222036-17-1
222036-17-1 structure
- Name: GW-8510
- Chemical Name: GW8510
- CAS Number: 222036-17-1
- Molecular Formula: C21H15N5O3S2
- Molecular Weight: 449.51
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2018-06-04 19:00:54
- Modify Date: 2024-01-09 14:55:49
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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].
| Name | GW8510 |
|---|
| 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 | |
| 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. |
| Molecular Formula | C21H15N5O3S2 |
|---|---|
| Molecular Weight | 449.51 |
| Appearance | solid |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |