Ceefourin 1_product_DataBase

Bioactivity

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].

Target

MRP4

Invitro

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].

Name

Ceefourin 1

CAS

315702-40-0

Formula

C11H10N4S3

Molar Mass

294.42

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

Ceefourin 1

CAS: 315702-40-0 F: C11H10N4S3 W: 294.42