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lactate transport inhibitor Contrary 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.
| Molecular Weight | 261.27 |
| Formula | C14H15NO4 |
| CAS Number | 50995-74-9 |
| Solubility (25°C) | DMSO 27 mg/mL |
| Storage | 2-8°C, protect from light, sealed |
| Related Monocarboxylate Transporter (MCT) Products |
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| Silicristin
Silychristin is a flavonoid rich in milk thistle fruits, which has antioxidant effects. Silychristin is an effective inhibitor of thyroid hormone transporter MCT8 and can strongly inhibit T3 uptake with IC50 of 110 nM. |
| AZD3965
AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with a binding affinity of 1.6 nM. |
| 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). |
| α-cyano-4-hydroxy-cinnamic acid
α-Cyano-4-hydroxycinnamic acid (α-CHCA) 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. |
| UK-5099
UK-5099 (PF-1005023) is a potent inhibitor of the mitochondrial pyruvate carrier (MPC), it inhibits pyruvate-dependent O2 consumption with an IC50 of 50 nM. UK-5099 is also a cuproptosis inhibitor. |
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