AR-C155858

For research use only. Not for therapeutic Use.

  • CAT Number: I003741
  • CAS Number: 496791-37-8
  • Molecular Formula: C21H27N5O5S
  • Molecular Weight: 461.54
  • Purity: ≥95%
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AR-C155858 (Cat No.: I003741)is a potent and selective inhibitor of solute carrier family 16 member 1 (SLC16A1, also known as MCT1), with an IC₅₀ of 2.3 nM. It effectively blocks lactate transport, making it valuable for cancer metabolism research, particularly in targeting glycolytic tumors that rely on lactate shuttling. AR-C155858 also inhibits MCT2 but with lower potency. It has been widely used to study metabolic pathways, tumor microenvironments, and cellular energy regulation, providing insights into therapeutic strategies for cancer and metabolic diseases.


CAS Number 496791-37-8
Synonyms

6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[(4S)-4-hydroxy-1,2-oxazolidine-2-carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione

Molecular Formula C21H27N5O5S
Purity ≥95%
Target Monocarboxylate Transporter
Solubility in DMSO > 10 mM
Storage Store at -20°C
IC50 2.3/<10 nM (Ki, MCT1/2)
IUPAC Name 6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[(4S)-4-hydroxy-1,2-oxazolidine-2-carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione
InChI InChI=1S/C21H27N5O5S/c1-10(2)7-25-20-17(18(28)24(5)21(25)30)16(19(29)26-8-13(27)9-31-26)15(32-20)6-14-11(3)22-23-12(14)4/h10,13,27H,6-9H2,1-5H3,(H,22,23)/t13-/m0/s1
InChIKey ISIVOJWVBJIOFM-ZDUSSCGKSA-N
SMILES CC1=C(C(=NN1)C)CC2=C(C3=C(S2)N(C(=O)N(C3=O)C)CC(C)C)C(=O)N4CC(CO4)O
Reference

1:Identification of key binding site residues of MCT1 for AR-C155858 reveals the molecular basis of its isoform selectivity. Nancolas B, Sessions RB, Halestrap AP.Biochem J. 2015 Apr 1;467(1):192. No abstract available. PMID: 25793420 <br />
2:Identification of key binding site residues of MCT1 for AR-C155858 reveals the molecular basis of its isoform selectivity. Nancolas B, Sessions RB, Halestrap AP.Biochem J. 2015 Feb 15;466(1):177-88. doi: 10.1042/BJ20141223. Erratum in: Biochem J. 2015 Apr 1;467(1):192. PMID: 25437897 Free PMC Article<br />
3:The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Ovens MJ, Manoharan C, Wilson MC, Murray CM, Halestrap AP.Biochem J. 2010 Oct 15;431(2):217-25. doi: 10.1042/BJ20100890. PMID: 20695846 Free PMC Article<br />
4:AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Ovens MJ, Davies AJ, Wilson MC, Murray CM, Halestrap AP.Biochem J. 2010 Jan 15;425(3):523-30. doi: 10.1042/BJ20091515. PMID: 19929853 Free PMC Article

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