222036-17-1

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222036-17-1 Structure

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[Name] GW8510
[CAS] 222036-17-1
[Synonyms] GW-8510 (GW8510 4-{[(7-oxo-6,7-dihydro-8h-[1,3]thiazolo[5,4-e]indol-8-ylidene)methyl]amino}-n-(2-pyridyl)benzenesulfonamide Benzenesulfonamide, 4-[[(6,7-dihydro-7-oxo-8H-pyrrolo[2,3-g]benzothiazol-8-ylidene)methyl]amino]-N-2-pyridinyl-
[Molecular Formula] C21H15N5O3S2
[MDL Number] MFCD03452930
[MOL File] 222036-17-1.mol
[Molecular Weight] 449.51

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[WGK Germany ] 3

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[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] Combination with GW8510 and Tamoxifen enhances tumoricidal effect on Tamoxifen-resistant BBC xenograft through autophagy induction^[3].
[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

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