CID755673

For research use only.

Catalog No.S7188

5 publications

CID755673 Chemical Structure

CAS No. 521937-07-5

CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs.

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Selleck's CID755673 has been cited by 5 publications

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Choose Selective PKD Inhibitors

Biological Activity

Description CID755673 is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, about 200-fold selectivity over other CAMKs.
Targets
PKD1 [1]
()
PKD3 [1]
()
PKD2 [1]
()
180 nM 227 nM 280 nM
In vitro

In LNCaP prostate cancer cells, CID755673 directly inhibits PKD1 activity. In HeLa cells, CID755673 significantly blocks PMA-induced nuclear export of HDAC5, and blocks PKD-mediated protein transport. In prostate cancer cells, CID755673 potently blocks cell migration and invasion, and also shows inhibition activity on tumor cell proliferation and cell cycle distribution. [1] In addition, CID755673 alter primary human NK cell effector functions. [3]

In vivo CID755673, via PKD/PKD1 inhibition, significantly ameliorates necrosis and severity of pancreatitis in a rat acute pancreatitis model. [2]

Protocol

Kinase Assay: [1]
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In Vitro Radiometric PKD Kinase Assay:

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. The filter papers are then washed three times in 0.5% phosphoric acid, air-dried, and counted using a Beckman LS6500 multipurpose scintillation counter.
Cell Research:[1]
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  • Cell lines: LNCaP or PC3 cells
  • Concentrations: ~25 μM
  • Incubation Time: 6 days
  • Method: Cell proliferation was determined by counting the number of viable cells upon trypan blue staining. Cell proliferation is measured by CellTiter-Glo Luminescent Cell Viability Assay according to the manufacturer's instructions.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: Rat pancreatitis model
  • Dosages: ~15 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 43 mg/mL (196.13 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2%DMSO+30%peg300+2%t-80+ddaH2O
For best results, use promptly after mixing.
6mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 219.24
Formula

C12H11NO3

CAS No. 521937-07-5
Storage powder
in solvent
Synonyms N/A
Smiles C1CC2=C(C(=O)NC1)OC3=C2C=C(C=C3)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID