5.09663

MCT1 Inhibitor, SR13800

• Synonym(s): MCT1 Inhibitor, SR13800, Monocarboxylate Transport I Inhibitor, SLC16A1 Inhibitor
• Empirical Formula (Hill Notation): C₂₅H₂₉N₃O₂S
• CAS Number: 227321-12-2
• Molecular Weight: 435.58
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥98% (HPLC)
• Quality Level: 200
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Description

General 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.

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MCT1

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Doherty, J., et al. 2014. Cancer Res.73,908.
Murray, C., et al. 2013. Nature. Chem. Biol.1, 371.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable