97534-21-9 Usage
Description
MERBARONE is a cell-permeable anticancer drug that selectively inhibits the catalytic activity of topoisomerase II (topo II) without causing DNA damage or stabilizing DNA-topo II cleavable complexes. It has an IC50 value of 20 μM for purified mammalian topo II and ~200 μM for topo I. MERBARONE also induces apoptosis in human leukemic CEM cells through a caspase-3-like protease-dependent mechanism.
Uses
Used in Cancer Research:
MERBARONE is used as a research tool for studying its effect on the occurrence of DNA lesions and its potential as an anticancer agent. Its ability to inhibit topo II without damaging DNA makes it a valuable compound for investigating the mechanisms of action and potential therapeutic applications in cancer treatment.
Used in Pharmaceutical Development:
MERBARONE is used as a lead compound in the development of new anticancer drugs. Its selective inhibition of topo II and induction of apoptosis in cancer cells make it a promising candidate for further research and development into more effective cancer therapies.
Used in Drug Delivery Systems:
Similar to gallotannin, MERBARONE could potentially be incorporated into drug delivery systems to improve its delivery, bioavailability, and therapeutic outcomes. This would involve the use of various organic and metallic nanoparticles as carriers for MERBARONE, aiming to enhance its efficacy against cancer cells.
Biochem/physiol Actions
Cell permeable: yes
Check Digit Verification of cas no
The CAS Registry Mumber 97534-21-9 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 9,7,5,3 and 4 respectively; the second part has 2 digits, 2 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 97534-21:
(7*9)+(6*7)+(5*5)+(4*3)+(3*4)+(2*2)+(1*1)=159
159 % 10 = 9
So 97534-21-9 is a valid CAS Registry Number.
InChI:InChI=1/C11H9N3O3S/c15-8(12-6-4-2-1-3-5-6)7-9(16)13-11(18)14-10(7)17/h1-5,7H,(H,12,15)(H2,13,14,16,17,18)
97534-21-9Relevant articles and documents
Pharmacophore Hybridization to Discover Novel Topoisomerase II Poisons with Promising Antiproliferative Activity
Ortega, Jose Antonio,Riccardi, Laura,Minniti, Elirosa,Borgogno, Marco,Arencibia, Jose M.,Greco, Maria L.,Minarini, Anna,Sissi, Claudia,De Vivo, Marco
, p. 1375 - 1379 (2018)
We used a pharmacophore hybridization strategy to combine key structural elements of merbarone and etoposide and generated new type II topoisomerase (topoII) poisons. This first set of hybrid topoII poisons shows promising antiproliferative activity on hu
