R162 Chemical Properties

Melting point:

120-120.5 °C(Solv: acetone (67-64-1))

Boiling point:

459.0±34.0 °C(Predicted)

Density 

1.308±0.06 g/cm3(Predicted)

storage temp. 

-20°C

solubility 

Soluble in DMSO (up to 10 mg/ml or in Ethanol (up to 5 mg/ml)

form 

solid

pka

7.43±0.20(Predicted)

color 

Orange

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

R162 Usage And Synthesis

Description

R162 (64302-87-0) is a selective inhibitor of glutamate dehydrogenase 1 (GDH1), a commonly upregulated enzyme in human cancers (Ki?= 28.6 μM).? It does not inhibit the activity of other NADPH enzymes such as 6-phosphogluconate dehydrogenase and fumarate hydratase. R162 treatment leads to decreased fumarate levels, lower glutathione peroxidase activity, increased ROS levels and reduced cell proliferation in H1299 and MDA-MB231 cells.? R162 sensitizes LKB-1 deficient tumor cells to anoikis induction.? R162 treatment (at 20 mg/kg/day) significantly attenuates metastatic potential in a xenograft mouse model.2? GDH1 is a promising antimetastasis target and R162 is a useful tool for proof of principal studies.

Uses

R162 is a glutamate dehydrogenase 1 inhibitor for the treatment of cancer. A useful bioactive chemical compound.

Definition

ChEBI: 2-allyl-1-hydroxy-9,10-anthraquinone is a monohydroxyanthraquinone that is 9,10-anthraquinone in which the hydrogens at positions 1 and 2 are replaced by a hydroxy and an allyl group, respectively. It has a role as an EC 1.4.1.3 {glutamate dehydrogenase [NAD(P)(+)]} inhibitor.

in vivo

References

[1] LINGTAO JIN. Glutamate dehydrogenase 1 signals through antioxidant glutathione peroxidase 1 to regulate redox homeostasis and tumor growth.[J]. Cancer Cell, 2015, 27 2: 257-270. DOI:10.1016/j.ccell.2014.12.006
[2] LINGTAO JIN. The PLAG1-GDH1 Axis Promotes Anoikis Resistance and Tumor Metastasis through CamKK2-AMPK Signaling in LKB1-Deficient Lung Cancer.[J]. Molecular Cell, 2018, 69 1: 87-99.e7. DOI:10.1016/j.molcel.2017.11.025

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