For research use only. Not for therapeutic Use.
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma[1][2].
Ceefourin 1 are highly selective for MRP4 over other ABC transporters, including P-glycoprotein (P-gp), ABCG2 (Breast Cancer Resistance Protein; BCRP) and MRP1 (ABCC1). Ceefourin 1 has limited off-target effects and high stability[1].
Ceefourin 1 (100 nM-100 μM) has low cellular toxicity (IC50>50) in two normal (HSF, MRC5), seven neuroblastoma (BE(2)-C, IMR-32, LAN-1, IMR-32, SK-N-SH, NBL-WN, SHEP) and four other human cancer cell lines (HEPG2, LNCap, SJ-G2, MCF7)[1].
Ceefourin 1 has an IC50 of 2.5 μM in HEK293 cell. Ceefourin 1 blocks D-luciferin efflux with an IC50 of 1.5 μM[1].
| Catalog Number | I011322 |
| CAS Number | 315702-40-0 |
| Synonyms | 3-(1,3-benzothiazol-2-ylsulfanylmethyl)-4-methyl-1H-1,2,4-triazole-5-thione |
| Molecular Formula | C11H10N4S3 |
| Purity | ≥95% |
| InChI | InChI=1S/C11H10N4S3/c1-15-9(13-14-10(15)16)6-17-11-12-7-4-2-3-5-8(7)18-11/h2-5H,6H2,1H3,(H,14,16) |
| InChIKey | KVNBVHCJAUXKPJ-UHFFFAOYSA-N |
| SMILES | CN1C(=NNC1=S)CSC2=NC3=CC=CC=C3S2 |
| Reference | [1]. Leanna Cheung, et al. High-throughput screening identifies Ceefourin 1 and Ceefourin 2 as highly selective inhibitors of multidrug resistance protein 4 (MRP4). Biochem Pharmacol. 2014 Sep 1;91(1):97-108. [2]. Tony Huynh, et al. CCI52 sensitizes tumors to 6-mercaptopurine and inhibits MYCN-amplified tumor growth. Biochem Pharmacol. 2020 Feb;172:113770. |
