5.38098
GDH1 Inhibitor, R162
Sinónimos:
GDH1 Inhibitor, R162, 2-Allyl-1-hydroxy-9,10-anthraquinone, Glutamate Dehydrogenase 1 Inhibitor, GDH1 Inhibitor, GLUD1 Inhibitor
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Fórmula empírica (notación de Hill):
C17H12O3
Número CAS:
Peso molecular:
264.28
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Servicio técnico
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Permítanos ayudarleassay
≥97% (HPLC)
Quality Segment
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
SMILES string
Oc1c2c(ccc1CC=C)C(=O)c3c(cccc3)C2=O
InChI
1S/C17H12O3/c1-2-5-10-8-9-13-14(15(10)18)17(20)12-7-4-3-6-11(12)16(13)19/h2-4,6-9,18H,1,5H2
InChI key
IMUBGIOLZQTIGI-UHFFFAOYSA-N
General description
A cell-permeable, bioavailable, non-toxic purpurin analog that directly binds to GDH1 (Glutamate dehydrogenase 1; Kd = 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.
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
Reversible: yes
Cell permeable: yes
Primary Target
GDH1
GDH1
Packaging
Packaged under inert gas
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificados de análisis (COA)
Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»
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