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.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 175205-09-1
- Formula: C9H4F6N4
- Molecular Weight:282.15
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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.
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Cell Line:HEK293T cell lysates
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Concentration:0, 5, 50, 100, 250, 500 μM and 1 mM, 2 mM
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Incubation Time:16 hours
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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.
Chemical Information
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CAS No. 175205-09-1
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Appearance Solid
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Molecular Weight 282.15
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Formula C9H4F6N4
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Color White to off-white
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SMILES
FC(C1=CC(C(F)(F)F)=CC(C2=NN=NN2)=C1)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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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)
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Handling Instructions (2659 KB)
References
[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 |
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