- Cat. No.
- A10776
Raltitrexed
Synonyms: Tomudex; TDX; ZD 1694
Raltitrexed (Tomudex) is an inhibitor of thymidylate synthase and also is one of the strongest antimetabolites in use.
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Synthase and synthetase inhibitors block enzymes that build nucleotides, cell wall polymers and lipids. Thymidylate synthase supplies thymidine nucleotides for DNA replication and is a classic target of antifolate compounds. Raltitrexed was reported in 1991 as a quinazoline antifolate inhibitor of this enzyme, and Nolatrexed Dihydrochloride is a further example. Caspofungin, micafungin and anidulafungin are echinocandins that inhibit fungal 1,3-β-D-glucan synthase. In Candida albicans, a glucan synthase subunit gene was identified in 1997 as the essential target of these inhibitors. Other compounds act on lipid synthesis, such as the squalene synthase inhibitor YM-53601. Triacsin C inhibits long-chain acyl-coenzyme A (acyl-CoA) synthetases, which activate fatty acids for further metabolism.
Synonyms: Tomudex; TDX; ZD 1694
Raltitrexed (Tomudex) is an inhibitor of thymidylate synthase and also is one of the strongest antimetabolites in use.
Micafungin (Mycamine; FK463) is an echinocandin antifungal drug which can inhibit 1,3-beta-D-glucan synthase.
Anidulafungin is a semi-synthetic cyclic lipopeptide belonging to the echinocandin class that was reported in 1995 and commercially developed by Eli Lilly. Anidulafungin inhibits the synthesis of ??-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi and is extensively referenced in the literature with over 400 citations.
Synonyms: MK-217,G-704650; Fosamax; Adronat
Alendronate is a nitrogen-containing bisphosphonate that is commonly used in the treatment of osteoporosis and other metabolic bone diseases.
Pneumocandin B0 is the major analogue of a family of lipopeptides isolated from several species of several different genera, notably Cryptosporiopsis, Glarea and Pezicula. Pneumocandin B0 is a potent antifungal and acts by inhibition of the synthesis of β-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi.
HQL-79 is a selective inhibitor of hematopoietic prostaglandin D (PGD) synthase, that structurally is a synthetic tetrazole compound originally prepared as a possible antihistamine.
Synonyms: AG 337; Thymitaq
Nolatrexed Dihydrochloride is an antifolate thymidylate synthase inhibitor.
Synonyms: Cancidas
Caspofungin is an antifungal medicine. It is used to help the body overcome serious fungus infections, including Candida and Aspergillosis infections. It is also used to treat serious fungus infections when other medicines (e.g., amphotericin B, itraconazole) have failed.
YM-53601 is a novel squalene synthase inhibitor. It suppresses lipogenic biosynthesis and lipid secretion in rodents.
Synonyms: WS1228A; FR 900190
Triacsin C, originally isolated from Streptomyces sp., is an inhibitor of long fatty acid acyl-CoA synthetase (IC50 = 6.3 uM in Raji cells).
Synonyms: GW1843; 1843U89; OSI-7904
OSI-7904L is a noncompetitive inhibitor of thymidylate synthase (TS), functioning as an antifolate compound and a substrate for folylpolyglutamate synthetase. This compound exhibits significant cytotoxicity against various solid tumor cell lines, demonstrating its potential in cancer research and therapeutic applications. The cytotoxic effects of OSI-7904L can be selectively mitigated by folic acid, highlighting its mechanism of action and potential for targeted treatment strategies.
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Bismuth Subcitrate is an antibiotic used to treat stomach ulcers associated with Helicobacter pylori, a bacterial infection.
Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
Synonyms: Genz123346
Genz-123346 free base is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; IC50 for GM1 inhibition is 14 nM.
Synonyms: NSC-326231; BSO
Buthionine Sulphoximine is a gamma-glutamylcysteine synthetase inhibitor potentially for the treatment of solid tumors.
Synonyms: GSK-2251052; Epetraborole HCl
AN3365 is a potent and selective leucyl-tRNA synthetase inhibitor.
Synonyms: Sulfamonmethoxine
Sulfamonmethoxine is a competitive inhibitor of dihydropteroate synthetase, blocking the synthesis of folic acid.
LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively.
GlyRS-IN-1 is a glycyl-tRNA synthase (GlyRS) inhibitor extracted from patent WO 2017066459 A1. GlyRS-IN-1 can also inhibit the growth of bacteria.
ATP synthase inhibitor 1 is a potent inhibitor of c subunit of the F1/FO-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels.
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation.
Arg-AMS is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.
Gln-AMS is an aminoacyl-tRNA synthetases (AARS) inhibitor, which binds the A-domain within the NRPS enzymes.
FAS-IN-1 is a potent inhibitor of Fatty acid synthase (FAS) wtih IC50 of 10 nM, extracted from Patnet WO2012/064642Al.
Diazaquinomycin A is a potent inhibitor of thymidylate synthase, a key enzyme involved in DNA synthesis. This diaza-anthracene antibiotic induces DNA damage and triggers cellular responses such as cell cycle arrest and apoptosis, evidenced by the cleavage of PARP. It serves as a valuable tool in cancer research and studies focused on therapeutic strategies targeting DNA replication and repair mechanisms.
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