| 产品描述： | HSF1 抑制剂;HSF1 InhiBitor;;InformationDTHIB DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities.TargetsHSF1 (Cell-free assay) 160 nM(Kd)In vitroDirect Targeted HSF1 InhiBitor (DTHIB) physically engages HSF1 and selectively stimulates degradation of nuclear HSF1. DTHIB robustly inhibits the HSF1 cancer gene signature and prostate cancer cell proliferation.In vivoDTHIB potently attenuates tumor progression in four therapy-resistant prostate cancer animal models, including an NEPC model, where it causes profound tumor regression.Cell Research(from reference)Cell lines：C4-2, PC-3, BPH-1 cells Concentrations：0.5 μM, 1.0 μM, 2.5 μM, 5 μM Incubation Time：36-hour, 48-hour, 96-hour |
| 靶点： |
Kd: 160 nM (DTHIB binding to the HSF1 DNA binding domain) |
| 体内研究： |
DTHIB (5 mg/kg；腹腔注射；每日一次，持续 3 周) 显著减弱了 C4-2 异种移植小鼠模型中的肿瘤进展。 |
| 参考文献： |
1. Bushu Dong, et al. Targeting therapy-resistant prostate cancer via a direct inhibitor of the human heat shock transcription factor 1. Sci Transl Med. 2020 Dec 16;12(574):eabb5647. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.229 ml |
16.146 ml |
32.291 ml |
| 5 mM |
0.646 ml |
3.229 ml |
6.458 ml |
| 10 mM |
0.323 ml |
1.615 ml |
3.229 ml |
| 50 mM |
0.065 ml |
0.323 ml |
0.646 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京