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  3. CID755673

CID755673 

Cat. No.: HY-12239 Purity: 99.54%
Handling Instructions

CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.

For research use only. We do not sell to patients.

CID755673 Chemical Structure

CID755673 Chemical Structure

CAS No. : 521937-07-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CID755673 purchased from MCE. Usage Cited in: Chinese Journal of Pathophysiology. 2016, 32(1):146-150, 155.

    The effects of PKD1 on the mRNA and protein expression of VEGF and KDR in the endothelial progenitor cells ( EPCs).

    CID755673 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(7):10528-10534.

    Effect of PKD1 on the expression levels of VEGF and KDR in the myocardial tissue in rat models of myocardial infarction. Rat models of myocardial infarction are treated with 10 mg/kg/d PKD1, alone or with 10 mg/kg/d CID755673 for 14 d. Then the mRNA and protein expression levels of VEGF and KDR are detected with RT-PCR.

    CID755673 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(7):10528-10534.

    Effect of PKD1 on the expression levels of VEGF and KDR in the myocardial tissue in rat models of myocardial infarction. Rat models of myocardial infarction are treated with 10 mg/kg/d PKD1, alone or with 10 mg/kg/d CID755673 for 14 d. Then the mRNA and protein expression levels of VEGF and KDR are detected with Western blot analysis.

    CID755673 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2020 Jan 24. pii: S0006-291X(20)30143-1.B

    Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with the indicative different small molecules for 1 h and then treated with CHIR for 24 h.

    View All PKD Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.

    IC50 & Target[1]

    PKD1

    182 nM (IC50)

    PKD3

    227 nM (IC50)

    PKD2

    280 nM (IC50)

    In Vitro

    CID755673 blocks phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. CID755673 inhibits the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. CID755673 inhibits prostate cancer cell proliferation, cell migration, and invasion[1].

    In Vivo

    Acute administration of the PKD inhibitor CID755673 to normal mice reduces both PKD1 and 2 phosphorylation in a time and dose-dependent manner. Chronic CID755673 administration to T2D db/db mice for two weeks reduces expression of the gene expression signature of PKD activation, enhances indices of both diastolic and systolic left ventricular function and is associated with reduced heart weight[2].

    Molecular Weight

    217.22

    Formula

    C₁₂H₁₁NO₃

    CAS No.

    521937-07-5

    SMILES

    O=C1NCCCC2=C1OC3=CC=C(O)C=C32

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (460.36 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.6036 mL 23.0181 mL 46.0363 mL
    5 mM 0.9207 mL 4.6036 mL 9.2073 mL
    10 mM 0.4604 mL 2.3018 mL 4.6036 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    The wound-induced migration is triggered by scraping the cells with a plastic pipette tip, and the wound is imaged immediately. The DU145 cells are then are treated with or without CID755673 at different concentrations. The wound is imaged immediately (0 h) and at different intervals with an inverted phase-contrast microscope with a ×10 objective. At the end of the assay, cells are fixed with methanol and stained with crystal violet for a final image[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice: For acute inhibitor studies, C57BL6 mice are administered a single dose of vehicle (5% DMSO in PBS, pH 7.4), or the selective PKD inhibitor CID755673 at 1 or 10mg/kg body weight. Mice are killed one or four hr later and heart collected for later analysis. For chronic inhibitor experiments, 8-week old db/db mice receives vehicle or CID755673 at 1 or 10mg/kg bodyweight for 16 days, by daily intraperitoneal (i.p.) injection[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.54%

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    Keywords:

    CID755673CID 755673CID-755673PKDProtein kinase DInhibitorinhibitorinhibit

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    Product Name:
    CID755673
    Cat. No.:
    HY-12239
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