315702-40-0

315702-40-0 structure

Name: Ceefourin 1
Chemical Name: 5-(Benzothiazol-2-ylsulfanylmethyl)-4-methyl-4H-[1,2,4]triazole-3-thiol
CAS Number: 315702-40-0
Molecular Formula: C₁₁H₁₀N₄S₃
Molecular Weight: 294.419
Catalog: Signaling Pathways Others Others
Create Date: 2018-07-09 23:17:57
Modify Date: 2025-08-25 21:12:57
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].

Name	5-(Benzothiazol-2-ylsulfanylmethyl)-4-methyl-4H-[1,2,4]triazole-3-thiol
Synonyms	MFCD03984494 3H-1,2,4-Triazole-3-thione, 5-[(2-benzothiazolylthio)methyl]-2,4-dihydro-4-methyl- 5-(Benzothiazol-2-ylsulfanylmethyl)-4-methyl-4H-[1,2,4]triazole-3-thiol 5-[(1,3-Benzothiazol-2-ylsulfanyl)methyl]-4-methyl-2,4-dihydro-3H-1,2,4-triazole-3-thione

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Others
Target	MRP4[1]
In Vitro	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].
References	[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.