2. Epigenetics Cytoskeleton Cell Cycle/DNA Damage GPCR/G Protein TGF-beta/Smad Stem Cell/Wnt
  3. ROCK G Protein-coupled Receptor Kinase (GRK) PKC
  4. CMPD101 hydrochloride

CMPD101 hydrochloride is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 hydrochloride also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s =1.4 μM and 8.1 μM, respectively).

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No. CAS : 1941168-71-3

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Top Publications Citing Use of Products

    CMPD101 hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 10;23(16):8903.

    CMPD101 (10 µM) significantly increased the maximal CI[3-20] and AUC[20-120].

    CMPD101 hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 Mar 10;12(3):426.

    CMPD101 (0.001–10 μM) significantly cancelled the ketamine-induced improvement of the decrease in MOR activity in HEK293 cells evoked by repeated administration of 100 nM fentanyl.

    CMPD101 hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 Mar 10;12(3):426.

    CMPD101 (1-10 µM) significantly cancelled the ketamine-induced improvement in the rescue of cAMP in HEK293 cells caused by repeated administration of 100 nM fentanyl.

    CMPD101 hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 Mar 10;12(3):426.

    CMPD101 (1–10 µM) significantly cancelled the ketamine-induced enhancement of β-arrestin recruitment to MOR U2OS OPRM1 induced by the repeated administration of 100 nM fentanyl.

    CMPD101 hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Jun 9;39(1):107.  [Abstract]

    CMPD101 (0.1-30 μM) significantly reduced growth of gastric cancer cells.

    Ver todos los productos específicos de isoformas ROCK:

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    ROCK ROCK1 ROCK2

    Ver todos los productos específicos de isoformas PKC:

    Ver todas las isoformas
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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    Descripciòn

    CMPD101 hydrochloride is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 hydrochloride also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s =1.4 μM and 8.1 μM, respectively)[1].

    IC50 & Target[1]

    GRK2

     

    PKCα

    8.1 μM (IC50)

    ROCK2

    1.4 μM (IC50)

    Peso molecular

    502.92

    Fòrmula

    C24H22ClF3N6O
    No. CAS
    SMILES

    O=C(C1=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=CC=C1)NCC4=CC=CC=C4C(F)(F)F.[H]Cl
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Pureza y Documentación
    Referencias
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    CMPD101 hydrochloride Related Classifications

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    CMPD1011941168-71-3CMPD 101CMPD-101ROCKG Protein-coupled Receptor Kinase (GRK)PKCRho-associated protein kinaseRho-associated kinaseRho-kinaseROKProtein kinase CInhibitorinhibitorinhibit

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    Nombre del producto:
    CMPD101 hydrochloride
    Cat. No.:
    HY-103045A
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