DTHIB 是一种直接和选择性的heat shock factor 1 (HSF1)抑制剂，DTHIB 与 HSF1 DNA 结合域结合的Kd为 160 nM。DTHIB 抑制HSF1癌症基因标记 (HSF1 CaSig)，并选择性刺激核HSF1的降解。DTHIB 具有有效的抗癌活性，可用于前列腺癌的研究。
| 生物活性 | DTHIB is a direct and selectiveheat shock factor 1 (HSF1)inhibitor with aKdof 160 nM forDTHIB binding to theHSF1DNA binding domain (DBD). DTHIB inhibitsHSF1cancergene signature (HSF1 CaSig) and selectively stimulates degradation of nuclearHSF1. DTHIB has potently anticancer activities and can be used for prostatecancerresearch[1]. |
| IC50& Target | Kd: 160 nM (DTHIB binding to the HSF1 DNA binding domain)[1] |
体外研究
(In Vitro) | DTHIB (5 μM; 48 hours) treatment of C4-2 cells induces cell cycle arrest, with accumulation in the G1 phase. DTHIB stimulates C4-2 PCa cell entry into senescence[1].
DTHIB (0.5-5 μM; 48 hours; C4-2 prostate cancer) treatment reduces steady-state protein abundance of the molecular chaperones P23, HSP27, HSP70, and HSP90-all bona fide HSF1 targets in C4-2 cells[1].
DTHIB dose-dependently reduces the clonal expansion of both C4-2 and PC-3 PCa cells with EC50values of 1.2 μM and 3.0 μM, respectively[1].
In mouse embryonic fibroblasts (MEFs), DTHIB (0.5-10 μM) attenuates the robust acute heat shock induction of the HSP70 and HSP25 molecular chaperones in a dose-dependent manner. DTHIB attenuates the heat shock response by reducing the steady-state transcript abundance of multiple molecular chaperones[1].
Cell Cycle Analysis[1] | Cell Line: | C4-2 cells | | Concentration: | 5 μM | | Incubation Time: | 48 hours | | Result: | Induced cell cycle arrest. |
Western Blot Analysis[1] | Cell Line: | C4-2 prostate cancer (PCa) cells | | Concentration: | 0.5 μM, 1 μM, 2.5 μM, 5 μM | | Incubation Time: | 48 hours | | Result: | Dose-dependently inhibited expression of molecular chaperones in C4-2 PCa cells. |
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体内研究
(In Vivo) | DTHIB (5 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment potently attenuates tumor progression in a C4-2 xenograft mouse model[1].
| Animal Model: | Nude mice (6 weeks of age) injected with C4-2 cells[1] | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection; daily; for 3 weeks | | Result: | Showed no visible tumor growth over a 3-week period and a 40% reduction in median tumor volume. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(322.91 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2291 mL | 16.1457 mL | 32.2914 mL | | 5 mM | 0.6458 mL | 3.2291 mL | 6.4583 mL | | 10 mM | 0.3229 mL | 1.6146 mL | 3.2291 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (6.72 mM); Clear solution; Need ultrasonic
此方案可获得 2.08 mg/mL (6.72 mM) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
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