Home Apoptosis PKD inhibitor - CaMK inhibitor CID755673

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CID755673 PKD inhibitor

Cat.No.S7188

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 PKD inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 217.22

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 217.22 Formula

C12H11NO3

 Storage (From the date of receipt)
CAS No. 521937-07-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CC2=C(C(=O)NC1)OC3=C2C=C(C=C3)O

Solubility

In vitro
Batch:

DMSO : 43 mg/mL (197.95 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Mechanism of Action

Targets/IC50/Ki
PKD1 [1]
180 nM
PKD3 [1]
227 nM
PKD2 [1]
280 nM
In vitro
In LNCaP prostate cancer cells, CID755673 directly inhibits PKD1 activity. In HeLa cells, this compound significantly blocks PMA-induced nuclear export of HDAC5, and blocks PKD-mediated protein transport. In prostate cancer cells, it potently blocks cell migration and invasion, and also shows inhibition activity on tumor cell proliferation and cell cycle distribution. [1] In addition, this chemical alter primary human NK cell effector functions. [3]
Kinase Assay
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.
In vivo
CID755673, via PKD/PKD1 inhibition, significantly ameliorates necrosis and severity of pancreatitis in a rat acute pancreatitis model. [2]
References

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