5.09663

MCT1 Inhibitor, SR13800

• 동의어(들): MCT1 Inhibitor, SR13800, Monocarboxylate Transport I Inhibitor, SLC16A1 Inhibitor
• 실험식(Hill 표기법): C₂₅H₂₉N₃O₂S
• CAS Number: 227321-12-2
• Molecular Weight: 435.58
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 200
• 형태: powder
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 100 mg/mL
• 저장 온도: 2-8°C

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
MCT1

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable