2. Metabolic Enzyme/Protease Apoptosis Stem Cell/Wnt PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation GPCR/G Protein
  3. Phospholipase Apoptosis GSK-3 Anaplastic lymphoma kinase (ALK) STAT Interleukin Related G Protein-coupled Receptor Kinase (GRK) CXCR Lactate Dehydrogenase
  4. CAY10594

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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CAY10594

CAY10594 構造式

CAS 番号 : 1130067-34-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 220 在庫あり
Solution
10 mM * 1 mL in DMSO USD 220 在庫あり
Solid
1 mg $95 在庫あり
5 mg $200 在庫あり
10 mg $340 在庫あり
25 mg $600 在庫あり
50 mg $900 在庫あり
100 mg $1350 在庫あり
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500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

CAY10594 関連抗体

Top Publications Citing Use of Products

Phospholipase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Phospholipase A PLD Phospholipase C

GSK-3 アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
GSK-3 GSK-3α GSK-3β

STAT アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
STAT3 STAT5 STAT6 STAT1

Interleukin Related アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

CXCR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

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  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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[1][2][3][4].

IC50 & Target[2][3][4]

p-STAT3

 

GSK-3β

 

IL-6

 

IL-17A

 

IL-23

 

IL-1β

 

CXCR2

 

GRK2

 

Cellular Effect
Cell Line Type Value Description References
Calu-1 IC50
1000 nM
Compound: 3
Inhibition of PLD1 in human Calu1 cells
Inhibition of PLD1 in human Calu1 cells
[PMID: 19299128]
Calu-1 IC50
1000 nM
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]
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]
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: 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]
体外実験

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.

CAY10594 関連抗体

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.
体内実験

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.
分子量

428.53

分子式

C26H28N4O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC2=C(C=C1)C=CC=C2)NCCN3CCC4(CC3)C(NCN4C5=CC=CC=C5)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
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 2.3336 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
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CAY10594 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

CAY105941130067-34-3CAY 10594CAY-10594PhospholipaseApoptosisGSK-3Anaplastic lymphoma kinase (ALK)STATInterleukin RelatedG Protein-coupled Receptor Kinase (GRK)CXCRLactate DehydrogenaseGlycogen synthase kinase-3Glycogen synthase kinase 3Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ILCXC chemokine receptorsC-X-C motif chemokine receptorsLDHacute liver injury modelcolitis modelMDA-2314T1PMTHUVECsprimary hepatocytesInhibitorinhibitorinhibit

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