Name | CCG-222740 |
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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]. |
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Related Catalog | |
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. |
References |
Molecular Formula | C23H19ClF2N2O3 |
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Molecular Weight | 444.86 |
Storage condition | -20°C |