CMPD101

SKU: orb1308435

Description

CMPD101 is a potent, cell-permeable inhibitor of GRK2 and GRK3, with IC50 values of 18 nM and 5.4 nM respectively. It is a valuable research tool for investigating heart failure mechanisms and GRK signaling in both cellular and animal models, though it shows weaker activity against GRK1, GRK5, ROCK-2, and PKCα.

Research Area

Cell Biology, Epigenetics & Chromatin, Pharmacology & Drug Discovery, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 865608-11-3
• MW: 466.46
• Purity: 99.52% (May vary between batches)
• Formula: C₂₄H₂₁F₃N₆O
• SMILES: Cn1c(CNc2cccc(c2)C(=O)NCc2ccccc2C(F)(F)F)nnc1-c1ccncc1
• Target: PKC,GRK,ROCK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (10.72 mM);DMSO:250 mg/mL (535.95 mM)

Bioactivity

• Target IC50:
  PKCα:8.1 μM|ROCK2:1.4 μM|GRK3:5.4 nM|GRK2:18 nM
• In Vitro:
  CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, significantly reduces the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line. CMPD101 (3-30 μM; pre-30 minutes) does not influence 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. 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 Cmpd101and it also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

desensitization, CMPD 101, CMPD101, CMPD-101, failure, GRK2, GRK3, heart, Inhibitor, Neuron, inhibit, PKC, PKCα, Rho-associated protein kinase, Rho-associated kinase, Rho-kinase, ROK, ROCK, ROCK2, Protein kinase C

Compound Identifiers

PubChem CID

11677079