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538098 GDH1 Inhibitor, R162 - CAS 64302-87-0 - Calbiochem

Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
64302-87-0C₁₇H₁₂O₃

Products

Catalog NumberPackaging Qty/Pack
5.38098.0001 Glass bottle 25 mg
Description
OverviewA 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.
Catalogue Number538098
Brand Family Calbiochem®
Synonyms2-Allyl-1-hydroxy-9,10-anthraquinone, Glutamate Dehydrogenase 1 Inhibitor, GDH1 Inhibitor, GLUD1 Inhibitor
DescriptionGDH1 Inhibitor, R162
References
ReferencesJin, L., et al. 2015. Cancer Cell. 27, 257.
Product Information
CAS number64302-87-0
FormYellow solid
Hill FormulaC₁₇H₁₂O₃
Chemical formulaC₁₇H₁₂O₃
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetGDH1
Primary Target IC<sub>50</sub>23 µ
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.38098.0001 04054839059292

Documentation

GDH1 Inhibitor, R162 - CAS 64302-87-0 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Jin, L., et al. 2015. Cancer Cell. 27, 257.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision22-January-2020 JSW
Synonyms2-Allyl-1-hydroxy-9,10-anthraquinone, Glutamate Dehydrogenase 1 Inhibitor, GDH1 Inhibitor, GLUD1 Inhibitor
DescriptionA 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.).
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number64302-87-0
Chemical formulaC₁₇H₁₂O₃
Purity≥97% by HPLC
SolubilityDMSO (5 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesJin, L., et al. 2015. Cancer Cell. 27, 257.