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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Monocarboxylate transporters (MCTs) in gliomas: expression and exploitation as therapeutic targets.
Miranda-Goncalves V, et al. Neuro Oncol. 2013 Feb;15(2):172-88. PMID: 23258846.
Targeting lactate-fueled respiration selectively kills hypoxic tumor cells in mice.
Sonveaux P, et al. J Clin Invest. 2008 Dec;118(12):3930-42. PMID: 19033663.
S107 is a Type 1 ryanodine receptor (RyR1) stabilizer.
3,3’,5,5’-Tetramethylbenzidine(TMB) is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualising reagent used in enzyme-linked immunosorbent assays (ELISA).
Coelenterazine is the luciferin, the light-emitting molecule, used for monitoring reporter genes in BRET, ELISA and HTS techniques.
Fluorescein is a synthetic organic compound and dye.
SBI-0640756 is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.
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