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.


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AZD0095

AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205)[1].

  • CAS Number: 2750001-23-9
  • MF: C27H32N8O2
  • MW: 500.60
  • Catalog: Monocarboxylate Transporter
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

α-Cyano-4-hydroxycinnamic acid

α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications[1][2].

  • CAS Number: 28166-41-8
  • MF: C10H7NO3
  • MW: 189.167
  • Catalog: Monocarboxylate Transporter
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 398.1±32.0 °C at 760 mmHg
  • Melting Point: 245-250 °C(lit.)
  • Flash Point: 194.5±25.1 °C

MCT1-IN-3

MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor with an IC50 value of 81.0 nM. MCT1-IN-3 has also significant inhibitivity against the multidrug transporter ABCB1. MCT1-IN-3 can be used for the research of cancer[1].

  • CAS Number: 2878360-80-4
  • MF: C22H19N3O4
  • MW: 389.40
  • Catalog: Monocarboxylate Transporter
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

UK-5099

UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 ihibits pyruvate-dependent O2 consumption with an IC50 of 50 nM.

  • CAS Number: 56396-35-1
  • MF: C18H12N2O2
  • MW: 288.300
  • Catalog: Monocarboxylate Transporter
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 448.6±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 225.1±28.7 °C

BAY 8002

BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity[1].

  • CAS Number: 724440-27-1
  • MF: C20H14ClNO5S
  • MW: 415.85
  • Catalog: Monocarboxylate Transporter
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7-Diethylaminocoumarin-3-carboxylic acid

7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.IC50 value: 0.86 uM(Lactate uptake inhibition) [1]Target: MCT inhibitor; lactate transport inhibitorContrary to the reference MCT1 inhibitor AR-C155858, 7ACC unexpectedly inhibited lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters. 7ACC delayed the growth of cervix SiHa tumors, colorectal HCT116 tumors, and orthoptopic MCF-7 breast tumors. MCT target engagement was confirmed by the lack of activity of 7ACC on bladder UM-UC-3 carcinoma that does not express functional MCT. 7ACC also inhibited SiHa tumor relapse after treatment with cisplatin. Finally, we found that contrary to AR-C155858, 7ACC did not prevent the cell entry of the substrate-mimetic drug 3-bromopyruvate (3BP) through MCT1, and contributed to the inhibition of tumor relapse after 3BP treatment.

  • CAS Number: 50995-74-9
  • MF: C14H15NO4
  • MW: 261.273
  • Catalog: Monocarboxylate Transporter
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 464.7±45.0 °C at 760 mmHg
  • Melting Point: 222-224ºC (dec.)(lit.)
  • Flash Point: 234.9±28.7 °C

SR 13800

MCT1-IN-2 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. MCT1-IN-2 has anti-cancer activity[1][2].

  • CAS Number: 227321-12-2
  • MF: C25H29N3O2S
  • MW: 435.58
  • Catalog: Monocarboxylate Transporter
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AR-C155858

AR-C155858 is a selective monocarboxylate transporter MCT1 and MCT2 inhibitor with Kis of 2.3 nM and 10 nM, respectively.

  • CAS Number: 496791-37-8
  • MF: C21H27N5O5S
  • MW: 461.535
  • Catalog: Monocarboxylate Transporter
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 763.1±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 415.3±35.7 °C

AZD3965

AZD3965 is a selective MCT1 inhibitor with a Ki of 1.6 nM, showing 6-fold selectivity over MCT2.

  • CAS Number: 1448671-31-5
  • MF: C21H24F3N5O5S
  • MW: 515.506
  • Catalog: Monocarboxylate Transporter
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 723.1±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 391.1±35.7 °C

7ACC2

7ACC2 is a new potent MCT inhibitor with IC50 of 11 nM for inhibition of [14C]-lactate influx; new antitumor treatment targeting lactate transport in cancer cells.IC50 value: 11 nM ([14C]-lactate influx) [1]Target: MCT inhibitor; lactate transport inhibitor7ACC2 did not influence the prothrombin time which, together with a good in vitro ADME profile, supports the potential of this new family of compounds to act as anticancer drugs through inhibition of lactate flux.

  • CAS Number: 1472624-85-3
  • MF: C18H15NO4
  • MW: 309.316
  • Catalog: Monocarboxylate Transporter
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 548.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 285.8±30.1 °C

AR-C141990 hydrochloride

AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively[1]. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response[2].

  • CAS Number: 2250019-94-2
  • MF: C26H29ClN4O4S
  • MW: 529.05
  • Catalog: Monocarboxylate Transporter
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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[1].

  • CAS Number: 2445185-57-7
  • MF: C26H20ClN3O6S
  • MW: 537.97
  • Catalog: Monocarboxylate Transporter
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VB124

VB124 is a potent and selective MCT4 inhibitor. VB124 might redirect glycolytic carbon flux into mitochondrial pyruvate oxidation. VB124 bolcks lactate import (IC50=8.6nM), and export (IC50=19nM) in MDA-MB-231 cells that are engineers to express MCT4 as the only major plasma membrane lactate transporter.

  • CAS Number: 2230186-18-0
  • MF: C23H23ClN2O4
  • MW: 426.89
  • Catalog: Monocarboxylate Transporter
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A