CAY10594
Based on 1 publication(s) in Google Scholar
CAY10594 is an orally active PLD2 inhibitor with an IC50 of 140 nM. CAY10594 has activities such as anti-tumor, anti-oxidation and liver protection. CAY10594 can be used for the research of diseases like breast cancer, acute liver injury and colitis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.64%
- No. CAS: 1130067-34-3
- Fòrmula: C26H28N4O2
- Peso molecular:428.53
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CAY10594
MoreVer todos los productos específicos de isoformas Phospholipase
More
Actividad biológica
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p-STAT3 |
GSK-3β |
IL-6 |
IL-17A |
IL-23 |
IL-1β |
CXCR2 |
GRK2 |
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Cell Line
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Type | Value | Description | References |
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| Calu-1 | IC50 |
1 μM
Compound: 72
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Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis
Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis
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[PMID: 19136975] |
| Calu-1 | IC50 |
1 μM
Compound: 3
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Inhibition of PLD1 in human Calu1 cells
Inhibition of PLD1 in human Calu1 cells
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[PMID: 19299128] |
| HEK293 | IC50 |
110 nM
Compound: 72
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Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis
Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis
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[PMID: 19136975] |
| HEK293 | IC50 |
110 nM
Compound: 3
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Inhibition of GFP-labeled PLD2 in human HEK293 cells
Inhibition of GFP-labeled PLD2 in human HEK293 cells
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[PMID: 19299128] |
| HEK293 | IC50 |
110 nM
Compound: 15a
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Inhibition of human GST-tagged PLD2A in human HEK293 cells
Inhibition of human GST-tagged PLD2A in human HEK293 cells
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[PMID: 20735042] |
CAY10594 (Compound 72) (20 μM; 48 h) inhibits the migration of MDA-231, 4T1, and PMT breast cancer cells[1].
CAY10594 (10 μM; 7 h) improves LPS (HY-D1056)-induced increased endothelial permeability and decreased transendothelial electrical resistance, inhibits phosphatidic acid production and STAT3 phosphorylation, and enhances the expression of tight junction proteins in HUVECs[2].
CAY10594 (10 μM; 0-16 h) significantly reduces Acetaminophen (HY-66005)-induced lactate dehydrogenase release and cell death, and blocks GSK-3β phosphorylation in primary hepatocytes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human umbilical vein endothelial cells (HUVECs) treated LPS (HY-D1056)
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Concentration:10 μM
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Incubation Time:Pretreated with 1 h, then co-incubation for 6 h
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Result:Increased the levels of occludin and ZO-1.
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Cell Line:Primary hepatocyte treated Acetaminophen (HY-66005)
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Concentration:10 μM
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Incubation Time:0, 2, 4, 6, 8 and 10 h
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Result:Inhibited the level of pGSK-3β.
CAY10594 (4 mg/kg; oral gavage; 10 days) shows ameliorative effects in a mouse model of colitis[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice treated Acetaminophen (HY-66005) to induce acute liver injury[3]
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Dosage:1, 4 and 8 mg/kg
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Administration:Intraperitoneal injection; single dose
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Result:Significantly alleviated hepatic pathological damage, as demonstrated by reduced necrosis and apoptosis in liver tissue sections.
Decreased serum levels of AST and ALT, key markers of liver injury.
Improved the survival rate of mice.
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Animal Model:C57BL/6 mice (20-25 g, 8-10 weeks old) treated DSS (HY-116282C) to induce colitis[4]
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Dosage:4 mg/kg
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Administration:Oral gavage; 10 days
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Result:Significantly improved clinical symptoms including higher survival rate, less body weight loss, and reduced bloody stools.
Alleviated pathological damage in colon tissues,
Decreased proinflammatory cytokines (TNF-α, IL-6, IL-17A, IL-23, IL-1β) expression, increased anti-inflammatory cytokine (IL-10) expression, and promoted neutrophil migration by upregulating CXCR2 and downregulating GRK2.
Chemical Information
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No. CAS 1130067-34-3
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Appearance Solid
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Peso molecular 428.53
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Fòrmula C26H28N4O2
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Color White to off-white
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SMILES
O=C(C1=CC2=C(C=C1)C=CC=C2)NCCN3CCC4(CC3)C(NCN4C5=CC=CC=C5)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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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Biochem Pharmacol
Phospholipase D2 regulation by transcription factor FOXA1 promotes the drug resistance of vemurafenib in melanoma cells. [Abstract]2025 Dec;242(Pt 4):117434. PMID: 41110487
Solvente y solubilidad
DMSO : 100 mg/mL (233.36 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)
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: ≥ 1.14 mg/mL (2.66 mM); Clear solution
This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 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.
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.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Scott SA, et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol. 2009 Feb;5(2):108-17. [Content Brief]
[2]. Qian T, et al. PLD2 deletion alleviates disruption of tight junctions in sepsis-induced ALI by regulating PA/STAT3 phosphorylation pathway. Int Immunopharmacol. 2023 Jan;114:109561. [Content Brief]
[3]. Lee SK, et al. A phospholipase D2 inhibitor, CAY10594, ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis. Sci Rep. 2019 May 10;9(1):7242. [Content Brief]
[4]. Zhou G, et al. Blockade of PLD2 Ameliorates Intestinal Mucosal Inflammation of Inflammatory Bowel Disease. Mediators Inflamm. 2016;2016:2543070. [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 | 2.3336 mL | 11.6678 mL | 23.3356 mL | 58.3390 mL |
| 5 mM | 0.4667 mL | 2.3336 mL | 4.6671 mL | 11.6678 mL | |
| 10 mM | 0.2334 mL | 1.1668 mL | 2.3336 mL | 5.8339 mL | |
| 15 mM | 0.1556 mL | 0.7779 mL | 1.5557 mL | 3.8893 mL | |
| 20 mM | 0.1167 mL | 0.5834 mL | 1.1668 mL | 2.9169 mL | |
| 25 mM | 0.0933 mL | 0.4667 mL | 0.9334 mL | 2.3336 mL | |
| 30 mM | 0.0778 mL | 0.3889 mL | 0.7779 mL | 1.9446 mL | |
| 40 mM | 0.0583 mL | 0.2917 mL | 0.5834 mL | 1.4585 mL | |
| 50 mM | 0.0467 mL | 0.2334 mL | 0.4667 mL | 1.1668 mL | |
| 60 mM | 0.0389 mL | 0.1945 mL | 0.3889 mL | 0.9723 mL | |
| 80 mM | 0.0292 mL | 0.1458 mL | 0.2917 mL | 0.7292 mL | |
| 100 mM | 0.0233 mL | 0.1167 mL | 0.2334 mL | 0.5834 mL |
CAY10594 Related Classifications
HY-121983 Related Classifications
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