General Information of the Drug (ID: ferrodrug0259)
Name
GW501516
Synonyms
317318-70-0; Endurobol; GW501516; GW 501516; GW-501516; Cardarine; GSK-516; GW1516; GW 1516; UNII-7I2HA1NU22; GW-1516; 2-(4-((2-(4-(Trifluoromethyl)phenyl)-4-methylthiazol-5-yl)methylthio)-2-methylphenoxy)acetic acid; 2-(2-Methyl-4-(((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methyl)thio)phenoxy)acetic acid; 2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid; GW-516; CHEMBL38943; 7I2HA1NU22; {2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid; 2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid; CHEBI:73726; GW501516(GSK-516); GW501,516; GW 501,516; GW-501,516; GSK 516; GW501516 (Endurobol); SCHEMBL68714; 2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]acetic Acid; MLS006010753; ENDUROBOL;GW501516; GTPL2687; DTXSID3041037; BDBM28661; EX-A723; HMS3674C03; HMS3744O09; BCP21491; MFCD09033000; PDSP1_000255; PDSP2_000254; s5615; AKOS015965103; CCG-269268; CS-0438; DB05416; EX-3881; SB19569; GW501516(G); NCGC00241455-01; NCGC00241455-02; NCGC00241455-08; AC-23001; HY-10838; SMR004701706; AM20040157; A26949; GW501516, >=98% (HPLC); 6T-0058; Benzenesulfonylchloride,4-(2-methylpropyl)-(9CI); J-018519; Q5515069; BRD-K14880289-001-01-4; (2-METHYL-4-(((4-METHYL-2-(4-(TRIFLUOROMETHYL)PHENYL)-1,3-THIAZOL-5-YL)METHYL)THIO)PHENOXY)ACETIC ACID; {2-Methyl-4-{{4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl}methylthio}phenoxy}acetic acid, analytical standard; {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]-2-methylphenoxy}acetic acid; 2-(2-methyl-4-((5-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-4-yl)methylthio)phenoxy)acetic acid;GW 501516; 2-{2-methyl-4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazole-5-yl}methyl)sulfanyl]phenoxy}acetic acid; 7T1; Acetic acid, (2-methyl-4-(((4-methyl-2-(4-(trifluoromethyl)phenyl)-5-thiazolyl)methyl)thio)phenoxy)-; Acetic acid, 2-[2-methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]-

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Status
Discontinued in Phase 4
Drug Type
Small molecular drug
Structure
Formula
C21H18F3NO3S2
IUPAC Name
2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid
Canonical SMILES
CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)OCC(=O)O
InChI
InChI=1S/C21H18F3NO3S2/c1-12-9-16(7-8-17(12)28-10-19(26)27)29-11-18-13(2)25-20(30-18)14-3-5-15(6-4-14)21(22,23)24/h3-9H,10-11H2,1-2H3,(H,26,27)
InChIKey
YDBLKRPLXZNVNB-UHFFFAOYSA-N
PubChem CID
9803963
TTD Drug ID
D05HDX
Full List of Ferroptosis Target Related to This Drug
Unspecific Target
In total 1 item(s) under this Target
Experiment 1 Reporting the Ferroptosis-centered Drug Act on This Target [1]
Responsed Disease Health ICD-11: N.A.
Responsed Regulator Peroxisome proliferator-activated receptor delta (PPARD) Suppressor
Pathway Response Fatty acid metabolism hsa01212
Ferroptosis hsa04216
Cell Process Cell ferroptosis
In Vitro Model mEFs (Mouse embryonic fibroblasts)
Response regulation GW501516-activated PPARD stabilized peroxisomes through catalase upregulation by targeting peroxisomal hydrogen peroxide-mediated lysosomal rupture, which led to ferroptosis of xCT-deficient MEFs.
References
Ref 1 Peroxisome proliferator-activated receptor rescues xCT-deficient cells from ferroptosis by targeting peroxisomes. Biomed Pharmacother. 2021 Nov;143:112223. doi: 10.1016/j.biopha.2021.112223. Epub 2021 Sep 25.