1. Epigenetics
    TGF-beta/Smad
    Cell Cycle/DNA Damage
    Stem Cell/Wnt
    Cytoskeleton
  2. PKC
    ROCK
  3. CMPD101

CMPD101 

Cat. No.: HY-103045 Purity: >98.0%
Handling Instructions

CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.

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

CMPD101 Chemical Structure

CMPD101 Chemical Structure

CAS No. : 865608-11-3

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Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure[1].

IC50 & Target[1]

GRK2

18 nM (IC50)

GRK3

5.4 nM (IC50)

PKCα

8.1 μM (IC50)

ROCK2

1.4 μM (IC50)

In Vitro

CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, remarkably decreases the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line[1].
CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375, which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101. It also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues[2].
CMPD101 (3-30 μM; pre-30 minutes) does not affect the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30 μM, this compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs[2].

Western Blot Analysis[2]

Cell Line: HEK 293 cells stably expressing HA-tagged rat MOPr
Concentration: 3 μM, 30 μM
Incubation Time: Pre-30 minutes
Result: Surpressed Ser375 expression completely at a high dose.

Western Blot Analysis[2]

Cell Line: HEK 293 cells stably expressing HA-tagged rat MOPr
Concentration: 3 μM, 30 μM
Incubation Time: Pre-30 minutes
Result: Had no effect on DAMGO-induced p-ERK1/2 and p-Elk-1 expression.
Molecular Weight

466.46

Formula

C₂₄H₂₁F₃N₆O

CAS No.

865608-11-3

SMILES

O=C(C1=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=CC=C1)NCC4=CC=CC=C4C(F)(F)F

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
References

Purity: >98.0%

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Keywords:

CMPD101CMPD 101CMPD-101PKCROCKProtein kinase CRho-associated protein kinaseRho-associated kinaseRho-kinaseROKNeuronheartfailuredesensitizationInhibitorinhibitorinhibit

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