KHK-IN-1
Based on 1 publication(s) in Google Scholar
KHK-IN-1 (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 has potential for the study of diabetes and obesity.
For research use only. We do not sell to patients.
- Purity: 99.00%
- CAS No.: 1303469-70-6
- Formula: C21H26N8S
- Molecular Weight:422.55
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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
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) KHK-IN-1
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Biological Activity
IC50=12 nM (KHK)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
<500 nM
Compound: 1
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Inhibition of KHKC in human HepG2 cells assessed as level of fructose-1-phosphate
Inhibition of KHKC in human HepG2 cells assessed as level of fructose-1-phosphate
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[PMID: 22795331] |
| HepG2 | IC50 |
400 nM
Compound: 8
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Inhibition of ketokinase isoform C in human HepG2 cells assessed as levels of fructose-1-phosphate preincubated for 30 mins followed by substrate addition measured after 3 hrs by LC-MS analysis
Inhibition of ketokinase isoform C in human HepG2 cells assessed as levels of fructose-1-phosphate preincubated for 30 mins followed by substrate addition measured after 3 hrs by LC-MS analysis
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[PMID: 24900346] |
KHK-IN-1 stable in human and rat liver microsome preparations (88 and 72% remaining at 10 min) and do not significantly inhibit cytochrome P450s from human liver microsomes (1A2, 2C19, 2D6, 2C9, and 3A4)[1].
KHK-IN-1 (0-10 µM; incubate 30 min, then add to 15 mM fructose and incubate for another 3 h) inhibits production of F1P in HepG2 cell lysates with an IC50 value of 400 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:0-10 µM
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Incubation Time:Incubate 30 min, then add to 15 mM fructose and incubate for another 3 h
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Result:Exhibited inhibition of F1P production in HepG2 cell lysates (IC50=400 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (~250 g)[1].
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Dosage:10 mg/kg
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Administration:Oral gavage; single
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Result:Exhibited reasonable oral bioavailability in rats (F=34%; oral t1/2=4 h), but had a high volume of distribution (Vdss= 32 L/kg) and a high rate of clearance (CL=160 mL/min/kg).
Chemical Information
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CAS No. 1303469-70-6
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Appearance Solid
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Molecular Weight 422.55
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Formula C21H26N8S
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Color Light yellow to yellow
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SMILES
CSC(C=CC=C1)=C1NC2=NC(N3CCNCC3)=NC4=C2N=CN=C4NCC5CC5
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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Exp Cell Res
Ketohexokinase-A deficiency attenuates the proliferation via reducing β-catenin in gastric cancer cells. [Abstract]2024 Apr 16;438(1):114038. PMID: 38614422
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KHK-IN-1 Related Classifications
HY-12841 Related Classifications
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