5.38098

GDH1 Inhibitor, R162

• Sinónimos: GDH1 Inhibitor, R162, 2-Allyl-1-hydroxy-9,10-anthraquinone, Glutamate Dehydrogenase 1 Inhibitor, GDH1 Inhibitor, GLUD1 Inhibitor
• Fórmula empírica (notación de Hill): C₁₇H₁₂O₃
• Número de CAS: 64302-87-0
• Peso molecular: 264.28
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Análisis: ≥97% (HPLC)
• Nivel de calidad: 100
• formulario: solid
• potencia: 23 μM IC₅₀
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: yellow
• solubilidad: DMSO: 5 mg/mL
• temp. de almacenamiento: 2-8°C

Descripción

Descripción general

A cell-permeable, bioavailable, non-toxic purpurin analog that directly binds to GDH1 (Glutamate dehydrogenase 1; K_d = 30 µM) and inhibits its activity in a mixed mode manner (IC₅₀ = 23 µM). Displays selectivity over other NADPH-dependent enzymes such as 6-phosphogluconate dehydrogenase (6PGD) and fumarate hydratase (FH). Show to appreciably decrease intracellular fumarate levels, lessen glutathione peroxidase (GPx) activity and elevate mitochondrial ROS levels. Preferentially arrests cancer cell proliferation of H1299, MDA-MB231 and primary leukemia cells over nonmalignant, proliferating human cells. Significantly decreases tumor growth and masses in H1299-xenograft tumor mouse models (30 mg/kg, i.p., q.d.).

A cell-permeable, bioavailable, non-toxic purpurin analog that directly binds to GDH1 (Glutamate dehydrogenase 1; K_d = 30 µM) and inhibits its activity in a mixed mode manner (IC₅₀ = 23 µM). Displays selectivity over other NADPH-dependent enzymes such as 6-phosphogluconate dehydrogenase (6PGD) and fumarate hydratase (FH). Show to appreciably decrease intracellular fumarate levels, lessen glutathione peroxidase (GPx) activity and elevate mitochondrial ROS levels. Preferentially arrests cancer cell proliferation of H1299, MDA-MB231 and primary leukemia cells over nonmalignant, proliferating human cells. Significantly decreases tumor growth and masses in H1299-xenograft tumor mouse models (30 mg/kg, i.p., q.d.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
GDH1

Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

Jin, L., et al. 2015. Cancer Cell.27, 257.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable