A family of proton-linked plasma membrane transporters known as monocarboxylate transporters (MCTs) carries monocarboxylates, such as lactate and pyruvate, across biological membranes. Highly malignant tumors must efflux lactic acid via MCTs to the tumor micro-environment to maintain a robust glycolytic flux and prevent the tumor from being "pickled to death" because they heavily rely on aerobic glycolysis (metabolism of glucose to lactic acid even under ample tissue oxygen; Warburg Effect). Alpha-cyano-4-hydroxycinnamic acid (ACCA; CHC), a small-molecule inhibitor, and RNA interference (RNAi) were successfully used to target the MCTs in pre-clinical studies to demonstrate how well lac acid efflux inhibition works to treat highly glycolytic malignant tumors.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V2930 | 7ACC2 | 1472624-85-3 | 7ACC2 (7-ACC2), an aminocarboxycoumarin derivative, is a novel and potent MCT (Monocarboxylate transporters) inhibitor with anticancer activity. |
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V74205 | AR-C141990 hydrochloride | 2250019-94-2 | AR-C141990 HCl is a potent inhibitor of monocarboxylate transporters (MCTs), with pKi of 7.6 and 6.6 for MCT-1 and MCT-2 respectively. |
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V74203 | AZD0095 | 2750001-23-9 | AZD0095 is a selective and orally bioactive MCT4 inhibitor (IC50= 1.3 nM). |
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V4197 | AZD3965 | 1448671-31-5 | AZD3965 is a novel, potent and selectiveMCT1 (monocarboxylate transporter 1)inhibitor with aKiof 1.6 nM, it showed 6-fold selectivity over MCT2. |
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V4196 | BAY-8002 | 724440-27-1 | BAY-8002 is a novel, potent, selective, and orally bioactive inhibitor ofmonocarboxylate transporter 1 (MCT1)with anIC50of 85 nM in the MCT1-expressing DLD-1 cells, it displays excellent selectivity against MCT4. |
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V80528 | Lactate transportor 1 | Lactate transportor 1 (compound 1) is the active lactate transporter in living cells. | |
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V74204 | MCT1-IN-3 | 2878360-80-4 | MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor (antagonist) with IC50 of 81.0 nM. |
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V3773 | Valbenazine tosylate | 1639208-54-0 | Valbenazine tosylate (NBI-98854;NBI98854; MT5199; MT-5199;Ingrezza), thetosylate salt of valbenazine,is a VMAT2 (vesicular monoamine transporter 2) inhibitor approved in 2017 by FDAfor the treatment of TD/tardive dyskinesia(uncontrollable movement of the face, tongue, or other body parts). |
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V74202 | VMAT2-IN-2 tosylate | 2608770-12-1 | VMAT2-IN-2 tosylate is a potent VMAT2 inhibitor. |
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