For research use only. Not for therapeutic Use.
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 /> |
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