| DC72952 |
Savirin
|
Savirin (S. aureus virulence inhibitor) is a small molecule that targets the agr (accessory gene regulator) quorum sensing system in Staphylococcus aureus (S. aureus). The agr system is a key regulatory pathway that controls the expression of virulence factors in S. aureus, which are critical for its pathogenicity. The system involves a two-component signal transduction pathway consisting of AgrC (a histidine kinase) and AgrA (a response regulator). |
| DC72935 |
JSF-2414
|
JSF-2414 (JSF2414) is a potent, small molecule GyrB/ParE dual binding inhibitor, simultaneously binds to ATP binding regions of DNA gyrase (GyrB) and topoisomerase (ParE) and displays potent in vitro activity against strains of MRSA, VRSA and VISA. |
| DC72144 |
TH-Z145
|
TH-Z145, a lipophilic bisphosphonate, is a FPPS inhibitor (IC50: 210 nM). |
| DC71474 |
VP-4604
|
VP-4604 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4604 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 4-8 µg/mL. VP-4604 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95%. |
| DC71466 |
EDA-DA
|
EDA-DA is an unnatural dipeptide building block (an ethynyl-D-alanine and a D-alanine). It incorporates a biorthogonal alkyne group into peptidoglycan (PG) through MurF in the cytoplasmic pathway, which enables selective labeling via a click-chemistry reaction. EDA-DA allows labeling of PG in Gram-positive (B. subtilis), Gram-negative (E. coli and C. trachomatis), Mycobacterium (M. smegmatis) and moss plastids (P. patens) with azide modified fluorescent dyes such as Alexa Fluor 488. |
| DC70750 |
Rv1625c agonist V-59
|
Rv1625c agonist V-59 (V-59) is a specific small molecule agonist of the Mtb adenylyl cyclase Rv1625c, inhibits Mtb growth in macrophages (EC50=0.3 uM) in an Rv1625c-dependent mechanism.V-59 inhibits Mtb growth in cholesterol media (EC50 0.70 uM), but not in media containing the two-carbon fatty acid acetate, or in standard rich growth media.V-59 stimulates Rv1625c to produce cAMP, which is necessary for V-59 to inhibit Mtb growth.Chemically activating Rv1625c via V-59 preferentially inhibits cholesterol utilization in WT Mtb, rather than equally inhibiting all lipid utilization by the bacterium. |
| DC70591 |
mCLB073
|
mCLB073 is an advanced, orally active small molecule agonist specifically designed to target Mtb adenylyl cyclase Rv1625c. As an optimized derivative of V-59, it demonstrates significantly enhanced potency and efficacy for in vivo applications. In cholesterol-based media, mCLB073 shows a remarkable 17-fold increase in activity against Mtb compared to its predecessor, V-59, while retaining favorable pharmacokinetic characteristics and a strong safety profile. In preclinical studies, oral administration of mCLB073 at 30 mg/kg led to a substantial reduction in Mtb colony-forming units (CFUs) in the lungs of mice, accompanied by a 45% decrease in lung pathology severity. These findings highlight its potential as a promising therapeutic candidate for tuberculosis treatment. |
| DC70459 |
GSK3011724A
|
GSK 3011724A (DG-167, GSK-3011724A) is a potent, specific inhibitor of β-ketoacyl-ACP synthase (KasA, Kd=9 nM), shows anti-tubercular activity (MIC H37Rv=0.8 uM); shows much weaker apparent dissociation constant for both Pks10 and Pks (Kd=1.4 uM); inhibits mycolic acid biosynthesis and shows negligible activity against a panel of unrelated proteins and 18 Gram-positive and Gram-negative bacterial species. |
| DC70368 |
DU011
|
DU011 is a noncanonical anti-infective agent and small-molecule inhibitor of capsule biogenesis, targets MprA (Kd=30 nM), a MarR family transcriptional repressor of multidrug efflux pumps, inhibits capsule expression in E. coli.
DU011 does not alter Escherichia coli antibiotic resistance and has significantly enhanced inhibition of capsule expression, compared with other proposed MprA ligands, such as salicylate and 2,4-dinitrophenol (DNP). |
| DC47231 |
Dup-721
|
DuP-721 is a broad spectrum and orally active antibacterial agent against a variety of clinically susceptible and resistant bacteria, especially M. tuberculosis. |
