Ceefourin 1

Names

[ Name ]:
Ceefourin 1

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Boiling Point ]:
422.1±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₁H₁₀N₄S₃

[ Molecular Weight ]:
294.419

[ Flash Point ]:
209.1±31.5 °C

[ Exact Mass ]:
294.006744

[ LogP ]:
1.85

[ Vapour Pressure ]:
0.0±1.0 mmHg at 25°C

[ Index of Refraction ]:
1.827

Related Compounds

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