Antifungal

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of iron death. Ferrostatin-1 potently inhibits Erastin-induced iron death in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin is a SET7 9 inhibitor and ameliorates renal fibrosis by inhibiting H3K4 methylation.

Tunicamycin is a mixture of antibiotics that inhibit N-linked glycosylation by blocking GlcNAc phosphotransferase (GPT). Tunicamycin has antitumor activity, as well as anti-bacterial, anti-fungal, and anti-viral activity.

Taniborbactam dihydrochloride (VNRX-5133 dihydrochloride) is a selective and potent novel cyclic boronic acid β-lactamase inhibitor with antimicrobial activity and significant inhibition of Gram-negative bacteria.Taniborbactam dihydrochloride inhibits KPC Taniborbactam dihydrochloride inhibits KPC-2, AmpC, OXA-48 and VIM-2 and can be used for the study of fungal infections.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Rezafungin (SP-3025) is a broad-spectrum and long-lasting echinocandin with potent antifungal activity against Candida, Aspergillus and Pneumocystis.

Olorofim（F-901318）is a novel selective antifungal compound targeting pyrimidine biosynthesis in mycobacteria, with inhibitory effect on Aspergillus fumigatus DHODH (IC50: 44 nM), but little inhibitory effect on human DHODH (>100 uM).Olorofim has good efficacy against a variety of pathogenic filamentous and dimorphic fungi, such as Penicillium spp, P. dermatitidis spp and Fusarium spp.

Hygromycin B (Hygrovetine) is an aminoglycoside antibiotic that inhibits protein synthesis by interfering with translocation and causing mistranslation of the 70S ribosome. Hygromycin B can be used to screen prokaryotic or eukaryotic cells transfected with hph or hyg resistance genes.

1. Isoliquiritin (Neoisoliquritin) has antitussive effects. 2. Isoliquiritin has antidepressant-like effects. 3. Isoliquiritin, liquiritin and isoliquirigenin inhibits the p53-dependent pathway and shows crosstalk between Akt activities.

Aureobasidin A is a cyclic peptide and an antifungal antibiotic. Aureobasidin A is an inhibitor of the inositolphosphorylceramide synthase AUR1.

Micafungin sodium (FK 463) is the sodium salt form of micafungin, a semi-synthetic echinocandin derived from a natural product of the fungus Coleophoma empetri with antifungal activity.

Albaconazole (W-0027) is a small molecule fungal cytochrome P450 family member 51 (fungal CYP51A1) inhibitor. It is used in the treatment of fungal infections, skin and musculoskeletal disorders, and can be used in the study of vulvovaginal candidiasis, Chagas disease and genitourinary disorders.

Oligomycin A (MCH 32) is an inhibitor of ATP synthase, inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria.

Caspofungin Acetate (MK 0991) is the acetate salt of an antimycotic echinocandin lipopeptide, semisynthetically derived from a fermentation product of the fungus Glarea lozoyensis. This agent is active against Aspergillus and Candida species.

Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1 exportin 1 by covalent modification at a cysteine residue.

Embeconazole (R 120758) is a triazole antifungal agent.Embeconazole has strong in vitro activity against clinically important fungi such as Candida, Aspergillus and Cryptococcus neoformans.

Voriconazole (UK-109496) is a triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 [CYP3A].

Cycloheximide (Naramycin A) is a natural product that reversibly inhibits translation elongation, is an antimitotic compound, and is an inhibitor of DNA and protein synthesis.

E1210 (APX001A) is broad-spectrum and orally active antifungal

Anidulafungin (Ecalta) (LY303366) is an echinocandin derivative used as an antifungal drug. It inhibits glucan synthase activity.

PC945 (Opelconazole) is a potent broad-spectrum antifungal compound with inhibitory effect on fumonisinol 14α-demethylase (CYP51A CYP51B), which can be used in the study of fungal infections of the lungs.

Rhapontigenin (Protigenin) is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. At higher concentrations, rhapontigenin inhibits the proliferation of HL-60R and HepG2 cancer cell lines (IC50: 48 μM).

Myriocin (Thermozymocidin), a metabolite derived from Myriococcum albomyces, is a serine-palmitoyltransferase (SPT) inhibitor with potential antitumour, anticancer, and antiparasitic activities.Myriocin inhibits tumour growth by regulating macrophage polarisation and function through the PI3K Akt mTOR pathway.Myriocin inhibits HCV infection and can be used in the study of neurological diseases. Myriocin inhibits HCV infection and can be used to study neuropathy and fungal infections.

Cyclo(L-Leu-L-Pro) is a compound from Pseudomonas sesquiterpenes BC42 that exhibits antifungal activity, inhibiting fungal pathogens, the proliferation of Aspergillus flavus, conidial germination, and conidial formation, making it useful for agricultural biocontrol.

Cerulenin is a natural inhibitor of fatty acid synthase (FAS). It is produced by the fungus Cephalosporium caeruleus.

Nourseothricin sulfate (Streptothricin sulfate) is a broad-spectrum antibiotic that inhibits protein biosynthesis in prokaryotic cells and significantly impedes the growth of eukaryotes, including fungi.

Hyperoside (Hyperin) is a naturally occuring flavonoid compound which shows multiple bioactivities, including myocardial protection, anti-redox, and anti-inflammatory activities.

Dimboa (2,4-dihydroxy-7-methoxy-1,4-benzoxazin-3-one) is an antifungal compound used in crops.

Posaconazole (POS) is a sterol C14ɑ demethylase inhibitor (IC50: 0.25 nM).

Deoxylapachol has anti-wood rot activity, it can inhibit the brown rot fungi Gloeophyllum sepiarium CBS 353.74 and Gloeophyllum trabeum CBS 318.50 and the white rot fungi Merulius tremellosus CBS 280.73 and Phlebia brevispora CBS 509.92. It also can induc

Filipin III is extracted from strain KPE18H and has significant antifungal activity.

Fluconazole (UK-49858) is a triazole antifungal agent used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS.

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

alpha-Mangostin (Mangostin) is a natural xanthonoid, a type of organic compound isolated from various parts of the mangosteen tree.

(+)-Magnoflorine (Thalictrin) has sedative and anxiolytic effects, probably mediated by Magnoflorine through a GABAergic mechanism of action. Magnoflorine and Sinomenine have protective effects, are mediated by some mechanism other than prevention of micelle formation or protection of the erythrocyte membrane against osmotic imbalance.

Rilopirox (HOE 351) initiated a novel antifungal compound for the study of mucosal Candida infections, lichen planus and seborrheic dermatitis.

Oteseconazole (VT-1161) is an orally active anti-fungal agent. Oteseconazole displays no obvious effect on human CYP51. It also potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM).

Piperlonguminine, an alkaloid amide isolated from the Piper species, exhibits anti-inflammatory, antitumor, neuroprotective, anti-platelet, anti-melanogenic, antifungal, and antibacterial activities. It inhibits Akt mTOR signaling, promotes autophagy, and mediates cancer cell death.

Nystatin (Fungicidin) is a topical and oral antifungal agent with activity against many species of yeast and candida albicans, which is used largely to treat skin and oropharyngeal candidiasis.

Ciclopirox (HOE296b) exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. Ciclopirox is a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, the organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).

Isavuconazole (RO-0094815)(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557 with MIC(50)s MIC(90)s ranged from 0.002 0.004 mg liter for C. albicans to 0.25 0.5 mg liter for C. glabrata.

NB-598 is an effective and competitive inhibitor of squalene epoxidase. It suppresses triglyceride biosynthesis through the farnesol pathway.

Kanosamine (3-Amino-3-deoxyglucose) is an antifungal agent produced by a Streptomyces species.

Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

Phenamacril (JS39919) is acyanoacrylate fungicide, has powerful inhibition against Fusarium species, especially to Fusarium graminearum. Phenamacril is a specific Fusarium myosin I inhibitor.

Idarubicin hydrochloride (Zavedos), a hydrochloride salt form of Idarubicin, is a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells ( IC50: 3.3 ng mL).

Calcimycin (A-23187) is an ionophorous, polyether carboxylic antibiotic from Streptomyces chartreusensis. It binds and transports calcium and other divalent cations across membranes, uncouples oxidative phosphorylation, and inhibits ATPase of rat liver mitochondria. The substance is primarily used as a biochemical tool to study the role of divalent cations in various biological systems.

Spathulenol is a natural ingredient from Aristolochia yunnanensis that has anti-inflammatory, antioxidant, anti-proliferation, anti-ulcer and anti-mycobacterium activities. Spathulenol showed significant antioxidant activity in DPPH system with IC50 of 85.60 μg mL.