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TBI-166, a riminophenazine analogue, is an orally active anti-tuberculosis agent with fewer adverse reactions than the lead riminophenazine compound, Clofazimine (HY-B1046) .
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 µg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization .
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 .
Wangzaozin A is an ent-kaurene diterpenoid. Wangzaozin A has cytotoxic against HepG2 cells and Tb cells with IC50 of 1.41 μM and 0.32 μM, respectively .
Antibacterial agent 121 (Compound 10) is an antibacterial agent. Antibacterial agent 121 shows anti-mycobacterial and anti-inflammatory activities and can be used in Tuberculosis (TB) research .
Antituberculosis agent-5 (compound 52) is a nitrofuranylamide derivative, inhibits M. tuberculosisUDP-Gal mutase. Antituberculosis agent-5 inhibits Glf activity with an IC50 value of 99 μM/mL and resists tuberculosis (TB) with a MIC value of 1.6 μg/mL .
Antitubercular agent-43 (compound A11) is an orally active and potent antitubercular agent. Antitubercular agent-43 shows highly metabolic stability against human and mouse cytochrome P450 enzymes. Antitubercular agent-43 exhibits bactericidal efficacy in acute TB infection mouse model .
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 .
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 .
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 .
4-Piperidinecarboxamide is a mycobacterial aspartyl-tRNA synthetase (AspS) inhibitor. 4-Piperidinecarboxamide is a promising anti-tuberculosis (TB) agent .
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 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. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM.
LeuRS-IN-1 is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tbLeuRS) inhibitor. LeuRS-IN-1 has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively . LeuRS-IN-1 inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM) .
LeuRS-IN-1 hydrochloride is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tbLeuRS) inhibitor. LeuRS-IN-1 hydrochloride has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively . LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM) .
Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 µM and 1.4 µM for Trypanosoma brucei (TB) and human CYP51, respectively .
Pks13-TE inhibitor 4 (compound 44) is an oxadiazole series Pks13 inhibitor that effectively inhibits tuberculosis (TB) and resolves its drug resistance .
Polyketide synthase 13-IN-3 (compound 41) is a polyketide synthase 13 inhibitor，with a MIC of 0.0625-0.125 μg/mL against the M. tuberculosis strain H37Rv .
Pks13-TE inhibitor 2 (compound 32) is a 13-Thioesterase (Pks13-TE) inhibitor (IC50=1.30 μM). Pks13-TE inhibitor 2 shows good anti-tuberculosis activity against both agent-sensitive and drug-resistant Mtb strains (MIC=0.0039-0.0078 μg/mL). Pks13-TE inhibitor 2 can be used in studies of multidrug-resistant TB and extensively drug-resistant TB .
Pks13-TE inhibitor 3 (compound 23) is a 13-Thioesterase (Pks13-TE) inhibitor (IC50=1.55 μM). Pks13-TE inhibitor 3 shows good anti-tuberculosis activity against both agent-sensitive and drug-resistant Mtb strains (MIC=0.0625-0.25 μg/mL). Pks13-TE inhibitor 3 can be used in studies of multidrug-resistant TB and extensively drug-resistant TB .
Patent Blue V has been widely used in sentinel lymph node mapping. Patent Blue V is also a food coloring agent and an alternative dye for trypan blue (TB) in descemet membrane endothelial keratoplasty (DMEK) .
Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast, as an adjunct, is used for the research of tuberculosis (TB) .
Z-Leu-Arg-AMC is a 4-methylcoumarinyl-7-amide (Amc) leucine derivative with carboxybenzoyl (Z). Z-Leu-Arg-AMC is the active site of cysteine proteinase trypanopain-Tb from Trypanosoma brucei brucei .
OJT008 is an inhibitor of MtMetAP1c. OJT008 inhibits NiCl2- and CoCl2 activated MtMetAP1c with IC50s of 11 and 40 μM, respectively. OJT008 can used to study tuberculosis .
PNU-101603 is a sulfoxide metabolite of Sutezolid (HY-10392). PNU-101603 alone or combined with SQ109 (HY-14989) shows excellent activity against Mycobacterium tuberculosis (MTB), as well as against agent-susceptible and multidrug-resistant TB .
CRK12-IN-1 is a potent CRK12 inhibitor. CRK12-IN-1 is extremely potent against T.b. brucei and rapidly cytocidal, as well as equally potent against T. congolense and T. vivax (EC50 of 1.3 and 18 nM, respectively) .
PSDalpha is an ERα degrader conjugating photosensitizer (PS), triphenylamine benzothiadiazole (TB) and 17β-estradiol via an acetylene bond. PSDalpha shows excellent anti-proliferation performance on MCF-7 cells. The maximum absorption wavelength of PSDalpha in the visible region is located at 465 nm .
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 Mycobacterium tuberculosis .
DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of 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 (Mycobacterium tuberculosis) agent with IC50 values of 0.59 µM intracellularly and 0.46 µM in broth[1].
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 Mycobacterium tuberculosis (Mtb). HadAB-IN-1 can be used for the research of tuberculosis (TB) .
DG70 (GSK1733953A), a biphenyl amide, is a respiration inhibitor in Mycobacterium tuberculosis, inhibits MenG activity with an IC50 value of 2.6 ± 0.6 μM. DG70 inhibits the catalytic methylation of Mycobacterium tuberculosis demethylmenaquinone methyltransferase enzymes. DG70 can be used for Tuberculosis (TB) research .
Mycobacterial Zmp1-IN-1 is a mycobacterial zinc metalloprotease-1 (Zmp1) inhibitor. Mycobacterial Zmp1-IN-1 has anti-mycobacterial activity for Mtb H37Ra in dose-dependent inhibition. Mycobacterial Zmp1-IN-1 can be used for the research of tuberculosis (TB) .
Bonducellin is a a homoisoflavonoid, which can be isolated from Caesalpinia digyna roots. Bonducellin is a potent inhibitor of efflux pump (EP), while EP induces resistance in mycobacteria and serves as a target of anti-TB (tuberculosis) agents. Bonducellin reduces MIC of EtBr by 8-fold against M. smegmatis (MIC=62.5 mg/L) .
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 Mycobacterium tuberculosis (M.tb) H37Rv. Antimycobacterial agent-2 shows cytotoxic activities with an IC50 of48.1 µM for CHO cells .
M8-B is a potent transient receptor potential melastatin-8 (TRPM8) antagonist. M8-B blocks cold-induced and TRPM8-agonist-induced activation TRPM8 channels. M8-B decreases deep body temperature (Tb) .
Harpagide is a class of iridoid glycoside isolated from Scrophularia ningpoensis and has antiparasitic activity, which exhibits good in vitro trypanocidal activities against African trypanosomes(T.b. rhodesiense) with an IC50 of 21 μg/mL. Harpagide exerts significant antileishmanial activity against L. donovani with an IC50 value of 2.0 μg/mL. Harpagide also possess significant anti-inflammatory activities .
DprE1-IN-5 (Compound 10) is a DprE1 inhibitor. DprE1-IN-5 has anti-TB activity against Mtb H37Rv strain (MIC: 4 μM). DprE1-IN-5 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-5 has high microsomal stability .
DprE1-IN-7 (Compound 64) is a DprE1 inhibitor. DprE1-IN-7 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-7 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-7 has high microsomal stability and medium clearance .
DprE1-IN-6 (Compound 56) is a DprE1 inhibitor. DprE1-IN-6 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-6 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-6 has high microsomal stability and medium clearance .
Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents .
Glutamate-5-kinase-IN-2 (compound 54) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.2 µM. Glutamate-5-kinase-IN-2 shows G5K inhibition by promotes conformational changes at the L-glutamate binding site. Glutamate-5-kinase-IN-2 has the potential for the research of anti-TB agents .
Streptomycin (Agrept) is an effective antibiotic against M. tuberculosis, is used for the research of tuberculosis (TB). Streptomycin also is a bacteriocidal agent that can be used for the research of a number of bacterial infections. Streptomycin can bind strongly to nucleic acids, interferes and blocks protein synthesis while permitting continued RNA and DNA synthesis. Streptomycin, as a common antibiotic used in culture media, also is a blocker of stretch-activated and mechanosensitive ion channels in neurons and cardiac myocytes .
ML338 is a selective small molecule inhibitor probe of non-replicating Mycobacterium tuberculosis 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 .
Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase . Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml . Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB) .
Tuberculosis (TB), usually caused by bacteria (Mycobacterium tuberculosis), 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 94 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
TB500 is a synthetic version of an active region of thymosin β4. TB500 is claimed to promote endothelial cell differentiation, angiogenesis in dermal tissues, keratinocyte migration, collagen deposition and decrease inflammation .
Serylleucine is a dipeptide. Serylleucine's core 1 o-glycosylated peptide (SLC1G) can be detected in urine as a metabolite and is a biomarker in TB studies .
Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 µM and 1.4 µM for Trypanosoma brucei (TB) and human CYP51, respectively .
Harpagide is a class of iridoid glycoside isolated from Scrophularia ningpoensis and has antiparasitic activity, which exhibits good in vitro trypanocidal activities against African trypanosomes(T.b. rhodesiense) with an IC50 of 21 μg/mL. Harpagide exerts significant antileishmanial activity against L. donovani with an IC50 value of 2.0 μg/mL. Harpagide also possess significant anti-inflammatory activities .
Wangzaozin A is an ent-kaurene diterpenoid. Wangzaozin A has cytotoxic against HepG2 cells and Tb cells with IC50 of 1.41 μM and 0.32 μM, respectively .
Bonducellin is a a homoisoflavonoid, which can be isolated from Caesalpinia digyna roots. Bonducellin is a potent inhibitor of efflux pump (EP), while EP induces resistance in mycobacteria and serves as a target of anti-TB (tuberculosis) agents. Bonducellin reduces MIC of EtBr by 8-fold against M. smegmatis (MIC=62.5 mg/L) .
TMSB4X proteins play a critical role in cytoskeletal organization, influencing actin dynamics by binding and sequestering actin monomers. As a potent inhibitor of actin polymerization, it affects the cytoskeleton. Thymosin beta 4 Protein, Human is the recombinant human-derived Thymosin beta 4 protein, expressed by E. coli , with tag free. The total length of Thymosin beta 4 Protein, Human is 43 a.a., with molecular weight of ~4.9 kDa.
CD40L (CD154; TRAP) is a ligand to CD40/TNFRSF5, acts function by generating a costimulatory signal that up-regulates IL-4 synthesis. CD40L is specifically expressed on activated CD4+ T-lymphocytes and involves in activation of NF-κB/MAPK pathway. CD40L also involves in B cell differentiation, maturation, and apoptosis. CD40L in mouse, cleaved into 2 chains of membrane form (1-260 a.a.) and soluble form (112-260 a.a.) which serves as a ligand for integrins (ITGA5:ITGB1 and ITGAV:ITGB3). CD40L/CD154/TRAP Protein, Mouse (HEK293, His) has a total length of 149 amino acids (M112-L260), is expressed in HEK392 cells with N-terminal 6*His-tag.
TMSB4X proteins play a critical role in cytoskeletal organization, influencing actin dynamics by binding and sequestering actin monomers. As a potent inhibitor of actin polymerization, it affects the cytoskeleton. TMSB4X Protein, Human (His) is the recombinant human-derived TMSB4X protein, expressed by E. coli , with N-6*His labeled tag. The total length of TMSB4X Protein, Human (His) is 43 a.a., with molecular weight of ~13 kDa.
PIGR proteins play a critical role in mediating the selective transcytosis of polymerized IgA and IgM across mucosal epithelial cells, which is critical for mucosal immunity. PIGR binds these immunoglobulins at the basolateral surface, forming a complex that is transported intracellularly and secreted apically. PIGR Protein, Human (HEK293, His) is the recombinant human-derived PIGR protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PIGR Protein, Human (HEK293, His) is 620 a.a., with molecular weight of ~88.0 kDa.
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 (Mycobacterium tuberculosis) agent with IC50 values of 0.59 µM intracellularly and 0.46 µM in broth[1].
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