KG-548
Based on 1 Customer Validation
KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.90%
- CAS 番号: 175205-09-1
- 分子式: C9H4F6N4
- 分子量:282.15
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Epigenetics Compound Library
HY-L005
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Reprogramming Compound Library
HY-L039
-
Oxygen Sensing Compound Library
HY-L045
-
Glycolysis Compound Library
HY-L058
-
Glutamine Metabolism Compound Library
HY-L064
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Angiogenesis-Related Compound Library
HY-L088
-
Transcription Factor-Targeted Library
HY-L090
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Cancer Stem Cells Compound Library
HY-L135
-
Metabolic Enzyme Compound Library
HY-L146
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Fibrosis Compound Library
HY-L185
-
Lactic Acid Metabolic Compound Library
HY-L204
-
High-Throughput Bioactive Compound Library
HY-L205
生物活性
HIF is a heterodimer of two bHLH-PAS (basic Helix Loop Helix-Per-ARNT-Sim) subunits, including a HIF-α paralog (HIF-1α, -2α, -3α) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β)[1].
KG-548 (0-250 μM; 16 h for over night) exhibits the great reduction of ARNT/CCC complex formation for both coactivators, and also disrupts ARNT2 PAS-B/TACC3 interactions[1].
KG-548 (0-2 mM; 16 h for over night) dose-dependently breaks up the (320 μM) ARNT PAS-B/TACC3 complex in vitro and in cell lysate with an IC50 value of 25 μM[1].
KG-548 significantly inhibits lactate production of glycolysis in FaDu hypopharyngeal carcinoma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293T cell lysates
-
Concentration:0, 5, 50, 100, 250, 500 μM and 1 mM, 2 mM
-
Incubation Time:16 hours
-
Result:Weakened the ARNT/TACC3 interaction from 5 μM to 500 μM dose-dependently, and decreased the protein intense of ARNT associated with immunoprecipitated TACC3 protein by 82% (500 μM), 59% (1 mM), 43% (2 mM), respectively.
化学情報
-
CAS 番号 175205-09-1
-
性状 Solid
-
分子量 282.15
-
分子式 C9H4F6N4
-
Color White to off-white
-
SMILES
FC(C1=CC(C(F)(F)F)=CC(C2=NN=NN2)=C1)(F)F
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (354.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (276 KB)
-
SDS (604 KB)
- English - EN (604 KB)
- Français - FR (604 KB)
- Deutsch - DE (604 KB)
- Norwegian - NO (604 KB)
- Español - ES (604 KB)
- Swedish - SV (604 KB)
- Italian - IT (604 KB)
- Korean - KR (604 KB)
- Portuguese - PT (604 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Guo Y, et al. Regulating the ARNT/TACC3 axis: multiple approaches to manipulating protein/protein interactions with small molecules. ACS Chem Biol. 2013 Mar 15;8(3):626-35. [Content Brief]
[2]. Kleszcz R, et al. The inhibition of c-MYC transcription factor modulates the expression of glycolytic and glutaminolytic enzymes in FaDu hypopharyngeal carcinoma cells. Adv Clin Exp Med. 2018 Jun;27(6):735-742. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5442 mL | 17.7211 mL | 35.4421 mL | 88.6054 mL |
| 5 mM | 0.7088 mL | 3.5442 mL | 7.0884 mL | 17.7211 mL | |
| 10 mM | 0.3544 mL | 1.7721 mL | 3.5442 mL | 8.8605 mL | |
| 15 mM | 0.2363 mL | 1.1814 mL | 2.3628 mL | 5.9070 mL | |
| 20 mM | 0.1772 mL | 0.8861 mL | 1.7721 mL | 4.4303 mL | |
| 25 mM | 0.1418 mL | 0.7088 mL | 1.4177 mL | 3.5442 mL | |
| 30 mM | 0.1181 mL | 0.5907 mL | 1.1814 mL | 2.9535 mL | |
| 40 mM | 0.0886 mL | 0.4430 mL | 0.8861 mL | 2.2151 mL | |
| 50 mM | 0.0709 mL | 0.3544 mL | 0.7088 mL | 1.7721 mL | |
| 60 mM | 0.0591 mL | 0.2954 mL | 0.5907 mL | 1.4768 mL | |
| 80 mM | 0.0443 mL | 0.2215 mL | 0.4430 mL | 1.1076 mL | |
| 100 mM | 0.0354 mL | 0.1772 mL | 0.3544 mL | 0.8861 mL |
Powered by Bioz