For research use only. Not for therapeutic Use.
Corrector C4 is a class II mutation corrector. It acts by rescuing CFTR mutations in nucleotide-binding domain 1 (NBD1) via proteostasis modulation.
| Catalog Number | I011829 |
| CAS Number | 421580-53-2 |
| Synonyms | Corrector C4; Corrector C-4; Corrector C 4; Corr-4a; Corr 4a; Corr4a;;N-(2-((5-chloro-2-methoxyphenyl)amino)-4/’-methyl-[4,5/’-bithiazol]-2/’-yl)benzamide |
| Molecular Formula | C21H17ClN4O2S2 |
| Purity | ≥95% |
| Solubility | Soluble in DMSO |
| Storage | Store at 0-8 °C |
| IUPAC Name | N-[5-[2-(5-chloro-2-methoxyanilino)-1,3-thiazol-4-yl]-4-methyl-1,3-thiazol-2-yl]benzamide |
| InChI | InChI=1S/C21H17ClN4O2S2/c1-12-18(30-21(23-12)26-19(27)13-6-4-3-5-7-13)16-11-29-20(25-16)24-15-10-14(22)8-9-17(15)28-2/h3-11H,1-2H3,(H,24,25)(H,23,26,27) |
| InChIKey | RDOBOPJBMQURAT-UHFFFAOYSA-N |
| SMILES | CC1=C(SC(=N1)NC(=O)C2=CC=CC=C2)C3=CSC(=N3)NC4=C(C=CC(=C4)Cl)OC |
| Reference | </br>1: Dekkers JF, Gogorza Gondra RA, Kruisselbrink E, Vonk AM, Janssens HM, de Winter-de Groot KM, van der Ent CK, Beekman JM. Optimal correction of distinct CFTR folding mutants in rectal cystic fibrosis organoids. Eur Respir J. 2016 Aug;48(2):451-8. doi: 10.1183/13993003.01192-2015. Epub 2016 Apr 21. PubMed PMID: 27103391.</br>2: van der Woerd WL, Wichers CG, Vestergaard AL, Andersen JP, Paulusma CC, Houwen RH, van de Graaf SF. Rescue of defective ATP8B1 trafficking by CFTR correctors as a therapeutic strategy for familial intrahepatic cholestasis. J Hepatol. 2016 Jun;64(6):1339-47. doi: 10.1016/j.jhep.2016.02.001. Epub 2016 Feb 12. PubMed PMID: 26879107.</br>3: Bali V, Lazrak A, Guroji P, Fu L, Matalon S, Bebok Z. A synonymous codon change alters the drug sensitivity of ΔF508 cystic fibrosis transmembrane conductance regulator. FASEB J. 2016 Jan;30(1):201-13. doi: 10.1096/fj.15-273714. Epub 2015 Sep 3. PubMed PMID: 26336913; PubMed Central PMCID: PMC4684529.</br>4: Lopes-Pacheco M, Boinot C, Sabirzhanova I, Morales MM, Guggino WB, Cebotaru L. Combination of Correctors Rescue ΔF508-CFTR by Reducing Its Association with Hsp40 and Hsp27. J Biol Chem. 2015 Oct 16;290(42):25636-45. doi: 10.1074/jbc.M115.671925. Epub 2015 Sep 2. PubMed PMID: 26336106; PubMed Central PMCID: PMC4646207.</br>5: Farinha CM, Sousa M, Canato S, Schmidt A, Uliyakina I, Amaral MD. Increased efficacy of VX-809 in different cellular systems results from an early stabilization effect of F508del-CFTR. Pharmacol Res Perspect. 2015 Aug;3(4):e00152. doi: 10.1002/prp2.152. Epub 2015 Jun 11. PubMed PMID: 26171232; PubMed Central PMCID: PMC4492728.</br>6: Rapino D, Sabirzhanova I, Lopes-Pacheco M, Grover R, Guggino WB, Cebotaru L. Rescue of NBD2 mutants N1303K and S1235R of CFTR by small-molecule correctors and transcomplementation. PLoS One. 2015 Mar 23;10(3):e0119796. doi: 10.1371/journal.pone.0119796. eCollection 2015. PubMed PMID: 25799511; PubMed Central PMCID: PMC4370480.</br>7: Holleran JP, Zeng J, Frizzell RA, Watkins SC. Regulated recycling of mutant CFTR is partially restored by pharmacological treatment. J Cell Sci. 2013 Jun 15;126(Pt 12):2692-703. doi: 10.1242/jcs.120196. Epub 2013 Apr 9. PubMed PMID: 23572510; PubMed Central PMCID: PMC3687701.</br>8: Yu GJ, Yoo CL, Yang B, Lodewyk MW, Meng L, El-Idreesy TT, Fettinger JC, Tantillo DJ, Verkman AS, Kurth MJ. Potent s-cis-locked bithiazole correctors of DeltaF508 cystic fibrosis transmembrane conductance regulator cellular processing for cystic fibrosis therapy. J Med Chem. 2008 Oct 9;51(19):6044-54. doi: 10.1021/jm800533c. Epub 2008 Sep 13. PubMed PMID: 18788728; PubMed Central PMCID: PMC3167067.</br></br> |
