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Roxadustat fg 4592

Manufactured by Cayman Chemical
Sourced in Canada, United States

Roxadustat (FG-4592) is a small molecule compound developed by Cayman Chemical. It functions as an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase, an enzyme involved in the regulation of the HIF pathway.

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3 protocols using roxadustat fg 4592

1

Inhibitors for Cellular Processes

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Proteasome inhibitor MG132 was from Calbiochem. eIF4A1 inhibitor Rocaglamide A, alpha-glucosidase inhibitor Acarbose, protein disulfide isomerase (PDI) inhibitor 16F16, microsomal triglyceride transfer protein (MTTP) inhibitor lomitapaide and pan prolyl hydroxylase inhibitor ethyl 3,4-dihydroxybenzoate (EDHB) were from MilliporeSigma. Hsp70 inhibitors JG40 and JG345 were a gift from J. Gestwicki. Calmodulin inhibitor W7, Grp94 inhibitor PU-WS13, anti-fibrotic Nintedanib (BIBF 1120), HIF prolyl hydroxylase inhibitor Roxadustat (FG-4592) were from Cayman Chemicals. Diethyl-pythiDC was from AOBIOS.
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2

Evaluating Anti-Cancer Drugs in Lung Cell Lines

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Human lung A549 (RRID:CVCL_0023), SK‐MES‐1 (RRID:CVCL_0630), H1299 (RRID:CVCL_0060), H1975 (RRID:CVCL_1511), and H460 (RRID:CVCL_0459) cancer cells were obtained from the American Type Culture Collection (ATCC: Manassa, VA). Cell lines were authenticated within the past 3 years using short tandem repeat DNA profiling and comparing the DNA sequences to the reference cell database, with an > 80% match being acceptable. Cells were assessed for mycoplasma contamination using the MycoAlert Mycoplasma Detection Kit (Lonza Group AG: Basel, Switzerland). Cell lines were cultured in DMEM (A549 and SK‐MES‐1), RPMI‐1640 (H1299 and H460) or ATCC‐modified RPMI‐1640 (H1975) with 10% FBS and 1% antibiotic‐antimycotic. All cells were maintained at 37 °C in a humidified 5% CO2 incubator. Cells were treated with canagliflozin (MedChemExpress LLC: Monmouth Junction, NJ) solubilized in dimethyl sulfoxide, cisplatin (Accord Healthcare Inc: Durham, NC), etoposide (Teva Canada Ltd: Toronto, Canada), radiation (6MV X‐rays as described [26 (link)]), Roxadustat (FG‐4592), BAY‐87‐2243, and IACS‐010759 (Cayman Chemical Company: Ann Arbor, MI).
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3

Hypoxia-inducible factor prolyl hydroxylase inhibitors

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Roxadustat or molidustat were dissolved in vehicle [10% ethanol (70% grade) and 90% corn oil] and administered i.p.; Roxadustat (FG-4592, Cayman Chemical, Ann Arbor, MI, USA) at a dose of 1, 2, 10, 20 or 30 mg kg -1 ; molidustat (BAY 85-3934, Cayman Chemical, MI Ann Arbor, USA) at a dose of 1 or 10 mg kg -1 . Given its longer half-life, two doses of Roxadustat were administered 48 hours apart, with the second dose given 6 hours prior to tissue harvest or initiation of surgical procedures. Three doses of 1 mg kg -1 of molidustat were administered 24 hours apart and two doses of 10 mg kg -1 of molidustat were given 48 hours apart, with the final doses given 4 hours prior to tissue harvest or initiation of surgical procedures. L-NAME (Sigma-Aldrich, Steinheim, Germany) was dissolved in the same vehicle and was injected i.p. at a dose of 10 mg kg -1 on the day of surgery at the time of final HIF-PHI administration.
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