tbi

TBI-223 is an orally effective antibiotic and antibacterial agent active against Mycobacterium tuberculosis. It demonstrates efficacy against methicillin-resistant Staphylococcus aureus infections in mouse interference models and is applicable for tuberculosis research.

MTOB (α-keto-γ-Methylthiobutyric acid) is a substrate for c-terminal binding protein (CtBP) that interferes with the carcinogenic activity of CtBP in cell culture and mice. It also actively regulates TCF-4 signaling, leading to cancer stem cell (CSC) growth and self-renewal.

Candesartan (CV 11974) is an angiotensin II receptor blocker widely used in the treatment of hypertension and heart failure.

TBI-166, an orally active riminophenazine analogue, serves as an anti-tuberculosis agent and exhibits fewer adverse reactions compared to its lead compound, Clofazimine [1] [2] [3].

tBID is a selective homeodomain-interacting protein kinase 2 (HIPK2) inhibitor (IC50 of 0.33 µM)

TBIA (trans-bis-isatoic anhydride) is a bifunctional SHAPE (selective 2'-hydroxyl acylation analyzed by primer extension) chemical cross-linking reagent.

Etbicyphat (Trimethylopropane phosphate), a potent competitive antagonist of GABA(A) receptors, binds to GABA(A)-benzodiazepine receptors and induces epileptiform activities in hippocampal CA1 neurons.

Maralixibat Chloride (LUM001 chloride), an apical, sodium-dependent, bile acid transport inhibitor, prevents enterohepatic bile acid recirculation.

Mtb-IN-2 is a small molecule compound of Mycobacterium tuberculosis (Mtb) with antimicrobial activity and low toxicity that interferes with methionine metabolism processes and can be used to study tuberculosis.

MDRTB-IN-1 (5aα) is an antibiotic effective against Mycobacterium tuberculosis H37Rv, with a MIC90 of 10.5 μM.

PROTAC BET-binding moiety 1 is a crucial intermediate used in synthesizing high-affinity BET inhibitors.

PROTAC BET-binding moiety 2 is an inhibitor of the BET bromodomain.

Mtb-IN-9 (Compound M1) is a selective Mtb inhibitor that suppresses the activity of MtbFadD32 and MtbFadD28. In a chronic infection model using BALB/c mice, Mtb-IN-9 reduced the survival rate of Mtb in infected macrophages and decreased Mtb burden and tuberculous granulomas. It holds promise for tuberculosis research.

Mtb-IN-10 (Compound P15) is an Rv1625c/Cya activator that influences the growth of Mycobacterium tuberculosis (Mtb) by modulating cAMP metabolism. It demonstrates an anti-tuberculosis activity with an EC50 of 1.96 µM in Mtb-infected macrophage models and achieves an oral bioavailability of 58.0% when administered orally to mice at 20 mg/kg. Mtb-IN-10 potentially regulates intracellular signaling and disrupts cholesterol metabolism within Mtb, thereby inhibiting bacterial proliferation. It holds promise for tuberculosis (TB) research, particularly targeting multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains of Mtb.

Mtb-IN-11 (Compound 1e) is an inhibitor of Mycobacterium tuberculosis salicylate synthase (MbtI) with an IC50 of 11.2 μM. It exhibits strong in vitro antitubercular activity, with an MIC99 of 32 μM against Mycobacterium bovis BCG. Mtb-IN-11 is applicable for tuberculosis research.

Mtb-IN-6 (Compound C10) is a Mycobacterium tuberculosis (Mtb) respiratory inhibitor. It enhances the bactericidal activity of isoniazid (INH) and inhibits wild-type Mtb with an IC50 of 25 µM.

Mtb-IN-7 (compound R7) is a MAO-A/MAO-B inhibitor with an IC50 greater than 40 μM. It exhibits antibacterial activity against Mycobacterium tuberculosis H37Rv, with a MIC of 2.01 μM.

Mtb-IN-12 (Compound 5m) is a dual-target inhibitor that acts on the Mycobacterium tuberculosis enzymes CYP125 with a dissociation constant (KD) of 40 nM and an inhibition constant (KI) of 0.1 μM, and CYP142 with a KD of 160 nM and a KI of 0.05 μM. It effectively inhibits both drug-sensitive and multidrug-resistant strains of the tuberculosis bacterium, with low toxicity to macrophages, making it useful for studying anti-tuberculosis treatments.

BRD32048 is the ETV1 transcription factor oncoprotein inhibitor.

BI-6C9 is an inhibitor of tBid (Kd = 20 µM).BI-6c9 prevented MOMP and mitochondrial fission, and protected the cells from cell death.

Montelukast bis-sulfide is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.

UT-B-IN-1 (UTBINH-14) is a reversible, competitive, and selective inhibitor of the urea transporter-B (UT-B) with IC50 values of 10 nM and 25 nM for human and mouse UT-B, respectively. It exhibits low toxicity and superior selectivity against UT-B compared to UT-A isoforms, enhances urine production, and decreases urine concentration in mice, making it suitable for research on diuretic mechanisms.

PRL 2915 is a potent antagonist of the human somatostatin subtype 2 receptor (hsst 2), exhibiting a binding affinity (K_i) of 12 nM [1].

Mtb-IN-3 (compound 10c), a selective and potent Mycobacterium tuberculosis (Mtb) inhibitor, exhibits strong antimycobacterial activity in vitro without inducing cytotoxic effects and inhibits colony formation in the spleen in murine tuberculosis models [1].