α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamic acid(α-CHCA)) (α-CHCA) is an inhibitor of monocarboxylate transporter 1 (MCT1) that blocks pyruvate transport in rat heart mitochondria (IC50 : 1.5 μM).

CHC在胶质瘤细胞中的有效性似乎依赖于单羧酸转运蛋白(MCTs)的膜表达。MCT1的下调在不同的胶质瘤细胞中显示了类似的效果，这支持了CHC作为MCT1抑制剂的观点。当CHC与替莫唑胺治疗结合使用时，在U251细胞中观察到了协同效应。在CAM体内模型中，CHC减小了肿瘤的大小和形成的血管数量[1]。

Cells were plated into 96-well plates, at a density of 3 × 10^3 cells per well.?The effect of treatment with CHC (0.6–12 mM) on cell number (total biomass) was determined at 24, 48, and 72 h by the?sulforhodamine B assay (SRB, TOX-6).?IC50 values (CHC concentration that corresponds to 50% of cell growth inhibition) were estimated from 3 independent experiments, each one in triplicate, using GraphPad Software.?Cell proliferation assay was performed as previously described32 and assessed under the treatment conditions previously described, for 5 mM and 10 mM of CHC.?After CHC treatment, cells were incubated with BrdU and its incorporation was assessed at 450 nm (λref = 655 nm) .?Cell growth (total biomass) and cell proliferation for glioma siMCT1 cells and the effect of CHC (1.25–15 mM) on cell number were performed[1].