α-CHCA is a classic monocarboxylate transporters (MCT) inhibitor. In the sensitive U251 cells, CHCA is able to inhibit cell proliferation and induce cell death, having a cytotoxic effect; however, in the less sensitive SW1088 cells, CHCA only inhibits cell proliferation but did not induce cell death. Transport by MCT1, 2, and 4 is competitively inhibited by CHCA whereas transport by MCT3 is insensitive to α-cyano-4-hydroxy-cinnamic acid.
| Molecular Weight | 189.17 |
| Formula | C10H7NO3 |
| CAS Number | 28166-41-8 |
| Solubility (25°C) | DMSO: ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Monocarboxylate Transporter (MCT) Products |
|---|
| 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. |
| MSC-4381
MSC-4381 (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. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research. |
| MCT1-IN-2
MCT1-IN-2 is a potent monocarboxylate transporter 1 (MCT1) inhibitor. MCT1-IN-2 has anti-cancer activity. |
| VB124
VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism. |
| 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. |
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