1. GPCR/G Protein
    Stem Cell/Wnt
    Cell Cycle/DNA Damage
    TGF-beta/Smad
  2. Ras
    ROCK
  3. CCG-222740

CCG-222740 

Cat. No.: HY-121750
Handling Instructions

CCG-222740 is a potent and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 also is a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.

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

CCG-222740 Chemical Structure

CCG-222740 Chemical Structure

CAS No. : 1922098-69-8

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Description

CCG-222740 is a potent and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor[1]. CCG-222740 also is a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis[2].

IC50 & Target

Rho/MRTF pathway[1]

In Vitro

CCG-222740 (10, 20 μM; for 72 hours) increases the protein levels of p27 and decreased cyclin D1. CCG-222740 decreases cell viability of CAFs, with an IC50 of ~10 μM[1].
CCG-222740 (10, 25 μM) is potent at decreasing αSMA protein expression in human conjunctival fibroblasts[2].
CCG-222740 has an IC50 of 5 μM in a fibroblast-mediated collagen contraction assay, and it is less cytotoxic[2].

Cell Cycle Analysis[1]

Cell Line: Cancer associated fibroblasts (CAFs)
Concentration: 10, 20 μM
Incubation Time: 72 hours
Result: Increased the protein levels of p27 and decreased cyclin D1.
In Vivo

CCG-222740 (Oral gavage; 100 mg/kg daily for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice[1].

Animal Model: KC mice (LSL-KrasG12D/+; Pdx-1-Cre) of age at 9 weeks[1]
Dosage: 100 mg/kg
Administration: Oral gavage; daily; for 7 days
Result: Reduced α-SMA levels in the pancreas of caerulein-stimulated KC mice.
Molecular Weight

444.86

Formula

C₂₃H₁₉ClF₂N₂O₃

CAS No.

1922098-69-8

SMILES

O=C(C1CN(C(C2=CC=CC(C3=CC=CO3)=C2)=O)CC(F)(F)C1)NC4=CC=C(Cl)C=C4

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CCG-222740CCG222740CCG 222740RasROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKInhibitorinhibitorinhibit

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CCG-222740
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