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AB145144

Ceefourin™ 1, MRP4 inhibitor

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(2 Publications)

MW 294.4 Da, Purity >99%. Highly selective multidrug resistance protein 4 (MRP4) inhibitor (IC50 = 1.5 µM). Blocked transport of MRP4 substrates 6-Mercaptopurine, SN 38, cAMP, D-Luciferin and E217βG. No detectable effect on MRP4 homologs MRP1, 2, 3 or 5, and related transporters P-gp and ABCG2 *in vitro*. Low cellular toxicity, and high microsomal and acid stability. Chemically distinctive to Ceefourin™ 2 (ab145145).

View Alternative Names

ABCC 4, ATP binding cassette sub family C (CFTR/MRP) member 4, ATP-binding cassette sub-family C member 4, Canalicular multispecific organic anion transporter, Canalicular multispecific organic anion transporter ABC superfamily, EST170205, MOAT-B, MRP/cMOAT-related ABC transporter, MRP4_HUMAN, Multi-specific organic anion transporter B, Multidrug resistance-associated protein 4, OTTHUMP00000018560, bA464I2.1, bA464I2.1 (ATP binding cassette, sub-family C (CFTR/MRP) member 4)

1 Images
Chemical Structure - Ceefourin™ 1, MRP4 inhibitor (AB145144)
  • Chemical Structure

Lab

Chemical Structure - Ceefourin™ 1, MRP4 inhibitor (AB145144)

2D chemical structure image of ab145144, Ceefourin™ 1, MRP4 inhibitor

Key facts

CAS number

315702-40-0

Purity

>99%

Form

Solid

form

Molecular weight

294.4 Da

Molecular formula

C<sub>1</sub><sub>1</sub>H<sub>1</sub><sub>0</sub>N<sub>4</sub>S<sub>3</sub>

PubChem

704306

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Biochemical name

5-[(1,3-benzothiazol-2-ylsulfanyl)methyl]-4-methyl-4H-1,2,4-triazole-3-thiol

Biological description

Highly selective multidrug resistance protein 4 (MRP4) inhibitor (IC50 = 1.5 µM). Blocked transport of MRP4 substrates 6-Mercaptopurine, SN 38, cAMP, D-Luciferin and E217βG. No detectable effect on MRP4 homologs MRP1, 2, 3 or 5, and related transporters P-gp and ABCG2 *in vitro*. Low cellular toxicity, and high microsomal and acid stability. Chemically distinctive to Ceefourin™ 2 (ab145145).

Canonical smiles

CN1C(=NNC1=S)CSC2=NC3=CC=CC=C3S2

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

IUPAC Name

3-(1,3-benzothiazol-2-ylsulfanylmethyl)-4-methyl-1H-1,2,4-triazole-5-thione

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Complementary Products

Biochemicals

AB145145

Ceefourin™ 2, MRP4 inhibitor

Chemical Structure - Ceefourin™ 2, MRP4 inhibitor (AB145145)

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Biochemicals

AB209693

Erastin, ferroptosis activator

Chemical Structure - Erastin, ferroptosis activator (AB209693)

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Assay Kits

AB211094

Adenosine Assay Kit (Fluorometric)

Functional Studies - Adenosine Assay Kit (Fluorometric) (AB211094)

  • 4
  • 3
Assay Kits

AB112155

Pyrophosphate Assay Kit (Fluorometric)

Functional Studies - Pyrophosphate Assay Kit (Fluorometric) (AB112155)

  • 4
  • 2
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Product details

Sold under exclusive licence from Children's Cancer Institute. Ceefourin™ is a trademark of Children's Cancer Institute.
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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months
Handling instructions

Need more advice on solubility, usage and handling? Please visit our our product support page for more details.

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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The MRP4 protein also known as Multidrug Resistance Protein 4 or ABCC4 is an ATP-binding cassette transporter with a mass of approximately 150 kDa. This protein is expressed in various tissues including the liver kidney and brain. It plays a mechanical role by transporting organic anions drugs and other xenobiotic compounds across cellular membranes. MRP4 is part of the wider ATP-binding cassette (ABC) transporter family which actively pumps substrates against concentration gradients using ATP hydrolysis.
Biological function summary

MRP4 impacts processes like pharmacokinetics and drug metabolism. The protein contributes to the efflux of endogenous substrates and medication from cells affecting their absorption and excretion. MRP4 also functions as part of a larger transporter complex working with other similar proteins to manage cellular detoxification systems. The MRP4 transporter maintains cellular homeostasis by removing harmful substances supporting cellular defense mechanisms against xenobiotic and endogenous compounds.

Pathways

MRP4 integrates into cellular processes such as prostaglandin and cyclic nucleotide signaling pathways. These pathways are important in regulating inflammatory responses and cardiovascular functions. MRP4 interacts with other proteins including MRP1 and MRP5 which facilitate the movement of similar substrates providing flexibility and redundancy within cellular transport systems. This involvement enables MRP4 to modulate biological effects via alteration in prostaglandin levels.

MRP4 connects to conditions such as cancer and viral infections. Elevated expression of MRP4 can lead to drug resistance in cancer therapy complicating treatment strategies. In viral infections MRP4 modulates the availability of nucleoside analogs used in antiviral therapies. The protein's role aligns with other transporters like P-glycoprotein showcasing its involvement in the multidrug resistance phenotype. Consequently understanding MRP4's function can aid in the development of new therapeutic approaches targeting these disorders.
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Product protocols

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Publications (2)

Recent publications for all applications. Explore the full list and refine your search

Medicina (Kaunas, Lithuania) 58: PubMed35743958

2022

Specific MRP4 Inhibitor Ceefourin-1 Enhances Apoptosis Induced by 6-Mercaptopurine in Jurkat Leukemic Cells, but Not in Normal Lymphoblast Cell Line CRL-1991.

Applications

Unspecified application

Species

Unspecified reactive species

Edgardo Becerra,Laura Berumen,Valeria Soto-Ontiveros,Guadalupe García-Alcocer

Scientific reports 7:12390 PubMed28959040

2017

Endoplasmic reticulum stress preconditioning modifies intracellular mercury content by upregulating membrane transporters.

Applications

Unspecified application

Species

Unspecified reactive species

Fusako Usuki,Masatake Fujimura,Akio Yamashita
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Product promise

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