| Identification | Back Directory | [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 |
| Chemical Properties | Back Directory | [density ]
1.635±0.06 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: soluble | [form ]
solid | [pka]
8.39±0.10(Predicted) | [color ]
Light yellow to yellow | [InChI]
InChI=1S/C21H15N5O3S2/c27-21-15(19-16(25-21)8-9-17-20(19)30-12-24-17)11-23-13-4-6-14(7-5-13)31(28,29)26-18-3-1-2-10-22-18/h1-12,23H,(H,22,26)(H,25,27) | [InChIKey]
GCYXEGSPUDSZJY-UHFFFAOYSA-N | [SMILES]
C1(S(NC2=NC=CC=C2)(=O)=O)=CC=C(NC=C2C3=C4SC=NC4=CC=C3NC2=O)C=C1 |
| Hazard Information | Back Directory | [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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