Monocarboxylate Transporters
Monocarboxylate transporters (MCTs) constitute a family of proton-linked plasma membrane transporters that carry molecules having one carboxylate group (monocarboxylates), such aslactate and pyruvate, across biological membranes. Highly malignant tumors rely heavily on aerobic glycolysis (metabolism of glucose to lactic acid even under ample tissue oxygen; Warburg Effect) and thus need to efflux lactic acid via MCTs to the tumor micro-environment to maintain a robust glycolytic flux and to prevent the tumor from being "pickled to death". The MCTs have been successfully targeted in pre-clinical studies using RNAi and a small-molecule inhibitor alpha-cyano-4-hydroxycinnamic acid (ACCA; CHC) to show that inhibiting lactic acid efflux is a very effective therapeutic strategy against highly glycolytic malignant tumors.
Products for Monocarboxylate Transporters
- Cat.No. Product Name Information
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GC13691
7ACC1
Coumarin D 1421, 7-DCCA, 7-Diethylamino-2-oxo-2H-chromen-3-carboxylic Acid
MCT inhibitor -
GC14642
7ACC2
MCT inhibitor
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GC50226
AR-C 141990 hydrochloride
MCT1 inhibitor
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GC10680
AR-C155858
An inhibitor of MCT1 and 2
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GC11010
AZD 3965
Ki = 1.6 nM for MCT1
AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1).
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GC68713
AZD0095
AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). When used in combination with Cediranib, AZD0095 effectively inhibits tumor growth of NCI-H358 xenografts.
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GC19488
BAY-8002
BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1)
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GC10877
CHC
CHC, α-CHCA, NSC 173138
CHC (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). -
GC73305
MCT-IN-1
MCT-IN-1 (compound 2) is a potent inhibitor of monocarboxylate transporter (MCT), with the IC50 of 9 nM and 14 nM for MCT1 and MCT4, respectively.
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GC63062
MCT4-IN-1
MCT4-IN-1
MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research. -
GC50163
SR 13800
SR 13800 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. SR 13800 has anti-cancer activity.
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GC63496
VB124
VB124 is an orally active, potent, and selective MCT4 inhibitor.