2. Metabolic Enzyme/Protease
  3. Ketohexokinase
  4. KHK-IN-1

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (KHK-IN-1 hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

KHK-IN-1 Chemical Structure

KHK-IN-1 Chemical Structure

CAS No. : 1303469-70-6

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KHK-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target

IC50=12 nM (KHK)[1].
Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
400 nM
Compound: 8
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
[PMID: 24900346]
In Vitro

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.

KHK-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2 cells
Concentration: 0-10 µM
Incubation Time: Incubate 30 min, then add to 15 mM fructose and incubate for another 3 h
Result: Exhibited inhibition of F1P production in HepG2 cell lysates (IC50=400 nM).
In Vivo

KHK-IN-1 (10 mg/kg; p.o.; single) shows oral bioavailability of 34% in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (~250 g)[1].
Dosage: 10 mg/kg
Administration: Oral gavage; single
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).
Molecular Weight

422.55

Formula

C21H26N8S
CAS No.
SMILES

CSC(C=CC=C1)=C1NC2=NC(N3CCNCC3)=NC4=C2N=CN=C4NCC5CC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KHK-IN-1 Related Classifications

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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:

KHK-IN-11303469-70-6KetohexokinaseKHKNIDDMHepG2 cellF1PdiabetesobesityInhibitorinhibitorinhibit

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