacterial cell wall. α-Mycolic acid (C80) can be isolated from Mycobacteriumtuberculosis Canetti. α-Mycolic acid (C80) significantly modulates membrane permeability and stability, promising for mycobacteriumtuberculosis infection research .
Mycolic acid IIa is a structural lipid component of mycobacterial cell wall. Mycolic acid IIa can be isolated from Mycobacterium bovis BCG. Mycolic acid IIa significantly modulates membrane permeability and stability, promising for mycobacteriumtuberculosis infection research .
Pyridomycin (Erizomycin) is a selective and low cytotoxic inhibitor of Mycobacteriumtuberculosis that effectively targets InhA. Pyrdomycin is also an antibiotic that can be obtained from metabolites of Dactylosporangium fulvum. Pyrdomycin can be used in the study of bacterial infections such as tuberculosis .
Propioxatin B is a tricyclic sesquiterpenoid compound isolated from the root of vetiver grass. It has anti-tuberculosis activity and inhibitory effects on a variety of drug-resistant mutants of Mycobacteriumtuberculosis. In computer simulation docking studies, it showed binding affinity with bacterial DNA gyrase and has a certain safety in vivo.
Rifamycin sodium (Rifamycin SV monosodium) is an orally active ansamycin antibiotic. Rifamycin sodium inhibits DNA-dependent RNA synthesis. Rifamycin sodium has antibacterial activity against Mycobacteriumtuberculosis. Rifamycin sodium interferes with hepatic bile acid metabolism. Rifamycin sodium has anti-inflammatory effects. Rifamycin sodium can be used in the study of Mycobacteriumtuberculosis, Bacteroides fragilis infection, and Lipopolysaccharide (HY-D1056B3)-induced inflammation .
Steviolbioside is a sweetener and also an important pharmaceutical intermediate. Steviolbioside can inhibit the proliferation of various tumor cells. Steviolbioside has an MIC of 3.8 µg/mL for Mycobacteriumtuberculosis. Steviolbioside also has antidiabetic activity. Steviolbioside can be used in the research of tuberculosis, diabetes and tumors such as breast cancer .
7-Oxo-ganoderic acid Z, a terpenoid, is a nature product that could be isolated from Resina Commiphora. 7-Oxo-ganoderic acid Z has Anti-Mycobacteriumtuberculosis activity .
Caprazene is an antimycobacterial compound and precursor molecule for semi-synthetic antibacterial antibiotics, used for studies on tuberculosis and Mycobacterium avium complex infections, which can be isolated from the acid-treated caprazamycin (CPZ) A-G mixture .
(Rac)-Sativan is an isoflavanoid with a broad spectrum of antimicrobial activity against bacteria and phytopathogenic fungi. (Rac)-Sativan exhibits antituberculosis activity against Mycobacteriumtuberculosis H37Rv, with MIC values of 50 µg/mL .
Rifamycin (sodium) (Standard) is the analytical standard of Rifamycin (sodium). This product is intended for research and analytical applications. Rifamycin sodium (Rifamycin SV sodium) is an orally active ansamycin antibiotic. Rifamycin sodium inhibits DNA-dependent RNA synthesis. Rifamycin sodium has antibacterial activity against Mycobacteriumtuberculosis. Rifamycin sodium interferes with hepatic bile acid metabolism. Rifamycin sodium has anti-inflammatory effects. Rifamycin sodium can be used in the study of Mycobacteriumtuberculosis, Bacteroides fragilis infection, and Lipopolysaccharide (HY-D1056B3)-induced inflammation .
Ganorbiformin B is a lanostane triterpenoid. Ganorbiformin B shares the same lanostane skeleton with known ganoderic acids. The C-3 epimer of ganoderic acid T exhibits potent antimycobacterial activity against Mycobacteriumtuberculosis H37Ra .
Steviolbioside (Standard) is the analytical standard of Steviolbioside (HY-N2547). This product is intended for research and analytical applications. Steviolbioside is a sweetener and also an important pharmaceutical intermediate. Steviolbioside can inhibit the proliferation of various tumor cells. Steviolbioside has an MIC of 3.8 µg/mL for Mycobacteriumtuberculosis. Steviolbioside also has antidiabetic activity. Steviolbioside can be used in the research of tuberculosis, diabetes and tumors such as breast cancer .
4-Allylcatechol (4-Allylpyrocatechol) is a xylan which has oral activity and can be isolated from the root of Piper taiwanense. 4-Allylcatechol has a strong inhibitory activity against collagen-induced platelet aggregation (IC50 = 5.3 μM). In addition, 4-Allylcatechol has anti-tuberculosis activity against Mycobacteriumtuberculosis H37Rv (MIC = 27.6 μg/mL) .
Cordycepin (3'-Deoxyadenosine) is a nucleoside derivative and inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner . Cordycepin kills Mycobacteriumtuberculosis through hijacking the bacterial adenosine kinase .
Miaosporone A, an angucyclic quinone, exhibits antimalarial activity against Plasmodium falciparum K1 and antibacterial activity against Mycobacteriumtuberculosis with respective IC50 values of 2.5 and 2.4 μM and displays cytotoxic activities against both cancerous (MCF-7 and NCI-H187) and nonmalignant (Vero) cells .
Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
Pyrazinamide (Standard) is the analytical standard of Pyrazinamide. This product is intended for research and analytical applications. Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
Cordycepin (Standard) is the analytical standard of Cordycepin. This product is intended for research and analytical applications. Cordycepin (3'-Deoxyadenosine) is a nucleoside derivative and inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner . Cordycepin kills Mycobacteriumtuberculosis through hijacking the bacterial adenosine kinase .
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines .
Dehydrocostus Lactone ((-)-Dehydrocostus lactone) is a natural sesquiterpene that can be isolated from Saussurea lappa. Dehydrocostus Lactone has multiple activities such as anti-inflammatory, antibacterial, anti-tumor, and immunomodulatory effects. Dehydrocostus Lactone has an MIC of 2 µg/mL against Mycobacteriumtuberculosis. Dehydrocostus Lactone can also inhibit the killing activity of cytotoxic T lymphocytes and induce apoptosis in tumor cells .
Saringosterol is found in Sargassum muticum. Saringosterol is a LXR agonist that lowers cholesterol. saringosterol inhibits the mRNA and protein expression of peroxisome proliferator-activated receptor γ and CCAAT enhancer-binding protein α in 3T3-L1 cells. Saringosterol has anti-Mycobacteriumtuberculosis activity. Saringosterol can be used in anti-obesity and anti-atherosclerosis research .
Celastramycin A isomer is an isomer of Celastramycin A (HY-122292), an antibiotic against Gram-negative bacteria and Mycobacteriumtuberculosis with an MIC of 0.05-3.1 μg/mL. Celastramycin A exerts immunosuppressive effects in Drosophila ex vivo via the immunodeficiency pathway (IC50 of 8 ng/mL), inhibits human innate immune responses via the TNF-α pathway, and inhibits IL-8 production in HUEVC with an IC50 of 60 ng/mL .
(+)-(3R,8S)-Falcarindiol is a polyacetylene found in carrots, has antimycobacterial activity, with an IC50 of 6 μM and MIC of 24 μM against Mycobacteriumtuberculosis H37Ra . Antineoplastic and anti-inflammatory activity . (+)-(3R,8S)-Falcarindiol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacteriumtuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic) .
Dehydrocostus Lactone (Standard) ((-)-Dehydrocostus lactone (Standard)) is the analytical standard of Dehydrocostus Lactone (HY-N0591). This product is intended for research and analytical applications. Dehydrocostus Lactone is a natural sesquiterpene that can be isolated from Saussurea lappa. Dehydrocostus Lactone has multiple activities such as anti-inflammatory, antibacterial, anti-tumor, and immunomodulatory effects. Dehydrocostus Lactone has an MIC of 2 µg/mL against Mycobacteriumtuberculosis. Dehydrocostus Lactone can also inhibit the killing activity of cytotoxic T lymphocytes and induce apoptosis in tumor cells.
(22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid (compound 15) is an antitubercular agent with MIC value of 12.5 μg/mL for Mycobacteriumtuberculosis H37Ra. (22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid shows cytotoxicity with IC50 value of 32 μM for Vero cells .
beta-Mangostin (Standard) is the analytical standard of beta-Mangostin. This product is intended for research and analytical applications. beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacteriumtuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic) .
5-Nitro-1,10-phenanthroline (5-NP), is a o-Phenanthroline (HY-W004544) derivative, as a mediator of glucose oxidase (GOX) with antituberculous activity. 5-Nitro-1,10-phenanthroline can be applied as redox mediators for oxidases and is suitable for the development of reagent-less biosensors and biofuel cells .
L-Ornithine (hydrochloride) (Standard) is the analytical standard of L-Ornithine (hydrochloride). This product is intended for research and analytical applications. L-Ornithine hydrochloride is a non-proteinogenic amino acid, is mainly used in urea cycle removing excess nitrogen in vivo. L-Ornithine hydrochloride shows nephroprotective .
ClpC1 NTD Protein, the ATP-dependent specificity component of the Clp protease, directs the protease to specific substrates and exhibits chaperone functions independently of ClpP. It plays a crucial role in the targeted degradation of substrates, such as the anti-sigma-E factor RseA, in the presence of ClpP2. ClpC1 NTD Protein, Mycobacterium tuberculosis is the recombinant ClpC1 NTD protein, expressed by E. coli , with tag free.
ClpC1 NTD Protein, the ATP-dependent specificity component of the Clp protease, directs the protease to specific substrates and exhibits chaperone functions independently of ClpP. It plays a crucial role in the targeted degradation of substrates, such as the anti-sigma-E factor RseA, in the presence of ClpP2. ClpC1 NTD Protein, Mycobacterium tuberculosis (His) is the recombinant ClpC1 NTD protein, expressed by E. coli , with N-6*His labeled tag.
PBP1A (penicillin-binding protein 1A) is involved in cell wall formation and plays a crucial role in the synthesis of cross-linked peptidoglycan from lipid intermediates. The enzyme has a bifunctional structure. The penicillin-insensitive transglycosylase N-terminal domain is responsible for the formation of linear glycan chains, and the penicillin-sensitive transpeptidase C-terminal domain promotes the cross-linking of peptide subunits. PBP1A Protein, Mycobacterium tuberculosis is the recombinant PBP1A protein, expressed by E. coli , with tag free.
PBP1A (penicillin-binding protein 1A) is involved in cell wall formation and plays a crucial role in the synthesis of cross-linked peptidoglycan from lipid intermediates. The enzyme has a bifunctional structure. The penicillin-insensitive transglycosylase N-terminal domain is responsible for the formation of linear glycan chains, and the penicillin-sensitive transpeptidase C-terminal domain promotes the cross-linking of peptide subunits. PBP1A Protein, Mycobacterium tuberculosis (His) is the recombinant PBP1A protein, expressed by E. coli , with N-6*His labeled tag.
The kshB protein significantly degrades cholesterol by catalyzing the introduction of the 9a-hydroxyl moiety into 1,4-androstadiene-3,17-dione (ADD), resulting in the 9OHADD intermediate. It is spontaneously converted to HSA through the cleavage of the B ring and aromatization of the A ring. kshB Protein, Mycobacterium tuberculosis is the recombinant kshB protein, expressed by E. coli , with tag free.
The kshB protein significantly degrades cholesterol by catalyzing the introduction of the 9a-hydroxyl moiety into 1,4-androstadiene-3,17-dione (ADD), resulting in the 9OHADD intermediate. It is spontaneously converted to HSA through the cleavage of the B ring and aromatization of the A ring. kshB Protein, Mycobacterium tuberculosis (His) is the recombinant kshB protein, expressed by E. coli , with N-6*His labeled tag.
CYP51 Proteinas is a sterol 14α-demethylase that acts with an unknown physiological substrate and accepts electrons from the iron-sulfur ferredoxin Fdx. In vitro, it catalyzes the C14-demethylation of lanosterol, 24,25-dihydrolanosterol, and obtanyol, showing stereoselectivity in producing 8,14-diene. CYP51 Protein, Mycobacterium tuberculosis (sf9, His) is the recombinant CYP51 protein, expressed by Sf9 insect cells , with N-10*His labeled tag.
(Rac)-Bedaquiline-d6 is the deuterium labeled Bedaquiline (HY-14881) . Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacteriumtuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
Lansoprazole sulfide-d4 is a deuterium labeled Lansoprazole Sulfide. Lansoprazole Sulfide is an active metabolite of the proton pump inhibitor Lansoprazole. Lansoprazole Sulfide is an orally active anti-TB (Mycobacteriumtuberculosis) agent with IC50 values of 0.59 μM intracellularly and 0.46 μM in broth .
4-Nitrobenzoic acid-d2 is the deuterium labeled 4-Nitrobenzoic acid (HY-Y0607). 4-Nitrobenzoic acid is a nitroaromatic compound that can be used in the synthesis of other active compounds. 4-Nitrobenzoic acid is also an inhibitor agent, which can be used for the recognition of the Mycobacteriumtuberculosis complex and differentiation from non-tuberculous mycobacteria .
Prothionamide-d5 is deuterium labeled Prothionamide (HY-B0306). Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacteriumtuberculosis and Mycobacterium lepraeInhA. Prothionamide can effectively inhibit the growth of Mycobacteriumtuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
Quabodepistat-d7 (OPC-167832-d7) is deuterium labeled Quabodepistat. Quabodepistat (OPC-167832) is a potent and orally active dprE1 inhibitor with?an IC50 of 0.258 μM. Quabodepistat has antituberculosis activity and can be used for the research of tuberculosis?caused by?Mycobacteriumtuberculosis .
Bedaquiline impurity 2-d6 is deuterium labeled Bedaquiline. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacteriumtuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
4-Nitrobenzoic acid-d4 is the deuterium labeled 4-Nitrobenzoic acid (HY-Y0607). 4-Nitrobenzoic acid is a nitroaromatic compound that can be used in the synthesis of other active compounds. 4-Nitrobenzoic acid is also an inhibitor agent, which can be used for the recognition of the Mycobacteriumtuberculosis complex and differentiation from non-tuberculous mycobacteria .
Pyrazinamide- 13C, 15N is 15N and 13C labeled Pyrazinamide (HY-B0271). Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
Brassicasterol is a metabolite of Ergosterol and has cardiovascular protective effects. Brassicasterol exerts anticancer effects in prostate cancer through dual targeting of AKT and androgen receptor signaling pathways. Brassicasterol inhibits HSV-1 (IC50=1.2 μM) and Mycobacteriumtuberculosis. Brassicasterol also inhibits sterol δ 24-reductase, slowing the progression of atherosclerosis. Brassicasterol is also a cerebrospinal fluid biomarker for Alzheimer's disease .
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