R162


Catalog No. Size PriceQuantity
M27162-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.

Product information

CAS Number: 64302-87-0

Molecular Weight: 264.28

Formula: C17H12O3

Chemical Name: 1-hydroxy-2-(prop-2-en-1-yl)-9,10-dihydroanthracene-9,10-dione

Smiles: C=CCC1=CC=C2C(=C1O)C(=O)C1=CC=CC=C1C2=O

InChiKey: IMUBGIOLZQTIGI-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 5.2 mg/mL (19.68 mM; Need ultrasonic). H2O : < 0.1 mg/mL (ultrasonic) (insoluble).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Inhibition of GDH1 activity by R162 treatment results in decreased intracellular fumarate levels, attenuated GPx activity, increased ROS levels, and reduced cell proliferation in H1299 and MDA-MB231 cells, which can be significantly rescued by methyl-α-KG treatment as well as by antioxidant NAC. R162 inhibits cell proliferation and tumor growth potential of human cancer cells.

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.

Products are for research use only. Not for human use.

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