Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
13 Results for "
GyrB
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "GyrB" in MCE Product Catalog:
14
Novobiocin (Albamycin; Cathomycin) is an orally active antibiotic and Hsp-90 antagonist that also inhibits the Polθ helicase/ATPase domain with IC50 values of 24 μM and 15-17 μM, respectively. Novobiocin binds to Hsp90, GyrB, and POLθ, inhibiting their ATPase activity and ssDNA binding. Novobiocin inhibits molecular chaperone function and DNA repair, and induces apoptosis and genomic instability. Novobiocin exhibits bactericidal and antiparasitic activities. Novobiocin inhibits tumor growth in vivo. Novobiocin is used for research on equine piroplasmosis, ovarian cancer, breast cancer, anthrax, and melioidosis .
14
14 Cited Publications
Synonyms: Albamycin sodium; Cathomycin sodium
Cat. No.: HY-12888
CAS No.: 907543-25-3
Target:
Research Areas:
AZD5099 is an orally effective pyrrole amide inhibitor and antibacterial agent. AZD5099 shows over 10000-fold higher selectivity for bacterial type II topoisomerases than for human topoisomerase IIα, with a IC50 value of 0.032 μmol/L against Staphylococcus aureus GyrB, a IC50 of 0.760 μmol/L against Escherichia coli GyrB, a IC50 of 73 nM against Escherichia coli ParE, a Kd of 83.8 nmol/L for Staphylococcus aureus GyrB, and a IC50 of >50 μM against human topoisomerase IIα. AZD5099 inhibits rat Mrp2 ATPase activity, competitively binds to the ATP-binding site of bacterial type II topoisomerases, blocks enzyme activity, reduces bacterial DNA and RNA synthesis, disrupts DNA replication and transcription processes, and induces mitochondrial toxicity. AZD5099 exhibits activity against Gram-positive bacteria, fastidious Gram-negative bacteria and drug-resistant strains, reduces bacterial loads in mouse infection models, and has a low spontaneous resistance frequency. AZD5099 can be used in studies related to infections caused by Gram-positive bacteria and fastidious Gram-negative bacteria, methicillin-resistant Staphylococcus aureus infections, Streptococcus pneumoniae pulmonary infections, as well as Staphylococcus aureus and Escherichia coli infections .
Cat. No.: HY-116783
CAS No.: 1870007-38-7
Target:
Research Areas:
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 .
Cat. No.: HY-141442
CAS No.: 29826-16-2
Category:
Target:
Cat. No.: HY-163104
CAS No.: 2879255-03-3
Antibacterial agent 169 (Compound 28) is a pyrrolamide-type GyrB/ParE inhibitor with antibacterial activity. Antibacterial agent 169 has an inhibitory effect on Gyrase and Topo IV of Staphylococcus aureus, with IC50 values of 49 nmol/L and 1.513 μmol/L respectively .
Cat. No.: HY-149925
CAS No.: 3034242-80-0
Target:
Research Areas:
Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor .
Cat. No.: HY-P701907
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: DNA gyrase subunit B; EC:5.6.2.2; Type IIA topoisomerase subunit GyrB; GyrB; acrB; cou; himB; hisU; nalC; parA; pcbA; b3699; JW5625
Species:
E.coli
Source:
E. coli
Cat. No.: HY-P701908
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: DNA gyrase subunit B; EC:5.6.2.2; Type IIA topoisomerase subunit GyrB; GyrB; acrB; cou; himB; hisU; nalC; parA; pcbA; b3699; JW5625
Species:
E.coli
Source:
E. coli
Cat. No.: HY-182936
Target:
Research Areas:
Antibacterial agent 338 (Compound 65) is an antibacterial agent and GyrB inhibitor, with an IC50 of 12.60 nM against GyrB from E. coli. Antibacterial agent 338 binds to the ATP-binding domain of E. coli GyrB, thereby inhibiting the ATPase activity of GyrB. Antibacterial agent 338 exhibits broad-spectrum antibacterial activity against multidrug-resistant Gram-negative bacteria. Antibacterial agent 338 reduces bacterial load in a neutropenic mouse thigh infection model. Antibacterial agent 338 can be used for the research of Acinetobacter baumannii infection .
Cat. No.: HY-189124
Target:
Research Areas:
Antibacterial agent 372 is a potent antibacterial agent. Antibacterial agent 372 is a DNA gyrase inhibitor that binds to the ATP-binding pocket of the GyrB subunit, downregulates gyrB gene expression, and impedes DNA replication and supercoiling. Antibacterial agent 372 exhibits broad-spectrum antibacterial activity against Gram-positive and Gram-negative bacteria. Antibacterial agent 372 can be used for research on microbial infections .
Cat. No.: HY-189125
Target:
Anticancer agent 360 is a broad-spectrum antibacterial agent. Anticancer agent 360 binds to the ATP pocket of the GyrB subunit of DNA gyrase via an Arg84 salt bridge, interfering with gyrase-dependent DNA supercoiling. Anticancer agent 360 disrupts bacterial biofilms and inhibits the metabolic activity of respiratory chain dehydrogenases. Anticancer agent 360 exhibits activity against Gram-positive bacteria, Gram-negative bacteria, and fungal strains. Anticancer agent 360 exerts selective cytotoxicity against liver cancer cells. Anticancer agent 360 can be used in studies related to bacterial infections and liver cancer .
Cat. No.: HY-116880
CAS No.: 2092352-48-0
Target:
Research Areas:
DS-2969b is an orally active GyrB inhibitor with antibacterial activity. DS-2969b is is active against Clostridium difficile infection (MIC90: 0.06 μg/mL), which is 2-, 16-, and 32-fold lower than those of Fidaxomicin (HY-17580), Metronidazole (HY-B0318), and Vancomycin (HY-B0671), respectively. DS-2969b inhibits the supercoiling activity of C. difficile DNA gyrase. DS-2969b also exhibits activity against other Gram-positive anaerobes, including strict and facultative anaerobes. DS-2969b is safe and well tolerated in preclinical toxicology studies .
- 1
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
