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Telacebec (Q203) is a midazopyridine amide compound. Telacebec is active against MycobacteriumtuberculosisH37Rv with an MIC50 of 2.7 nM in culture broth medium.
2-Mercaptopyridine N-oxide sodium has bactericidal effect and is against a standard strain of MycobacteriumtuberculosisH37Rv (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 .
BTZ043 is an inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), with MICs of of 2.3 nM and 9.2 nM for M. tuberculosisH37Rv and Mycobacterium smegmatis, respectively.
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of MycobacteriumtuberculosisH37Rv with a MIC value of 0.1 μg/mL .
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 MycobacteriumtuberculosisH37Rv (MIC = 27.6 μg/mL) .
3-Hydroxypicolinic acid is a heterocyclic carboxylic acid ligand and cytotoxin, with a MIC90 of >25 μg/mL against MycobacteriumtuberculosisH37Rv. 3-Hydroxypicolinic acid inhibits the growth of cancer cells and normal fibroblasts. 3-Hydroxypicolinic acid is applicable to research related to chronic myeloid leukemia, human lung adenocarcinoma, and tuberculosis .
NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent MycobacteriumtuberculosisH37Rv.
Thiocarlide is a potent antibacterial agent. Thiocarlide inhibits MycobacteriumtuberculosisH37Rv, Mycobacterium bovisBCG, Mycobacterium avium, and Mycobacterium aurum A+ with MICs of 2.5, 0.5, 2.0 and 2.0 μg/mL, respectively .
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 MycobacteriumtuberculosisH37Rv and its auxotrophic, attenuated derivative mc2 6230 (ΔRD1, ΔpanCD) with an MIC of 8 μM .
Thiolactomycin is an orally active bacterial type II fatty acid synthase (FAS-II) inhibitor with antibacterial and antimalarial activities. Thiolactomycin specifically targets KasA/KasB in mycobacteria and FabB/FabF in bacteria, thereby inhibiting the biosynthesis of fatty acids and mycolic acids. Thiolactomycin can be used in studies related to tuberculosis, systemic bacterial infections, and experimental pyelonephritis .
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 MtbH37Rv (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 .
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 .
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 MycobacteriumtuberculosisH37Rv .
Telacebec ditosylate is a midazopyridine amide compound. Telacebec ditosylate is active against MycobacteriumtuberculosisH37Rv with an MIC50 of 2.7 nM in culture broth medium.
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 .
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 .
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 .
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 .
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 MycobacteriumtuberculosisH37Rv strain (MIC=6.25 μg/mL) and significantly inhibits VEGFR-2 (IC50=15.27 nM) .
Antituberculosis agent-16 is an orally active antituberculosis agent. Antituberculosis agent-16 exhibits stable antituberculosis activity with a MIC of 0.48 μg/mL against MycobacteriumtuberculosisH37Rv sensitive strain and 0.49 μg/mL against multidrug-resistant strain 14862. Antituberculosis agent-16 shows high Caco-2 permeability. Antituberculosis agent-16 can be used for the research of infection .
Antitubercular agent-58 is an antitubercular agent with an IC50 of 51 nM against MycobacteriumtuberculosisH37Rv. Antitubercular agent-58 can be used for the research of tuberculosis .
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 .
Maniladiol is a triterpenoid that can be isolated from the flowers of Chrysanthemum morifolium. Maniladiol exhibits antitubercular activity against Mycobacteriumtuberculosis strain H37Rv with a MIC of 4 mg/mL. Maniladiol can be used for Mycobacteriumtuberculosis infection research .
The minimum inhibitory concentration (MIC) of a new 2- (quinoline-4-methoxy) acetamide antituberculotic agent against the reference strain of MycobacteriumtuberculosisH37Rv was as low as 0.3 μ M. It also inhibited the growth of Mycobacteriumtuberculosis in the macrophage model of tuberculosis infection.
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 .
(Rac)-Sativan is an isoflavanoid with a broad spectrum of antimicrobial activity against bacteria and phytopathogenic fungi. (Rac)-Sativan exhibits antituberculosis activity against MycobacteriumtuberculosisH37Rv, 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 .
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. tuberculosisH37Rv strain with a MIC value of 0.4 μM .
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. tuberculosisH37Rv and Mycobacterium smegmatis, respectively.
MmpL3-IN-5 (Compound 3G) is a MmpL3 inhibitor. MmpL3-IN-5 has an antitubercular activity with a pMIC of 7.0 μM for MycobacteriumtuberculosisH37Rv strain. MmpL3-IN-5 can be used for tuberculosis research .
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 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 .
Anti-infective agent 8 (compound 9d) is an antibacterial agent with an MIC of 0.5 μg/mL against Staphylococcus aureus and MycobacteriumtuberculosisH37Rv. Anti-infective agent 8 has anti-biofilm activity and significantly reduces Staphylococcus aureus biofilm formation .
HT1171 is a potent and selective inhibitor of mycobacteriumtuberculosis proteasome. HT1171 shows strong anti-tuberculosis activity against MycobacteriumtuberculosisH37Rv 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 .
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 MycobacteriumtuberculosisH37Rv with a MIC value of 0.1 μg/mL[1].
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 MtbH37Rv and low cytotoxicity in human fibroblast cells MRC-5. MtTMPK-IN-1 can be used for researching 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.
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 MtbH37Rv (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 MtbH37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)
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 MtbH37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 86 μg/mL) .
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 MycobacteriumtuberculosisH37Rv strain (ATCC-27294) in vitro and depletes intracellular ATP levels at an IC50 value of 30μM .
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 .
2-Chloroisonicotinohydrazide (2-Chloro-isonicotinic acid hydrazide) (Compound 13a) is an Antibacterial agent. 2-Chloroisonicotinohydrazide exhibits antibacterial activity against Mycobacteriumtuberculosis strain H37Rv, with a MIC50 of 392.0 μM. 2-Chloroisonicotinohydrazide can be used in the research of tuberculosis .
(24S)-Cycloartane-3β,24,25-triol, a cycloartane, has antitubercular activity against MycobacteriumtuberculosisH37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium .
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 .
Pks13-IN-2 (Compound 43) is an orally active inhibitor of Pks13. Pks13-IN-2 exhibits inhibitory activity against MycobacteriumtuberculosisH37Rv, 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-17 (compound 21) is a potent and selective antituberculosis agent. Antituberculosis agent-17 displays excellent anti-Tuberculosis (TB) activity against H37Rv, MDR and XDR strains of TB (MIC = 0.2-0.78 μM). Antituberculosis agent-17 exhibits selectivity for Mycobacteriumtuberculosis over selected non-TB forming mycobacteria and bacteria. Antituberculosis agent-17 can be used for TB research .
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 MtbH37Rv (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-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 MycobacteriumtuberculosisH37Rv. 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 MycobacteriumtuberculosisH37Rv. Antitubercular agent-28 shows effective intracellular antimycobacterial activity and low cytotoxicity .
CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacteriumtuberculosis (H37RvMIC90～6.25 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 .
Antimicrobial agent-47 is an anti-mycobacterial agent. Antimicrobial agent-47 exhibits inhibitory activity against MycobacteriumtuberculosisH37Rv, with a MIC50 of 0.78 μg/mL. Antimicrobial agent-47 can be used in the research of tuberculosis .
Antimycobacterial agent-16 is a pyrazinamide derivative and antimycobacterial agent with a selectivity index >25 against HepG2 cells.Antimycobacterial agent-16 does not undergo hydrolysis by mycobacterial pyrazinamidase.Antimycobacterial agent-16 exerts activity against MycobacteriumtuberculosisH37Rv, multidrug-resistant Mycobacteriumtuberculosis strains, and Mycobacterium kansasii.Antimycobacterial agent-16 shows no inhibitory activity against mycobacterial enoyl-ACP reductase (InhA).Antimycobacterial agent-16 has low cytotoxicity against HepG2 cells.Antimycobacterial agent-16 can be used for the research of tuberculosis .
T504 is an oxazolidinone antibiotic. T504 exhibits significant growth inhibitory effects on MycobacteriumtuberculosisH37Rv, Mycobacterium bovis BCG, and Mycobacterium abscessus, and the MIC value for the reference strain MycobacteriumtuberculosisH37Rv is 0.5-1.0 μg/mL. T504 effectively inhibits the growth of Mycobacteriumtuberculosis within macrophages and does not show obvious cytotoxicity. T504 can be used in the research of mycobacterial infections .
I2906 is an orally active isocitrate lyase (ICL) inhibitor with a Mycobacterium tuberculosisIC50 of 134.3 μg/mL. I2906 inhibits the growth of Mycobacterium tuberculosis. I2906 can be used for the research of tuberculosis .
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 .
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 MycobacteriumtuberculosisH37Rv, and a selectivity index greater than 15 .
Antitubercular agent-54 is an antitubercular agent with potent intramacrophage activity (EC50 = 0.68 μM). Antitubercular agent-54 shows a MIC of 0.31 μM against Mycobacteriumtuberculosis (Mtb) H37Rv in cholesterol-containing medium. Antitubercular agent-54 can be used for the research of tuberculosis .
Antimycobacterial agent-15 (Compound 55) is a highly selective anti-mycobacterial agent that has an MIC99 of 8 μM against MycobacteriumtuberculosisH37Rv. Antimycobacterial agent-15 exhibits significant efficacy against multidrug-resistant and extensively drug-resistant isolates. This agent can be used in the research of tuberculosis .
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 .
Antitubercular agent-55 (Compound 2e) is an anti-tuberculous agent. Antitubercular agent-55 exhibits significant inhibitory activity against the standard strain of MycobacteriumtuberculosisH37Rv and also has moderate inhibitory activity against multidrug-resistant TB (MDR-TB). Antitubercular agent-55 has a strong affinity for the key enzyme InhA involved in the biosynthesis of mycotic acids. Antitubercular agent-55 can be used for research on tuberculosis infection caused by Mycobacteriumtuberculosis.
Antitubercular agent-59 is an orally active antitubercular agent with an IC50 of 51 nM against MycobacteriumtuberculosisH37Rv. Antitubercular agent-59 inhibits growth of Bedaquiline (HY-14881)-resistant Rv0678G12C mutant strains. Antitubercular agent-59 exerts bactericidal activity in chronic tuberculosis mouse models with 1-Aminobenzotriazole (HY-103389) coadministration .
EGFR/InhA-IN-1 (Compound 15) is an inhibitor of the anti-cancer target EGFR tyrosine kinase (1M17) (Ki = 0.05 μM) and the anti-tuberculosis target InhA enzyme (1OUZ) (Ki = 0.02 μM). EGFR/InhA-IN-1 exhibits anti-proliferative activity against A549 cells, with an IC50 of 10.38 μM. EGFR/InhA-IN-1 has inhibitory activity against MycobacteriumtuberculosisH37Rv, with a MIC of 6.25 μM. EGFR/InhA-IN-1 can be used for research on non-small cell lung cancer and Mycobacteriumtuberculosis infection .
Antibacterial agent 228 (Compound 8) inhibits the mycobacterial ribosome (IC50 for Mycobacterium smegmatis is 2.31 μM) and exhibits antibacterial activity against M. tuberculosisH37Rv (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) .
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 .
GSK 124576A (compound 8) is a Mycobacterium tuberculosis cytochrome bc1 complex inhibitor and member of the 2-(quinolin-4-yloxy)acetamide class. GSK 124576A can be used for the research of tuberculosis .
PknB-IN-3 is a Mycobacterium tuberculosisProtein kinase B (PknB) inhibitor with an IC50 of 0.06 μM. PknB-IN-3 inhibits growth of Mycobacterium tuberculosis and can be used for the research of tuberculosis .
F1414-1444 is a DBPI skeleton derivative and a potent inhibitor of IspQ (Rv0338c)-targeting Mycobacterium tuberculosis. F1414-1444 binds to the membrane-bound iron-sulfur oxidoreductase IspQ, induces oxidative stress and thiol stress in bacterial cells, upregulates the expression of stress-related genes such as the SigK regulon, thereby inhibiting bacterial proliferation and exerting bactericidal activity. F1414-1444 only inhibits the Mycobacterium tuberculosis complex and Mycobacterium marinum. F1414-1444 can be used in studies related to Mycobacterium tuberculosis .
ETX1975-3 is an orally active inhibitor and bactericide targeting the bdcytochrome oxidase of Mycobacterium tuberculosis. ETX1975-3 disrupts electron transfer between the b-heme centers of the target enzyme, and in combination with Q203 (HY-101040), exerts bactericidal activity against both replicating and non-replicating Mycobacterium tuberculosis, and reduces bacterial loads in acute mouse models. ETX1975-3 retains activity against clinical isolates of multidrug-resistant/extensively drug-resistant Mycobacterium tuberculosis and non-tuberculous mycobacteria, while possessing favorable preclinical ADMET properties. ETX1975-3 can be used in studies related to tuberculosis and non-tuberculous mycobacterial infections .
CB6513745 is a MelF flavin-dependent oxidoreductase inhibitor with a Ki of 18 μM against Mycobacterium marinumMelF. CB6513745 inhibits the activity of MelF flavin-dependent oxidoreductase via hydrophobic interactions with the binding pocket of the protein. CB6513745 is applicable to research related to tuberculosis .
MptpB-IN-3 is a selective inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with an IC50 of 0.19 μM. MptpB-IN-3 blocks MptpB-mediated inhibition of the macrophage MAPK pathway and restores the phosphorylation levels of Erk1/2 and p38. MptpB-IN-3 exhibits direct anti-tuberculosis activity against Mycobacterium tuberculosis and reduces the Mycobacterium tuberculosis load in mouse macrophages. MptpB-IN-3 can be used for tuberculosis research .
MmpL3-IN-6 is a mycobacterial membrane protein large 3 (MmpL3) transporter inhibitor and is an antitubercular agent. MmpL3-IN-6 exerts bactericidal activity against replicating Mycobacterium tuberculosis.MmpL3-IN-6 retains activity against drug-resistant Mycobacterium tuberculosis.MmpL3-IN-6 can be used for the research of tuberculosis .
InhA-IN-11 is a Mycobacterium tuberculosis InhA inhibitor with an IC50 of 0.36 μM. InhA-IN-11 exhibits activity against Mycobacterium tuberculosis, disrupts pre-formed Mycobacterium tuberculosis biofilms, and reduces bacterial viability within biofilms. InhA-IN-11 is applicable for the research of tuberculosis .
GyrB-IN-1 is a DNA gyrase (GyrB) inhibitor. GyrB-IN-1 shows an IC50 of 19.1 μM against Mycobacterium smegmatis GyrB ATPase activity and 21.9 μM against Mycobacterium tuberculosis GyrB DNA supercoiling activity. GyrB-IN-1 exerts antimycobacterial activity and has cytotoxicity. GyrB-IN-1 can be used for the research of tuberculosis .
Pyridomycin-4-F, Pyridomycin (HY-111402) derivative, is an antimycobacterial agent targeting fatty acid synthesis enzyme InhA (enoyl ACP reductase). Pyridomycin-4-F binds to the pyridomycin binding pocket of InhA, forms hydrogen bond interactions with Lys-165. Pyridomycin-4-F can be used for the research of tuberculosis .
DprE1-IN-15 is a covalent Mycobacterium tuberculosis essential cell wall enzyme DprE1 inhibitor with an IC50 of 0.073 μM. DprE1-IN-15 forms an irreversible covalent adduct with its target enzyme. DprE1-IN-15 shows inhibitory effects against multiple Mycobacterium tuberculosis .
UCI-14 is a gltA1/lprQ modulator with in vitro anti-tuberculosis activity against drug-sensitive and multidrug-resistant mycobacteria. UCI-14 upregulates the expression of genes encoding citrate synthase I, downregulates the expression of genes encoding conserved mycobacterial lipoprotein, and alters the carbon metabolism of mycobacteria. UCI-14 reactivates the expression of wild-type p53 target genes in p53-mutated cells. UCI-14 can be used in the research of tuberculosis and cancer .
RMR-Tre is a fluorescent probe targeting the mycobacterial acyltransferase Ag85. Under the catalysis of Ag85, RMR-Tre undergoes 6-position mycoloylation and anchors to the mycobacterial membrane, while achieving fluorescence activation by inhibiting the intramolecular twisted charge transfer state transition. RMR-Tre can distinguish live mycobacteria from dead ones through metabolism-driven labeling, enabling rapid, wash-free, low-background detection of viable bacteria. RMR-Tre reports the drug resistance of Mycobacterium tuberculosis via the trehalose catalytic shift activity readout associated with TreS. In addition, RMR-Tre can be combined with flow cytometry or high-content imaging techniques to visualize and quantitatively analyze the metabolic heterogeneity of Mycobacterium tuberculosis related to persistence and drug resistance. RMR-Tre is widely used in tuberculosis-related research .
IDD-AN-A1 is a potent Mycobacterium tuberculosis (Mtb) isocitrate lyase (ICL) inhibitor with an IC50 of 7 μg/mL. IDD-AN-A1 shows additive and synergistic activity with anti-tuberculosis agents. , respectively.IDD-AN-A1 exhibits potent anti-tuberculosis activity. IDD-AN-A1 can be used for the research of tuberculosis .
RMR-Tre is a fluorescent probe targeting the mycobacterial acyltransferase Ag85. Under the catalysis of Ag85, RMR-Tre undergoes 6-position mycoloylation and anchors to the mycobacterial membrane, while achieving fluorescence activation by inhibiting the intramolecular twisted charge transfer state transition. RMR-Tre can distinguish live mycobacteria from dead ones through metabolism-driven labeling, enabling rapid, wash-free, low-background detection of viable bacteria. RMR-Tre reports the drug resistance of Mycobacterium tuberculosis via the trehalose catalytic shift activity readout associated with TreS. In addition, RMR-Tre can be combined with flow cytometry or high-content imaging techniques to visualize and quantitatively analyze the metabolic heterogeneity of Mycobacterium tuberculosis related to persistence and drug resistance. RMR-Tre is widely used in tuberculosis-related research .
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 .
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 MycobacteriumtuberculosisH37Rv (MIC = 27.6 μg/mL) .
3-Hydroxypicolinic acid is a heterocyclic carboxylic acid ligand and cytotoxin, with a MIC90 of >25 μg/mL against MycobacteriumtuberculosisH37Rv. 3-Hydroxypicolinic acid inhibits the growth of cancer cells and normal fibroblasts. 3-Hydroxypicolinic acid is applicable to research related to chronic myeloid leukemia, human lung adenocarcinoma, and tuberculosis .
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 MycobacteriumtuberculosisH37Rv .
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 .
Maniladiol is a triterpenoid that can be isolated from the flowers of Chrysanthemum morifolium. Maniladiol exhibits antitubercular activity against Mycobacteriumtuberculosis strain H37Rv with a MIC of 4 mg/mL. Maniladiol can be used for Mycobacteriumtuberculosis infection research .
(Rac)-Sativan is an isoflavanoid with a broad spectrum of antimicrobial activity against bacteria and phytopathogenic fungi. (Rac)-Sativan exhibits antituberculosis activity against MycobacteriumtuberculosisH37Rv, with MIC values of 50 µg/mL .
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 .
(24S)-Cycloartane-3β,24,25-triol, a cycloartane, has antitubercular activity against MycobacteriumtuberculosisH37Rv (MIC: 32 μg/mL). (24S)-Cycloartane-3β,24,25-triol can be isolated from the flowers of Chrysanthemum morifolium .
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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