| Bioactivity | 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]. |
| Invitro | 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: |
| 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]。 |
| Name | GW8510 |
| CAS | 222036-17-1 |
| Formula | C21H15N5O3S2 |
| Molar Mass | 449.51 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |