| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C12H11NO3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CID755673 is a potent inhibitor of protein kinase D (PKD), with IC50 values of 182 nM, 280 nM, and 227 nM against PKD1, PKD2, and PKD3, respectively. It is supplied as a white to off-white solid (C12H11NO3, MW 217.22) at 99.13% purity.
Physical & Chemical Properties
| CAS Number | 521937-07-5 |
|---|---|
| Molecular Formula | C12H11NO3 |
| Molecular Weight | 217.22 g/mol |
| Purity | 99.13% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C1NCCCC2=C1OC3=CC=C(O)C=C32 |
| Target | PKD1/PKCμ, PKD3, PKD2 |
| Signaling Pathway | Apoptosis |
| Solubility | In Vitro: DMSO: 100 mg/mL (460.36 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
PKD1/PKCμ 182 nM (IC50) |
PKD3 227 nM (IC50) |
PKD2 280 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (460.36 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (11.51 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (11.51 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (11.51 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
CID755673 blocks phorbol ester-induced activation of endogenous PKD1 in LNCaP cells, in a concentration-dependent manner. The known biological actions of PKD1 are inhibited by CID755673, including phorbol ester-induced nuclear exclusion of class IIa histone deacetylase 5, transport of vesicular stomatitis virus glycoprotein from the Golgi to the plasma membrane, and ilimaquinone-induced Golgi fragmentation. CID755673 inhibits proliferation, migration, and invasion of prostate cancer cells[1].
In Vivo
In normal mice, acute administration of the PKD inhibitor CID755673 lowers both PKD1 and 2 phosphorylation in a time and dose-dependent manner. In T2D db/db mice, chronic CID755673 administration for two weeks lowers the PKD-activation gene expression signature, improves indices of both diastolic and systolic left ventricular function, and is associated with lower heart weight[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Trigger wound-induced migration by scraping the cells with a plastic pipette tip, and image the wound immediately. Treat the DU145 cells with or without CID755673 at different concentrations. Image the wound immediately (0 h) and at various intervals using an inverted phase-contrast microscope equipped with a ×10 objective. At the end of the assay, fix the cells with methanol and stain with crystal violet for a final image[1].
Animal Administration[2]
Mice: For acute inhibitor studies, administer C57BL6 mice a single dose of vehicle (5% DMSO in PBS, pH 7.4) or CID755673, a selective PKD inhibitor, at 1 or 10mg/kg body weight. Kill the mice one or four hr later and collect the hearts for later analysis. For chronic inhibitor experiments, give 8-week old db/db mice vehicle or CID755673 at 1 or 10mg/kg bodyweight for 16 days by daily intraperitoneal (i.p.) injection[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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The L1 cell adhesion molecule affects protein kinase D1 activity in the cerebral cortex in a mouse model of Alzheimer's disease. Brain Res Bull 2020 Sep:162:141-150. PMID: 32540419
Protein kinase D1 promotes the survival of random-pattern skin flaps in rats. Biochem Biophys Res Commun 2023 Jan 22:641:67-76. PMID: 36525926
β-catenin stimulates Tcf7l1 degradation through recruitment of casein kinase 2 in mouse embryonic stem cells. Biochem Biophys Res Commun 2020 Apr 2;524(2):280-287.
Angiogenic function of astragaloside IV in rats with myocardial infarction occurs via the PKD1-HDAC5-VEGF pathway. Exp Ther Med 2019 Apr;17(4):2511-2518.
Int J Clin Exp Med. 2017;10(7):10528-10534.
Chinese Journal of Pathophysiology. 2016, 32(1):146-150, 155.
