2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. KG-548

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.

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KG-548 Chemical Structure

KG-548 Chemical Structure

CAS No. : 175205-09-1

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Based on 1 publication(s) in Google Scholar

KG-548 Related Antibodies

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HIF-1α HIF

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Description

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[1][2].

IC50 & Target

HIF-β[1]; HIF-1α[2]
In Vitro

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.

KG-548 Related Antibodies

Western Blot Analysis[1]

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.
Molecular Weight

282.15

Formula

C9H4F6N4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C1=CC(C(F)(F)F)=CC(C2=NN=NN2)=C1)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5442 mL 17.7211 mL 35.4421 mL
5 mM 0.7088 mL 3.5442 mL 7.0884 mL
View the 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.

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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 99.92%

COA (250 KB) HNMR (130 KB) RP-HPLC (204 KB) LCMS (272 KB)

Handling Instructions (2659 KB)
References

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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KG-548 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KG-548175205-09-1KG548KG 548HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHFaDu cellsc-MYCenergy metabolismthe Warburg effectHEK293T cellInhibitorinhibitorinhibit

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