CCG-222740 is a potent MRTF/SRF inhibitor. CCG-222740 markedly decreased SRF reporter gene activity and showed a greater inhibitory effect on MRTF/SRF target genes than the previously described MRTF-A inhibitor CCG-203971. CCG-222740 was also five times more potent, with an IC50 of 5 μM, in a fibroblast-mediated collagen contraction assay, was less cytotoxic, and a more potent inhibitor of alpha-smooth muscle actin protein expression than CCG-203971.
Chemical Formula: C23H19ClF2N2O3
Exact Mass: 444.1052
Molecular Weight: 444.8628
Elemental Analysis: C, 62.10; H, 4.31; Cl, 7.97; F, 8.54; N, 6.30; O, 10.79
Chemical Name: N-(4-chlorophenyl)-5,5-difluoro-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide
InChi Code: InChI=1S/C23H19ClF2N2O3/c24-18-6-8-19(9-7-18)27-21(29)17-12-23(25,26)14-28(13-17)22(30)16-4-1-3-15(11-16)20-5-2-10-31-20/h1-11,17H,12-14H2,(H,27,29)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
CCG-222740 (10, 20 μM; for 72 hours) increases the protein levels of p27 and decreases cyclin D1. CCG-222740 decreases cell viability of CAFs, with an IC50 of ~10 μM.
CCG-222740 (10, 25 μM) is potent at decreasing αSMA protein expression in human conjunctival fibroblasts.
CCG-222740 has an IC50 of 5 μM in a fibroblast-mediated collagen contraction assay, and it is less cytotoxic.
CCG-222740 (oral gavage; 100 mg/kg/day for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice.
- Tagalakis AD, Madaan S, Larsen SD, Neubig RR, Khaw PT, Rodrigues I, Goyal S,Lim KS, Yu-Wai-Man C. In vitro and in vivo delivery of a sustained releasenanocarrier-based formulation of an MRTF/SRF inhibitor in conjunctival fibrosis.J Nanobiotechnology. 2018 Nov 27;16(1):97. doi: 10.1186/s12951-018-0425-3. PubMed PMID: 30482196; PubMed Central PMCID: PMC6258153.
- Yu-Wai-Man C, Spencer-Dene B, Lee RMH, Hutchings K, Lisabeth EM, Treisman R, Bailly M, Larsen SD, Neubig RR, Khaw PT. Local delivery of novel MRTF/SRFinhibitors prevents scar tissue formation in a preclinical model of fibrosis. SciRep. 2017 Mar 31;7(1):518. doi: 10.1038/s41598-017-00212-w. PubMed PMID:28364121; PubMed Central PMCID: PMC5428058.
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