Sigma-Aldrich Monocarboxylate Transport

Assay

≥95% (HPLC)

Quality Level

100

Form

solid

Potency

1.2 nM K_i

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

brown

Solubility

DMSO: 50 mg/mL

Storage Temp.

−20°C

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

General Description

A cell-permeable thieno[2,3-d]pyrimidinedione compound that acts as a highly potent inhibitor of monocarboxylate transporter 1 (MCT1; K_i= 2.3 nM for lactate uptake in rat erythrocytes). Also shown to inhibit MCT2 when associated with basigin (IC₅₀= 10 nM). Does not affect the activity of MCT4 even at higher concentration. Also shown to block MCT1 expressed in Xenopus oocytes Binds to MCT1 from the intracellular side involving transmembrane helices 7-10. Its inhibitory effect is significantly reduced with either F360Y or S364G mutations (~100 nM) and the inhibitory effect is lost with both sites are mutated (~5 µM). Displays high metabolic stability and low inhibition of CYP. Shown to block lactate transport and increase intracellular lactate levels in Raji Burkitt and MCF-7 cells and reduces their proliferation.A cell-permeable thieno[2,3-d]pyrimidinedione compound that acts as a highly potent inhibitor of monocarboxylate transporter 1 (MCT1; K_i= 2.3 nM for lactate uptake in rat erythrocytes). Also shown to inhibit MCT2 when associated with basigin (IC₅₀= 10 nM). Does not affect the activity of MCT4 even at higher concentration. Also shown to block MCT1 expressed in Xenopus oocytes Binds to MCT1 from the intracellular side involving transmembrane helices 7-10. Its inhibitory effect is significantly reduced with either F360Y or S364G mutations (~100 nM) and the inhibitory effect is lost with both sites are mutated (~5 µM). Displays high metabolic stability and low inhibition of CYP. Shown to block lactate transport and increase intracellular lactate levels in Raji Burkitt and MCF-7 cells and reduces their proliferation.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.Monocarboxylate Transport Inhibitor, AR-C155858, CAS 496791-37-8, is a cell-permeable, potent inhibitor of monocarboxylate transporter 1 (MCT1; K_i= 2.3 nM for lactate uptake in rat erythrocytes).

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
MCT1

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Nancolas, B., et Al. 2015.Biochem. J. 467,192.
Ovens, M. J. et Al. 2010.Biochem. J. 425,523.
Guile, S. D., et Al. 2007.J. Med. Chem. 50,254.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany