GW-8510

Names

[ CAS No. ]:
222036-17-1

[ Name ]:
GW-8510

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

Research Areas >> Neurological Disease

[Target]

CDK2

CDK5

RRM2

[In Vitro]

GW8510 (0.5-4 μM; 72 h) 以剂量依赖性方式抑制 HCT116 细胞的活力[2]。 GW8510 (1-4 μM; 24 h) 抑制 RRM2 表达而不改变 RRM1 表达[2]。 GW8510 在体外生化分析中测试时抑制 CDK2 和其他 CDK，当用于培养的神经元时它仅抑制 CDK5[1]。 GW8510 抑制由高钾培养基转为低钾培养基引起的小脑颗粒神经元死亡[1]。 GW8510 (5 μM; 48 h) 与 Tamoxifen (5 μM; 48 h) 联合使用，可通过诱导自噬性细胞死亡显着抑制 Tamoxifen 耐药乳腺癌细胞 (BBC) 的存活[3]。 Cell Viability Assay[2] Cell Line: HCT116 cells Concentration: 0.5, 1, 2, 4 μM Incubation Time: 72 hours Result: Inhibited HCT116 cells growth. Western Blot Analysis[2] Cell Line: HCT116 cells Concentration: 1, 2, 4 μM Incubation Time: 24 hours Result: Inhibited RRM2 expression. The reduction of RRM2 protein level can be reversed by MG132.

[In Vivo]

GW8510 与 Tamoxifen 联用可通过诱导自噬增强对他莫昔芬耐药的 BBC 异种移植物的杀瘤作用[3]。

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₁₅N₅O₃S₂

[ Molecular Weight ]:
449.51

[ Appearance of Characters ]:
solid

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Cytoplasmic nucleophosmin has elevated T199 phosphorylation upon which G2/M phase progression is dependent.

Sci. Rep. 5 , 11777, (2015)

The cytoplasmic mutant of nucleophosmin (NPMc) is found approximately in one-third of acute myeloid leukemia (AML) cases and is highly associated with normal karyotype. Whereas previous studies have f...

Glycogen synthase kinase 3 is a potential drug target for African trypanosomiasis therapy.

Antimicrob. Agents Chemother. 52(10) , 3710-7, (2008)

Development of a safe, effective, and inexpensive therapy for African trypanosomiasis is an urgent priority. In this study, we evaluated the validity of Trypanosoma brucei glycogen synthase kinase 3 (...

Related Compounds

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