GW8510

Uses

GW8510 is a potent cyclin-dependent kinase-2 (CDK2) inhibitor. GW8510 is also a ribonucleotide reductase M2 (RRM2) inhibitor. GW8510 exhibits neuroprotective and anticancer activities[1][2][3].

Definition

ChEBI: 4-[(7-oxo-6H-pyrrolo[2,3-g][1,3]benzothiazol-8-ylidene)methylamino]-N-(2-pyridinyl)benzenesulfonamide is a sulfonamide and a member of benzenes.

Biochem/physiol Actions

Initially characterized as an inhibitor of cyclin-dependent kinase 2 (CDK2), subsequent research has shown GW8510 to be non-selective.

in vivo

IC 50

CDK2; CDK5; RRM2

References

[1] ARCAMONE F, et, al. STRUCTURE AND SYNTHESIS OF DISTAMYCIN A. Nature. 1964 Sep 5;203:1064-5. DOI:10.1038/2031064a0
[2] Hiraku Y, et, al. Distamycin A, a minor groove binder, changes enediyne-induced DNA cleavage sites and enhances apoptosis. Nucleic Acids Res Suppl. 2002;(2):95-6. DOI:10.1093/nass/2.1.95
[3] Majumder P, et, al. Effect of DNA groove binder distamycin A upon chromatin structure. PLoS One. 2011;6(10):e26486. DOI:10.1371/journal.pone.0026486