product name CID755673
Description: CID755673, also known as benzoxoloazepinolone, is a cell-active pan-PKD1/2/3 inhibitor with IC50 of 180 nM, 280nM, and 227 nM, respectively, it shows about 200-fold selectivity over other CAMKs. CID755673 is the first identified cell-active small molecule PKD antagonist. It inhibits the activity of PKD1 with an IC50 of 182 nM and demonstrates highest selectivity to PKD1 when compared with AKT, PLK1, CAK, CAMKIIα, PKD2 and PKD3. Moreover, it was not competitive with ATP for enzyme inhibition. In HeLa cells, CID755673 significantly blocks PMA-induced nuclear export of HDAC5, and blocks PKD-mediated protein transport.
References: J Biol Chem. 2008 Nov 28;283(48):33516-26; Front Physiol. 2012 Mar 27;3:60; Front Immunol. 2013 Mar 18;4:66.
219.24
Formula
C12H11NO3
CAS No.
521937-07-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 43 mg/mL (196.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. In addition, CID755673 alter primary human NK cell effector functions. 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 Assay: Cell proliferation was determined by counting the number of viable cells (LNCaP or PC3 cells) upon trypan blue staining. Cell proliferation is measured by CellTiter-Glo Luminescent Cell Viability Assay according to the manufacturers instructions. |
|---|---|
| In Vivo | CID755673, via PKD/PKD1 inhibition, significantly ameliorates necrosis and severity of pancreatitis in a rat acute pancreatitis model. |
| Animal model | Rat pancreatitis model |
| Formulation & Dosage | Dissolved in DMSO; 15 mg/kg; i.p. injection |
| References | J Biol Chem. 2008 Nov 28;283(48):33516-26; Front Physiol. 2012 Mar 27;3:60; Front Immunol. 2013 Mar 18;4:66. |
