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A cell-permeable pyrole pyrimidine-based compound that acts as an inhibitor of monocarboxylate transporter 1 (MCT1, SLC16A1) and blocks the proliferation of Raji Burkitt lymphoma (Raji BL) cells expressing MCT1 (EC50 = 5 nM). Also shown to inhibit the growth of MCF-7 breast cancer cells. Effectively increases intracellular lactate levels while reducing lactate export and intracellular ATP levels in Raji cells. However, it does not affect basal oxygen consumption or the mitochondrial mass in these cells. Delays or even eliminates tumor growth in NOD/SCID mice injected with Raji lymphoma cells. Acts synergistically with metformin (Cat. No. 317240) to block monocarboxylate transport and tumor growth in humans and in murine models. Their combined effect also reduces cellular levels of glutathione with concomitant increase in hydrogen peroxide levels, which increases the death of Raji BL cells.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number
509663
Brand Family
Calbiochem®
Synonyms
Monocarboxylate Transport I Inhibitor, SLC16A1 Inhibitor
References
References
Doherty, J., et al. 2014. Cancer Res.73,908. Murray, C., et al. 2013. Nature. Chem. Biol.1, 371.
Doherty, J., et al. 2014. Cancer Res.73,908. Murray, C., et al. 2013. Nature. Chem. Biol.1, 371.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
28-April-2014 JSW
Synonyms
Monocarboxylate Transport I Inhibitor, SLC16A1 Inhibitor
Description
A cell-permeable pyrole pyrimidine-based compound that acts as an inhibitor of monocarboxylate transporter 1 (MCT1, SLC16A1) and blocks the proliferation of Raji Burkitt lymphoma (Raji BL) cells expressing MCT1 (EC50 = 5 nM). Also shown to inhibit the growth of MCF-7 breast cancer cells. Effectively increases intracellular lactate levels while reducing lactate export and intracellular ATP levels in Raji cells. However, it does not affect basal oxygen consumption or the mitochondrial mass in these cells. Delays or even eliminates tumor growth in NOD/SCID mice injected with Raji lymphoma cells. Acts synergistically with metformin (Cat. No. 317240) to block monocarboxylate transport and tumor growth in humans and in murine models. Their combined effect also reduces cellular levels of glutathione with concomitant increase in hydrogen peroxide levels, which increases the death of Raji BL cells.
Form
White powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
227321-12-2
Chemical formula
C₂₅H₂₉N₃O₂S
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Doherty, J., et al. 2014. Cancer Res.73,908. Murray, C., et al. 2013. Nature. Chem. Biol.1, 371.
