For research use only. Not for therapeutic Use.
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].
GW8510 (0.5-4 μM; 72 h) inhibits viability of HCT116 cells in a dose-dependent manner[2].
GW8510 (1-4 μM; 24 h) inhibits RRM2 expression without alteration of RRM1 expression[2].
GW8510 inhibits CDK2 and other CDKs when tested in in vitro biochemical assays, when used on cultured neurons it only inhibits CDK5[1].
GW8510 inhibits the death of cerebellar granule neurons caused by switching them from high potassium medium to low potassium medium[1].
Combination with GW8510 (5 μM; 48 h) and Tamoxifen (5 μM; 48 h) significantly inhibits survival of the Tamoxifen-resistant breast cancer cells (BBCs) through induction of autophagic cell death[3].
Combination with GW8510 and Tamoxifen enhances tumoricidal effect on Tamoxifen-resistant BBC xenograft through autophagy induction[3].
| Catalog Number | I012587 |
| CAS Number | 222036-17-1 |
| Synonyms | 4-[(7-hydroxy-6H-pyrrolo[2,3-g][1,3]benzothiazol-8-yl)methylideneamino]-N-pyridin-2-ylbenzenesulfonamide |
| Molecular Formula | C21H15N5O3S2 |
| Purity | ≥95% |
| 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/h1-12,25,27H,(H,22,26) |
| InChIKey | CDNIYBIKHDLGMT-UHFFFAOYSA-N |
| SMILES | C1=CC=NC(=C1)NS(=O)(=O)C2=CC=C(C=C2)N=CC3=C(NC4=C3C5=C(C=C4)N=CS5)O |
| Reference | [1]. ARCAMONE F, et, al. STRUCTURE AND SYNTHESIS OF DISTAMYCIN A. Nature. 1964 Sep 5;203:1064-5. [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. [3]. Majumder P, et, al. Effect of DNA groove binder distamycin A upon chromatin structure. PLoS One. 2011;6(10):e26486. |
