- R162
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- $40.00
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2026-06-02
- CAS:64302-87-0
- Purity: 98.15%
- Supply Ability: 10g
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| Product Name: | R162 | | Synonyms: | R162;R-162;R 162;R162, >98%;2-Allyl-1-hydroxy-9,10-anthraquinone;9,10-Anthracenedione, 1-hydroxy-2-(2-propen-1-yl)-;R162,inhibit,R-162,Inhibitor,R 162;9,10-Anthracenedione, 1-hydroxy-2-(2-propenyl)-;R162, 10 mM in DMSO;2-ALLYL-1-HYDROXY-ANTHRAQUINONE | | CAS: | 64302-87-0 | | MF: | C17H12O3 | | MW: | 264.28 | | EINECS: | | | Product Categories: | | | Mol File: | 64302-87-0.mol |  |
| 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. |
| 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 | R162 (30 mg/kg/day, i.p.) does not result in a significant histopathological change between the vehicle-treated and R162-treated groups, nor alters complete blood counts, or hematopoietic properties in xenograft tumor mouse models. R162 (20 mg/kg/day) results in significantly decreased tumor growth and masses in mice compared with control mice and effectively inhibits GDH1 activity in resected tumors from xenograft nude mice[1]. | | 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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