5.38098

GDH1 Inhibitor, R162

• Synonym(s): GDH1 Inhibitor, R162, 2-Allyl-1-hydroxy-9,10-anthraquinone, Glutamate Dehydrogenase 1 Inhibitor, GDH1 Inhibitor, GLUD1 Inhibitor
• Empirical Formula (Hill Notation): C₁₇H₁₂O₃
• CAS Number: 64302-87-0
• Molecular Weight: 264.28
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥97% (HPLC)
• Quality Level: 100
• form: solid
• potency: 23 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 5 mg/mL
• storage temp.: 2-8°C

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
GDH1

Reversible: yes

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

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable