CAY10594 |
Catalog No.GC18691
One-Click Copy Product Info
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CAY10594 is an orally active phospholipase D2 (PLD2) inhibitor (IC50=140nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1130067-34-3
Sample solution is provided at 25 µL, 10mM.
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CAY10594 is an orally active phospholipase D2 (PLD2) inhibitor (IC50=140nM). CAY10594 inhibits tumor cell invasion and migration by suppressing PLD2 enzyme activity and reducing phosphatidic acid production. CAY10594 reduces inflammation through regulation of the phosphorylated GSK-3β/JNK axis. CAY10594 can be used in research related to breast cancer, acute liver injury and colitis[1-4].
In vitro, treatment with 10 μM CAY10594 for 1 hour or 3 hours in HEp-2, U-2 OS, PC-3 and CaCo-2 cells inhibited phospholipase D activity, caused elevated diacylglycerol and phosphatidylglycerol levels, enlarged endosomes with tubular structures, and enhanced clathrin-independent retrograde transport[5]. Treatment of human RPMI 8226 cells with 10 μM CAY10594 for 5-15 minutes followed by ATP stimulation inhibited ATP-induced CD23 shedding and blocked ATP-induced ethidium entry into RPMI 8226 cells[6]. Pre-treatment of C2C12 cells with 10 μM CAY10594 for 20 minutes followed by co-treatment with 100 mM ethanol for 50 minutes prevented ethanol-induced Akt phosphorylation and blocked ethanol-induced increase in Rictor binding to mTOR[7].
In vivo, daily oral gavage of 4 mg/kg CAY10594 for 10 consecutive days in DSS-induced C57BL/6 mice improved survival rate, reduced body weight loss and bloody stool severity, and lowered pathological scores[8]. A single intraperitoneal injection of 8 mg/kg CAY10594 in C57BL/6 mice 30 minutes before acetaminophen challenge (500 mg/kg; oral gavage) blocked acetaminophen-induced acute liver injury, reduced hepatic necrosis and hepatocyte apoptosis, and decreased serum AST and ALT levels[9].
References:
[1] Roy A, Derakhshan F, Wilson RJ. Stress peptide PACAP engages multiple signaling pathways within the carotid body to initiate excitatory responses in respiratory and sympathetic chemosensory afferents. Am J Physiol Regul Integr Comp Physiol. 2013 Jun 15;304(12):R1070-84.
[2] Park SY, Kang HM, Oh JW, et al. Cucurbitacin B-, E-, and I-Induced Browning of White Adipocytes Is Promoted by the Inhibition of Phospholipase D2. Int J Mol Sci. 2022 Dec 6;23(23):15362.
[3] Obata Y, Natsume M, Shiina I, et al. Golgi retention of KIT in gastrointestinal stromal tumour cells is phospholipase D activity-dependent. Sci Rep. 2025 Aug 6;15(1):28778.
[4] Choudhary V, Olala LO, Qin H, et al. Aquaporin-3 re-expression induces differentiation in a phospholipase D2-dependent manner in aquaporin-3-knockout mouse keratinocytes. J Invest Dermatol. 2015 Feb;135(2):499-507.
[5] Lingelem ABD, Kavaliauskiene S, Halsne R, et al. Diacylglycerol kinase and phospholipase D inhibitors alter the cellular lipidome and endosomal sorting towards the Golgi apparatus. Cellular and Molecular Life Sciences. 2021;78(3):985-1009.
[6] Pupovac A, Stokes L, Sluyter R, et al. CAY10593 inhibits the human P2X7 receptor independently of phospholipase D1 stimulation. Purinergic Signalling. 2013 Sep;9(3):609-19.
[7] Hong-Brown LQ, Brown CR, Navaratnarajah M, et al. Activation of AMPK/TSC2/PLD by alcohol regulates mTORC1 and mTORC2 assembly in C2C12 myocytes. Alcohol Clin Exp Res. 2013 Nov;37(11):1879-92.
[8] Zhou G, Yu L, Yang W, et al. Blockade of PLD2 ameliorates intestinal mucosal inflammation of inflammatory bowel disease. Mediators of Inflammation. 2016;2016:Article ID 2543070.
[9] Lee SK, Bae GH, Kim YS, et al. A phospholipase D2 inhibitor, CAY10594, ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis. Scientific Reports. 2019 May 10;9:7242.
| Cell experiment [1]: | |
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Cell lines |
RPMI 8226 multiple myeloma B cells, P2X7-transfected HEK-293 cells, human peripheral blood mononuclear cells |
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Preparation Method |
RPMI 8226 cells, P2X7-transfected HEK-293 cells and human peripheral blood mononuclear cells were maintained in appropriate complete medium at 37°C, 5% CO2. Cells were pre-incubated with 10μM CAY10594 for 5–15 minutes followed by ATP stimulation, then ethidium+ uptake (pore formation), CD23 shedding or inward current were measured by flow cytometry, fluorescent plate reader or electrophysiology. |
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Reaction Conditions |
10μM; 5–15min pre-incubation |
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Applications |
CAY10594 impaired ATP-induced CD23 shedding from RPMI 8226 cells, inhibited ATP-induced ethidium+ uptake into RPMI 8226 cells, P2X7-transfected HEK-293 cells and human B cells, T cells and monocytes, and showed lower potency than CAY10593 against P2X7-induced pore formation. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice (8-10 weeks, 20-25g) |
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Preparation Method |
C57BL/6 mice were given 2.5% DSS in drinking water for 7 days followed by sterile water for 3 days; concurrently, mice were orally gavaged with 4mg/kg CAY10594 daily for 10 days. On day 10, mice were sacrificed and colonic tissues plus bone marrow neutrophils were collected for H&E staining, qRT-PCR, flow cytometry, and Transwell migration assay. |
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Dosage form |
4mg/kg; oral gavage; daily for 10 days |
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Applications |
CAY10594 administration increased survival rate, attenuated body weight loss and bloody stools, lowered pathological score of colonic mucosa, decreased colonic mRNA and supernatant levels of TNF-α, IL-6, IL-23, IL-1β and IL-17A, increased IL-10 expression, reduced neutrophil percentage in bone marrow, upregulated CXCR2 and downregulated GRK2 in bone marrow neutrophils, and enhanced Transwell migration capacity of bone marrow neutrophils. |
References: [1] Pupovac A, Stokes L, Sluyter R, et al. CAY10593 inhibits the human P2X7 receptor independently of phospholipase D1 stimulation. Purinergic Signalling. 2013 Sep;9(3):609-19. [2] Zhou G, Yu L, Yang W, et al. Blockade of PLD2 ameliorates intestinal mucosal inflammation of inflammatory bowel disease. Mediators of Inflammation. 2016;2016. | |
| Cas No. | 1130067-34-3 | SDF | |
| Chemical Name | N-[2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4,5]dec-8-yl)ethyl]-2-naphthalenecarboxamide | ||
| Canonical SMILES | O=C(NCCN1CCC2(C(NCN2C3=CC=CC=C3)=O)CC1)C4=CC(C=CC=C5)=C5C=C4 | ||
| Formula | C26H28N4O2 | M.Wt | 428.5 |
| Solubility | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3337 mL | 11.6686 mL | 23.3372 mL |
| 5 mM | 466.7 μL | 2.3337 mL | 4.6674 mL |
| 10 mM | 233.4 μL | 1.1669 mL | 2.3337 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)