PF-06835919
Based on 1 Customer Validation
PF-06835919 (Ketohexokinase inhibitor 1) is a ketohexokinase (KHK) inhibitor, with IC50 values of 0.028 μM and 0.17 μM against human KHK-C and KHK-A, respectively, and an IC50 value of 0.21 μM against rat KHK. PF-06835919 blocks fructose (HY-N0395) phosphorylation and fructose metabolism. PF-06835919 can be used for research on metabolic dysfunction-associated steatotic liver disease, type 2 diabetes, hereditary fructose intolerance, and related conditions.
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 : 99.53%
- CAS 番号: 2102501-84-6
- 分子式: C16H19F3N4O2
- 分子量:356.34
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
IC50: 8.4 nM (KHK-C), 66 nM (KHK-A)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | IC50 |
>150 μM
Compound: 2; PF-06835919
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Toxicity in human Primary hepatocyte incubated for 48 hrs by Celltiter-Glo assay
Toxicity in human Primary hepatocyte incubated for 48 hrs by Celltiter-Glo assay
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[PMID: 37766386] |
| HepG2 | IC50 |
>150 μM
Compound: 2; PF-06835919
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Cytotoxicity against human HepG2 cells measured after 48 hrs by microscopy based analysis
Cytotoxicity against human HepG2 cells measured after 48 hrs by microscopy based analysis
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[PMID: 37766386] |
| HepG2 | IC50 |
>150 μM
Compound: 2; PF-06835919
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Mitotoxicity in human HepG2 cells incubated for 2 hrs by Celltiter-Glo assay
Mitotoxicity in human HepG2 cells incubated for 2 hrs by Celltiter-Glo assay
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[PMID: 37766386] |
| HepG2 | IC50 |
146 nM
Compound: 2; PF-06835919
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Antiproliferative activity against human HepG2 cells incubated for 3 hrs by LC-MS analysis
Antiproliferative activity against human HepG2 cells incubated for 3 hrs by LC-MS analysis
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[PMID: 37766386] |
体外実験
PF-06835919 reduces steatosis and fibrosis in human hepatocyte-non-parenchymal cell co-cultures exposed to fructose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2102501-84-6
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性状 Solid
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分子量 356.34
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分子式 C16H19F3N4O2
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Color White to off-white
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SMILES
O=C(C[C@H]1[C@@]2(CN(C[C@]12[H])C3=NC(N4[C@H](CC4)C)=NC(C(F)(F)F)=C3)[H])O
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別名
Ketohexokinase inhibitor 1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (280.63 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)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (1.40 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
純度とドキュメンテーション
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データシート (274 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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取扱説明書 (2659 KB)
参考文献
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 | 2.8063 mL | 14.0315 mL | 28.0631 mL | 70.1577 mL |
| 5 mM | 0.5613 mL | 2.8063 mL | 5.6126 mL | 14.0315 mL | |
| 10 mM | 0.2806 mL | 1.4032 mL | 2.8063 mL | 7.0158 mL | |
| 15 mM | 0.1871 mL | 0.9354 mL | 1.8709 mL | 4.6772 mL | |
| 20 mM | 0.1403 mL | 0.7016 mL | 1.4032 mL | 3.5079 mL | |
| 25 mM | 0.1123 mL | 0.5613 mL | 1.1225 mL | 2.8063 mL | |
| 30 mM | 0.0935 mL | 0.4677 mL | 0.9354 mL | 2.3386 mL | |
| 40 mM | 0.0702 mL | 0.3508 mL | 0.7016 mL | 1.7539 mL | |
| 50 mM | 0.0561 mL | 0.2806 mL | 0.5613 mL | 1.4032 mL | |
| 60 mM | 0.0468 mL | 0.2339 mL | 0.4677 mL | 1.1693 mL | |
| 80 mM | 0.0351 mL | 0.1754 mL | 0.3508 mL | 0.8770 mL | |
| 100 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7016 mL |
PF-06835919 関連分類
HY-U00461 関連分類
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Keywords
- PF-06835919
- 2102501-84-6
- Ketohexokinase inhibitor 1
- PF06835919
- PF 06835919
- Ketohexokinase inhibitor1
- Ketohexokinase inhibitor-1
- Ketohexokinase
- type 2 diabetes
- ketohexokinase
- hereditary fructose intolerance
- type 2 diabetes mellitus
- metabolic dysfunction-associated steatotic liver disease
- fructose phosphorylation
- KHK-C
- fructose metabolism
- human hepatocyte-non-parenchymal cell co-cultures
- KHK-A
- Inhibitor
- inhibitor
- inhibit