Art. -Nr.: HY-121983

CAY10594

1 Cited Publications

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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.

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Reinheit: 98.64%
CAS. Nr.: 1130067-34-3
Formel: C₂₆H₂₈N₄O₂
Molecular Weight:428.53

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CAY10594 Chemical Structure

CAS. Nr.: 1130067-34-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]^[3]^[4]

p-STAT3

GSK-3β

IL-6

IL-17A

IL-23

IL-1β

CXCR2

GRK2

Alle Phospholipase Isoform-spezifische Produkte anzeigen :

Alle GSK-3 Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

Alle CXCR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Calu-1	IC₅₀	1 μM Compound: 72	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	[PMID: 19136975]
Calu-1	IC₅₀	1 μM Compound: 3	Inhibition of PLD1 in human Calu1 cells Inhibition of PLD1 in human Calu1 cells	[PMID: 19299128]
HEK293	IC₅₀	110 nM Compound: 72	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	[PMID: 19136975]
HEK293	IC₅₀	110 nM Compound: 3	Inhibition of GFP-labeled PLD2 in human HEK293 cells Inhibition of GFP-labeled PLD2 in human HEK293 cells	[PMID: 19299128]
HEK293	IC₅₀	110 nM Compound: 15a	Inhibition of human GST-tagged PLD2A in human HEK293 cells Inhibition of human GST-tagged PLD2A in human HEK293 cells	[PMID: 20735042]

In Vitro

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.

Western Blot Analysis^[2]

Cell Line:

Human umbilical vein endothelial cells (HUVECs) treated LPS (HY-D1056)
Concentration:

10 μM
Incubation Time:

Pretreated with 1 h, then co-incubation for 6 h
Result:

Increased the levels of occludin and ZO-1.

Western Blot Analysis^[3]

Cell Line:

Primary hepatocyte treated Acetaminophen (HY-66005)
Concentration:

10 μM
Incubation Time:

0, 2, 4, 6, 8 and 10 h
Result:

Inhibited the level of pGSK-3β.

In Vivo

CAY10594 (1-8 mg/kg; intraperitoneal injection; single dose) exerts a protective effect in a mouse model of acute liver injury^[3].
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.

Animal Model:

C57BL/6 mice treated Acetaminophen (HY-66005) to induce acute liver injury^[3]
Dosage:

1, 4 and 8 mg/kg
Administration:

Intraperitoneal injection; single dose
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.

Animal Model:

C57BL/6 mice (20-25 g, 8-10 weeks old) treated DSS (HY-116282C) to induce colitis^[4]
Dosage:

4 mg/kg
Administration:

Oral gavage; 10 days
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

CAS. Nr. 1130067-34-3
Appearance Solid
Molecular Weight 428.53
Formel C₂₆H₂₈N₄O₂
Color White to off-white
SMILES

O=C(C1=CC2=C(C=C1)C=CC=C2)NCCN3CCC4(CC3)C(NCN4C5=CC=CC=C5)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3336 mL

11.6678 mL

23.3356 mL

5 mM

0.4667 mL

2.3336 mL

4.6671 mL

10 mM

0.2334 mL

1.1668 mL

2.3336 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.14 mg/mL (2.66 mM); Clear solution

This protocol yields a clear solution of ≥ 1.14 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.4 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

1 Cited Publications

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CAY10594

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Publications Citing Use of MedChemExpress (MCE) CAY10594

Alle Phospholipase Isoform-spezifische Produkte anzeigen

Alle GSK-3 Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Alle CXCR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CAY10594 Related Classifications

HY-121983 Related Classifications