CID755673

Catalog No.S7188

For research use only.

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.

CID755673 Chemical Structure

CAS No. 521937-07-5

Selleck's CID755673 has been cited by 5 Publications

Purity & Quality Control

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 (from reference)

Kinase Assay: [1]
  • 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]
  • 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.
Animal Research:[2]
  • Animal Models: Rat pancreatitis model
  • Dosages: ~15 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 217.22
Formula

C12H11NO3

CAS No. 521937-07-5
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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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 ddH2O, 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.

Molarity Calculator

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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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