Home Cell Cycle Rho inhibitor - Actin inhibitor CCG-222740 For research use only.

CCG-222740

CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression.

CCG-222740 Chemical Structure

CCG-222740 Chemical Structure

CAS: 1922098-69-8

Purity & Quality Control

Batch: S667301 DMSO] 89 mg/mL] false] Ethanol] 89 mg/mL] false] Water] Insoluble] false Purity: 99.98%
99.98

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Signaling Pathway

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Biological Activity

Description CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression.
Targets
Rho [1] α-SMA [1]
In vitro
In vitro

CCG-222740 increases the protein levels of p27 and decreased cyclin D1. CCG-222740 treatment decreased cell viability of CAFs, with an IC50 of~10 μM, as measured by the MTT assay. In pancreatic cancer, CAFs are one of the main producers of matrix proteins, including several collagen isoforms. The Rho/MRTF pathway inhibitor CCG-222740 decreases the levels of collagens I, 2a and IV, as well as α-SMA in the CAFsIn cancer cells. CCG-222740 treatment leads to the exclusion of MRTF from the nucleus. [1].
Cell Research Cell lines Cancer associated fibroblasts (CAFs)
Concentrations 10 μM and 20 μM
Incubation Time 72 hours
Method

Murine cancer associated fibroblasts (CAFs) are cultured in DMEM supplemented with 10% fetal bovine serum(FBS). CAFs are treated with several concentrations of CCG-222740 (740) for 72 hours, and levels of Cyclin D1 and p27 are evaluated by western blot.
In Vivo
In vivo

CCG-222740 significantly reduces α-SMA levels in the pancreas of caerulein- stimulated KC mice.[1]
Animal Research Animal Models Nine-week old KC mice
Dosages 100 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 444.86 Formula

C23H19ClF2N2O3
CAS No. 1922098-69-8 SDF --
Smiles C1C(CN(CC1(F)F)C(=O)C2=CC=CC(=C2)C3=CC=CO3)C(=O)NC4=CC=C(C=C4)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 89 mg/mL ( (200.06 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 89 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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