DTHIB

製品コードS9806 バッチS980601

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₃H₉ClFN₃O₃

分子量

309.68

CAS No.

897326-30-6

Solubility (25°C)*

体外

DMSO

86 mg/mL (277.7 mM)

Ethanol

17 mg/mL (54.89 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (16.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (16.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
in vitro	Direct Targeted HSF1 InhiBitor (DTHIB) physically engages HSF1 and selectively stimulates degradation of nuclear HSF1. This compound robustly inhibits the HSF1 cancer gene signature and prostate cancer cell proliferation.^[1]
in vivo	DTHIB potently attenuates tumor progression in four therapy-resistant prostate cancer animal models, including an NEPC model, where this compound causes profound tumor regression.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	C4-2, PC-3, BPH-1 cells
	濃度	0.5 μM, 1.0 μM, 2.5 μM, 5 μM
	反応時間	36-hour, 48-hour, 96-hour
	実験の流れ	C4-2 Scr and shHSF1 cells exposed to 36-hour treatment with 2.5 μM DTHIB are evaluated for HSF1 target gene expression by qRT-PCR.
動物実験	動物モデル	6-week-old nude (nu/nu) mice; 6 week-old C57BL/6 mice
	投薬量	1 mg/kg, 5 mg/kg
	投与方法	IP

参考

https://pubmed.ncbi.nlm.nih.gov/33328331/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Heat shock factor 1 promotes proliferation and chemoresistance in diffuse large B-cell lymphoma by enhancing the cell cycle and DNA repair [ Cell Death Dis, 2025, 16(1):533]	PubMed: 40675964
Wu-Mei-Wan enhances brown adipose tissue function and white adipose browning in obese mice via upregulation of HSF1 [ Chin Med, 2025, 20(1):1]	PubMed: 39754217
Human coronaviruses activate and hijack the host transcription factor HSF1 to enhance viral replication [ Cell Mol Life Sci, 2024, 81(1):386]	PubMed: 39243335
Increased mitochondria are responsible for the acquisition of gemcitabine resistance in pancreatic cancer cell lines [ Cancer Sci, 2023, 114(11):4388-4400.]	PubMed: 37700464

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。