CID755673
Based on 6 publication(s) in Google Scholar
CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.13%
- CAS. Nr.: 521937-07-5
- Formel: C12H11NO3
- Molecular Weight:217.22
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) CID755673
More- Brain Res Bull. 2020 Sep;162:141-150. [Abstract]
- Exp Ther Med. 2019 Apr;17(4):2511-2518. [Abstract]
- Biochem Biophys Res Commun. 2023 Jan 22:641:67-76. [Abstract]
- Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]
- Int J Clin Exp Med. 2017;10(7):10528-10534.
- Chinese Journal of Pathophysiology. 2016, 32(1):146-150, 155.
Customer Validation & Images
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RT-PCR
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Biologische Aktivität
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PKD1/PKCμ 182 nM (IC50) |
PKD3 227 nM (IC50) |
PKD2 280 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| LNCaP | IC50 |
11.8 μM
Compound: CID755673
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Inhibition of PKD1 autophosphorylation at Ser916 in human PMA-induced LNCAP cells by Western blotting
Inhibition of PKD1 autophosphorylation at Ser916 in human PMA-induced LNCAP cells by Western blotting
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[PMID: 21617763] |
CID755673 blocks phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. CID755673 inhibits the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. CID755673 inhibits prostate cancer cell proliferation, cell migration, and invasion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 521937-07-5
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Appearance Solid
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Molecular Weight 217.22
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Formel C12H11NO3
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Color White to off-white
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SMILES
O=C1NCCCC2=C1OC3=CC=C(O)C=C32
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Brain Res Bull
The L1 cell adhesion molecule affects protein kinase D1 activity in the cerebral cortex in a mouse model of Alzheimer's disease. [Abstract]2020 Sep;162:141-150. PMID: 32540419 -
Exp Ther Med
Angiogenic function of astragaloside IV in rats with myocardial infarction occurs via the PKD1-HDAC5-VEGF pathway. [Abstract]2019 Apr;17(4):2511-2518. PMID: 30906439 -
Biochem Biophys Res Commun
2023 Jan 22:641:67-76. PMID: 36525926 -
Biochem Biophys Res Commun
β-catenin stimulates Tcf7l1 degradation through recruitment of casein kinase 2 in mouse embryonic stem cells. [Abstract]2020 Apr 2;524(2):280-287. PMID: 31987502
CID755673 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]
Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with the indicative different small molecules for 1 h and then treated with CHIR for 24 h.
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CID755673 purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Med. 2017;10(7):10528-10534.
Effect of PKD1 on the expression levels of VEGF and KDR in the myocardial tissue in rat models of myocardial infarction. Rat models of myocardial infarction are treated with 10 mg/kg/d PKD1, alone or with 10 mg/kg/d CID755673 for 14 d. Then the mRNA and protein expression levels of VEGF and KDR are detected with RT-PCR.
CID755673 purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Med. 2017;10(7):10528-10534.
Effect of PKD1 on the expression levels of VEGF and KDR in the myocardial tissue in rat models of myocardial infarction. Rat models of myocardial infarction are treated with 10 mg/kg/d PKD1, alone or with 10 mg/kg/d CID755673 for 14 d. Then the mRNA and protein expression levels of VEGF and KDR are detected with Western blot analysis.
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CID755673 purchased from MedChemExpress. Usage Cited in: Chinese Journal of Pathophysiology. 2016, 32(1):146-150, 155.
The effects of PKD1 on the mRNA and protein expression of VEGF and KDR in the endothelial progenitor cells ( EPCs).
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (460.36 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (11.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Protokoll
The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μL of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The wound-induced migration is triggered by scraping the cells with a plastic pipette tip, and the wound is imaged immediately. The DU145 cells are then are treated with or without CID755673 at different concentrations. The wound is imaged immediately (0 h) and at different intervals with an inverted phase-contrast microscope with a ×10 objective. At the end of the assay, cells are fixed with methanol and stained with crystal violet for a final image[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: For acute inhibitor studies, C57BL6 mice are administered a single dose of vehicle (5% DMSO in PBS, pH 7.4), or the selective PKD inhibitor CID755673 at 1 or 10mg/kg body weight. Mice are killed one or four hr later and heart collected for later analysis. For chronic inhibitor experiments, 8-week old db/db mice receives vehicle or CID755673 at 1 or 10mg/kg bodyweight for 16 days, by daily intraperitoneal (i.p.) injection[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 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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Handling Instructions (2659 KB)
Verweise
[1]. Sharlow ER, et al. Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone. J Biol Chem. 2008 Nov 28;283(48):33516-26. [Content Brief]
[2]. Venardos K, et al. The PKD inhibitor CID755673 enhances cardiac function in diabetic db/db mice. PLoS One. 2015 Mar 23;10(3):e0120934. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.6036 mL | 23.0181 mL | 46.0363 mL | 115.0907 mL |
| 5 mM | 0.9207 mL | 4.6036 mL | 9.2073 mL | 23.0181 mL | |
| 10 mM | 0.4604 mL | 2.3018 mL | 4.6036 mL | 11.5091 mL | |
| 15 mM | 0.3069 mL | 1.5345 mL | 3.0691 mL | 7.6727 mL | |
| 20 mM | 0.2302 mL | 1.1509 mL | 2.3018 mL | 5.7545 mL | |
| 25 mM | 0.1841 mL | 0.9207 mL | 1.8415 mL | 4.6036 mL | |
| 30 mM | 0.1535 mL | 0.7673 mL | 1.5345 mL | 3.8364 mL | |
| 40 mM | 0.1151 mL | 0.5755 mL | 1.1509 mL | 2.8773 mL | |
| 50 mM | 0.0921 mL | 0.4604 mL | 0.9207 mL | 2.3018 mL | |
| 60 mM | 0.0767 mL | 0.3836 mL | 0.7673 mL | 1.9182 mL | |
| 80 mM | 0.0575 mL | 0.2877 mL | 0.5755 mL | 1.4386 mL | |
| 100 mM | 0.0460 mL | 0.2302 mL | 0.4604 mL | 1.1509 mL |
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