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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

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Size/SKUAvailabilityPrice
25 mg
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$221.00

About This Item

Empirical Formula (Hill Notation):
C17H12O3
CAS Number:
Molecular Weight:
264.28
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light

$221.00


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assay

≥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.

Biochem/physiol Actions

Reversible: yes
Cell permeable: yes
Primary Target
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)

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This Item
509663531170538759
description

-

description

-

description

-

description

-

form

solid

form

powder

form

powder

form

solid

assay

≥97% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥97% (HPLC)

Quality Level

100

Quality Level

200

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

solubility

DMSO: 5 mg/mL

solubility

DMSO: 100 mg/mL

solubility

DMSO: 50 mg/mL

solubility

DMSO: 50 mg/mL


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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