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F3680 10058-F4 ≥98% (HPLC), solid 10058-F4 is a c-Myc inhibitor that induces cell-cycle arrest and apoptosis. 10058-F4 is a cell-permeable thiazolidinone that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 inhibits tumor cell growth in a c-Myc-dependent manner both in vitro and in vivo (64 μM using c-Myc transfected Rat1a fibroblasts).
 
F3806 Fadrozole hydrochloride ≥98% (HPLC) Fadrozole is a nonsteroidal aromatase inhibitor. Fadrozole is a very potent and highly selective inhibitor of the aromatase enzyme system in vitro and estrogen biosynthesis in vivo. It inhibited the conversion of [4-14C]androstenedione to [4-14C]estrone by human placental microsomes in a competitive manner (Ki = 1.6 nM). At a substrate concentration 3-fold the Km, Fadrozole was 180 times more potent, as an inhibitor, than aminoglutethimide (Cat. No. A9657), exhibiting half-maximal inhibition at 1.7 nM as compared to 0.3 μM. In vivo, Fadrozole lowered ovarian estrogen synthesis by gonadotropin-primed, androstenedione treated, immature rats by 90% at a dose of 260 μg/kg (PO). In vivo, Fadrozole leads to sequelae of estrogen deprivation (e.g. regression of DMBA-induced mammary tumors) without causing adrenal hypertrophy in adult rats. It blocked aromatase by 50% in human breast cancer homogenates, live breast cancer cells, human placental microsomes, and porcine ovarian microsomes at concentrations of 0.008 to 0.02 μM.
 
SML0837   FAK Inhibitor 14 ≥95% (HPLC) 1,2,4,5-Benzenetetraamine tetrahydrochloride (FAK Inhibitor 14; Y15) is a cell-permeable, selective focal adhesion kinase (FAK) inhibitor. Focal adhesion kinase (FAK) is essential in regulating integrin signaling pathways responsible for cell survival, cell proliferation and motility. Phosphorylation of FAK tyrosine 397 (Y397) forms a high affinity binding site for the SH2 domain of the Src family kinases and PI3 kinase. FAK is overexpressed in a number of human tumors. 1,2,4,5-Benzenetetraamine tetrahydrochloride (FAK Inhibitor 14, Y15) blocks phosphorylation of Y397-FAK, which results in neuroblastoma cell detachment and apoptosis.
 
F7932 Famciclovir ≥98% (HPLC) Famciclovir is an antiretroviral guanosine analog used to treat herpesvirus infections and hepatitis B. Famciclovir is rapidly converted to penciclovir. Viral thymidine kinase phosphorylates penciclovir to a monophosphate form that celular kinases convert in turn to penciclovir triphosphate. Penciclovir triphosphate competitively inhibits viral DNA polymerase and thus viral replication. Prolonged administration can lead to resistance; it is often manifested as selection of pre-existing resistant strains with mutations in the reverse transcriptase domain of the DNA polymerase gene.
 
F6889 Famotidine H2 histamine receptor antagonist; anti-ulcer agent
human ... HRH2(3274)
F8182 Faropenem sodium hydrate ≥98% (HPLC) Faropenem sodium is an ultra-broad spectrum, β-lactamase resistant, β-lactam antibiotic active against both Gram-positive and Gram-negative bacteria.
 
SML1389 Farrerol ≥98% (HPLC) Farrerol is major bioactive component from Rhododendron dauricum L. (Man-Shan-Hong). Farrerol exhibits numerous activities including antibechic, anti-bacterial, anti-inflammatory and inhibition of vascular smooth muscle cells (VSMC) proliferation. Recent study shows that Farrerol regulates occludin expression by preventing H2O2-induced activation ERK 1/2 in human endothelium-derived EA.hy926 cells.
 
F5557 Fasentin ≥98% (HPLC) Fasentin is a novel inhibitor of glucose uptake, GluT1 inhibitor. Fasentin is a novel inhibitor of glucose uptake that sensitizes cells to FAS-induced cell death. Fasentin selectively sensitized to death ligands, but did not decrease FLIP expression. It alters expression of genes associated with nutrient and glucose deprivation. Fasentin interacted with a unique site in the intracellular channel of the glucose transport protein GLUT1.
 
SML1815 Fasnall benzenesulfonate salt ≥98% (HPLC) Fasnall is a fatty acid synthase (FASN or FAS) inhibitor (IC50 = 3.71 ?M by cell-free assay with 200 μM NADPH; IC50 = 147 and 213 nM against acetate and glucose lipids incorporation in HepG2 cells) composed of two enantiomers (HS-79 and HS-80) that selectively target FASN co-factor nucleotide-binding sites without affecting ACC, ZipK, AMPKα, AMPKγ, TRAP1, HSP70, NS5, IRAK2 nucleotide binding or the ATP-binding activity of BT474 cellular proteins. Fasnall is shown to completely block the proliferation in multiple breast cancer cultures at 50 μM as a result of apoptosis induction with much reduced cytotoxicity than C75 toward the non-tumorigenic cell line MCF10A. When administered via i.p. injection, Fasnall is efficacious in prolonging the survival of MMTV-Neu mice by effectively suppressing mammary adenocarcinoma tumor progression (15 mg/kg dosed alone twice weekly or 50 mg/kg dosed with carboplatin once weekly).
 
F8932   Fatostatin hydrobromide ≥98% (HPLC), powder Fatostatin hydrobromide is an SREBP inhibitor. Fatostatin hydrobromide inhibits fat production and lowers glucose levels in mice by inhibiting SREBP (Sterol Regulatory Element Binding Proteins).
 
F4429 FAUC 213 ≥98% (HPLC), solid Highly selective D4 dopamine receptor full antagonist
human ... DRD2(1813), DRD3(1814), DRD4(1815)
T5699 m-3M3FBS >97% (HPLC) First known direct activator of phospholipase C (activates β2, β3, γ1, γ2, δ1 isoforms).
 
SML2371 FC-99 hydrochloride ≥98% (HPLC) FC-99 is a benzenediamine derivative that inhibits LPS-induced IRAK4 phosphorylation/activation and downstream signaling events (5-45 μM; murine RAW 264.7 & peritoneal macrophages), including IRAK1 (a TLR3 pathway negative regulator) degradation, p38/ERK/JNK activation, and cytokines production. FC-99 inhibits RSV replication (50 μM; A549) and poly(I:C)-indued IRF3/IFN-α/JAK/STAT1 signalling in cultures (0.5-50 μM; murine peritoneal macrophages), and ameliorates sepsis induction following caecal ligation puncture (CLP) in mice in vivo (100/70/32.5% motality in 7 days with 0/30/100 mg/kg i.p. 2 h prior to CLP).
FC-99 is known to affect the levels of serum immunoglobulin. It might be therapeutically beneficial in systemic lupus erythematosus.
 
SML1392 FDI-6 ≥98% (HPLC) FDI-6 is a potent and specific inhibitor of FOXM1 that blocks DNA binding. FDI-6 binds to FOXM1 protein and specifically downregulates FOXM1-activated genes.
Forkhead domain inhibitor-6 (FDI-6) is used to treat anaemia patients because of diminished red blood production. In Hep-2 cells, FDI-6 can stimulate cell death and also helps to prevent cell proliferation, invasion and migration.
 
SML0681 Febrifugine dihydrochloride ≥95% (HPLC) Febrifugine dihydrochloride exhibits strong antimalarial activity against Plasmodium falciparum, the most insidious malaria causative agent. The adverse effects of febrifugine include diarrhoea, vomiting and liver toxicity.
Febrifugine is an antimalarial, the active component of the Chinese herb Chang Shan. Recent studies indicate that its mechanism of action is as an inhibitor of prolyl-transfer RNA synthetase (ProRS).
 
F0778 Felbamate Anticonvulsant agent that is an allosteric antagonist at the NR2B subunit of the NMDA glutamate receptor; also has γ-aminobutyric acid (GABAA) receptor agonist properties.
human ... GRIN2B(2904)
F9677 Felodipine solid L-type calcium channel blocker
human ... CACNA2D1(781)
F112 (+)-Fenfluramine hydrochloride (+)-Fenfluramine is a serotonin uptake inhibitor; anoxexic. (+)-Fenfluramine is neurotoxic on prolonged administration or at high dosage. (+)-Fenfluramine releases serotonin from axon terminals by a nonexocytotic mechanism.
 
F0430 Fenobam ≥98% (HPLC), solid Fenobam is a potent, selective, noncompetitive glutamate mGluR5 receptor antagonist. Fenobam displays inverse agonist properties; blocks mGluR5 constitutive activity in vitro (IC50 = 87 nM, slightly weaker than MPEP). Fenobam acts at an allosteric modulatory site shared with MPEP and binds the mGlu5 receptor with Kd values of 54 and 31 nM for rat and human receptors, respectively. Fenobam belongs to a structurally different class than MPEP; devoid of GABAergic activity and thus typical benzodiazepine-like side effects; displays anxiolytic activity.
 
F6020 Fenofibrate ≥99%, powder Fenofibrate increases high density lipoprotein levels by reducing cholesteryl ester transfer protein expression. It is used in treating the condition of increased cholesterol levels in the blood, abnormal lipid levels in the body and also hypertriglyceridaemia. Fenofibrate is a lipid regulating drug and proliferator-activated receptor-α (PPARα) mediates its action. It decreases the plasma levels of fibrinogen and C-reactive protein. By this fenofibrate allows better flow-mediated dilatation and reduces the risk of atherosclerosis. Fenofibrate is also known to reduce uric acid levels.
human ... PPARA(5465)
SML0198 Fenoldopam mesylate ≥98% (HPLC) Fenoldopam mesylate is a selective dopamine D1 receptor agonist used as an antihypertensive agent. It is an agonist for D1-like dopamine receptors and binds with moderate affinity to α2-adrenoceptors. It has no significant affinity for D2-like receptors, α1 and α-adrenoceptors, 5HT1 and 5HT2 receptors, or muscarinic receptors. Fenoldopam mesylate causes peripheral vasodilation by stimulating dopamine-1receptors and α2-adrenoceptors, increasing renal blood flow.
 
F1016 Fenoterol hydrobromide β2-adrenoceptor agonist; bronchodilator.
human ... ADRB2(154)
F3886 Fentanyl citrate salt Phenylpiperidine analgesic that is 80 times more potent than morphine as an analgesic and 6000 times more potent than morphine as a μ opioid receptor agonist.
 
F1428 Fenvalerate ≥97% Fenvalerate has good insecticidal potential and is less toxic to animals. It might cause endocrine disruption and reproductive dysfunction in humans. Metabolism of fenvalerate includes oxidation, ester cleavage and conjugation reaction. It is stable at pH 5 and 7, while it gets hydrolyzed at pH 9. In rat models it is found to hinder the action of mitochondrial enzymes.
Fenvalerate is a type II semi-synthetic pyrethrin, which acts as a potent inhibitor of calcineurin (protein phosphatase 2B). This inhibitory action results in cellular hyperexcitability by causing non-mutated calcium channels to remain open for an extended period of time allowing an abundance of Ca2+ to enter the cell.
Type II pyrethroid. Potent inhibitor of calcineurin (protein phosphatase 2B).
 
SML2350 Ferroquine ≥98% (HPLC) Ferroquine (SSR 97193) is an antimalarial chloroquine analog effective against chloroquine-resistant Plasmodium falciparum. Ferroquine is thought to act by producing oxidative stress and by inhibiting the formation of hemozoin, produced by Malaria parasites as a disposal product of heme, which would otherwise be toxic to the Plasmodium cells.
 
SML0583   Ferrostatin-1 ≥95% (HPLC) Ferrostatin-1 is a potent inhibitor of non-apoptotic cell death induced by erastin call ferroptosis. Ferrostatin-1 prevents ferroptopic cell death in cancer cells and glutamate-induced toxicity in organotypic rat brain slices. It appears that Ferrostatin-1 controls lipid soluble ROS.
Ferrostatin-1 is an active radical-trapping antioxidant that traps peroxyl radicals, and thus serves as a potential inhibitor of ferroptosis. Ferroptosis is considered as regulated necrosis, which differs from apoptosis and autophagy. Ferrostatin-1 is known to show protective effects against Huntington’s disease and also prevents neurotoxicity induced by glutamate in cellular models.
 
SML1609 Ferutinin ≥98% (HPLC) An ERα (estrogen receptor) agonist; phytoestrogen
Ferutinin is a naturally occurring non-steroidal phytoestrogen. It is a strong agonist for estrogen receptor (ER)α and agonist/antagonist for Erβ with IC50 values of 33.1 nM for ERα and 180.5 nM for Erβ. It has been shown to have both ionophoretic and apoptotic properties. It increases calcium permeability in the lipid bilayer and has been shown to improve bone regeneration in a rat study. It caused significant regression in tumor size in a mouse colon cancer model.
 
SML1390 Fexaramine ≥98% (HPLC) Fexaramine is a potent and selective agonist of the bile acid sensor farnesoid X receptor (FXR) in the gut with an EC50 of 25 nM and no activity found for other nuclear receptors. Fexaramine induces enteric fibroblast growth factor 15 (FGF15), causing alterations in bile acid composition without activating FXR target genes in the liver. In mouse studies, fexaramine enhanced thermogenesis and browning of white adipose tissue while reducing diet-induced weight gain, body-wide inflammation and hepatic glucose production. Fexaramine also improved insulin responsiveness.
Fexaramine might regulate lipid and glucose metabolism and can serve as a therapeutic target in the treatment of fatty liver disease, type 2 diabetes and obesity. Fexaramine might mediate cholesterol homeostasis and promotes osteoblast differentiation and suppresses differentiation of osteoclast.
 
F9427 Fexofenadine hydrochloride >98% (HPLC) Fexofenadine is a non-sedating H1 histamine receptor antagonist.
human ... HRH1(3269)
SML1172 FFN102 ≥98% (HPLC) FFN102 is a pH-responsive fluorescent false neurotransmitter that acts as a dopamine transporter substrate (DAT) and also a substrate for vesicular monoamine transporter 2 (VMAT2). FFN102 selectively labels dopamine cell bodies and dendrites in ventral midbrain and dopaminergic synaptic terminals in dorsal striatum. Its greater fluorescence emission in neutral than acidic environments allows the visualization of dopamine release at individual presynaptic terminals and in situ pH measurement of catecholamine secretory vesicles.
 
F9932 FFN511 trifluoroacetate salt hydrate ≥98% (HPLC) FFN511 is a fluorescent substrate for the synaptic vesicle monoamine transporters. FFN511 is used as an optical tracer of dopamine, a fluorescent false neurotransmitter (FFN) to visualize dopamine release from individual presynaptic terminals using time-lapse microscopsy fluorescence. The probe is sufficiently fluorescent so as to provide resolution of individual dopamine terminals at concentrations that do not interfere with normal catecholamine accumulation and transmission. FFN511 is compatible with GFPbased tags, the FM1-43 endocytic marker (Synapto Green), and other optical probes.
 
SML0826   FH1 ≥98% (HPLC) FH1 (BRD-K4477) was found to enhance hepatocyte functions and promote the differentiation of induced pluripotent stem cell–derived hepatocytes toward a more mature phenotype than what had previouslybeen obtainable. Human induced pluripotent stem (iPS) cells that are differentiated toward hepatocyte-like (iHep) cells typically show an immature hepatic phenotype and have limited use as a renewable source of functional human hepatocytes. Cultures treated with both FH1 (BRD-K4477) and another compound that induces proliferation, FPH1 (BRD-6125), contained larger colonies of iHep cells, which showed more pronounced hepatocyte morphologies with a more mature phenotype than previously obtainable.
 
F5682 FH535 ≥98% (HPLC) FH535 has the ability to block the development of colon cancer cells. It can change several cancer-associated biological processes. FH535 can also prevent PARylation of Axin2 in osteosarcoma cells.
FH535 is a reversible dual inhibitor of Wnt/β-catenin and a PPARγ and PPARδ signaling antagonist. FH535 is unique in its ability to inhibit the Wnt/β-catenin pathway. The compound is selectively toxic to some carcinomas expressing the Wnt/β-catenin pathway.
 
SML1734 FHZ ≥98% (HPLC) FHZ is a highly selective, cell-permeable, non-cytotoxic, non-fluorescent 6-triethylene glycol-substituted fluorescein hydrazide that is an efficient fluorescent turn-on probe for dual channel detection of (•OH) and HOCl in live cells and zebrafish embryos. FHZ selectively reacts with hydroxyl (•OH) and HOCl, respectively, to form highly fluorescent FOBA (Ex: 410 nm & Em.: 486 nm; Φ = 0.42; ε410 = 12000/M/cm) and F-TEG (Ex: 490 nm & Em.: 520 nm; Φ = 0.34; ε490 = 7000/M/cm), while exhibiting no reactivity toward H2O2 1O2, O2•–, NO, or ONOO–. Cyan and green fluorescence dual-channel detection with two exciting wavelengths (405 nm and 488 nm) and two collection windows (430–490 nm; 510–560 nm) allows time-dependent quantitative detection of cellular •OH and HOCl by FHZ in live cells (50-100 μM; HeLa and RAW 264.7 macrophages) cells and zebrafish embryos (50 μM).
 
SML0632 Fialuridine ≥98% (HPLC) Fialuridine (1-(2-deoxy-2-fluoro-β-d-arabinofuranosyl)-5-iodouracil, or FIAU) and its metabolites blocks DNA polymerase at sites of multiple adjacent analog incorporation, reduces the presence of mtDNA (mitochondrial DNA) and results in mitochondrial structural defects in cultured hepatoblasts. It is considered as an efficient drug against hepatitis B virus (HBV) infection.
Fialuridine is a nucleoside analog antiviral agent. The compound displays significant mitochondrial toxicity.
 
SML1489   FICZ ≥95% (HPLC) FICZ (6-formylindolo(3,2b)carbazole) being a photooxidation product of tryptophan, might serve as a chemical messenger of light.
FICZ is a potent high affinity ligand of the aryl hydrocarbon receptor (AhR), which is a ligand-activated transcription factor that activates the expression of aromatic hydrocarbon metabolizing enzyme genes such as the CYP1A1 gene and has also been shown to have multiple additional roles in cell-cycle regulation, development and maturation of many tissues, control of inflammation, and immune response. FICZ is a photoproduct of tryptophan and is believed to be an endogenous AhR ligand. It is extremely potent, with a Kd value of 0.07 nM.
 
SML1956   FIIN-4 ≥98% (HPLC) FIIN-4 is a potent, irreversible, type II inhibitor against FGFR (IC50 = 2.6, 2.6, 5.6, 9.2 nM, respectively, against FGFR1-4) whose 4-acrylamidebenzyl moiety covalently modifies FGFR P-loop cysteine in its DFG-out conformation with good target selectivity based on a 456-kinase panel (354 non-mutants kinases) kinome profiling. FIIN-4 effectively inhibits FGF2-induced Erk1/2 phosphorylation in serum-starved D2.A1 murine mammary carcinoma cells (by 100% wtih 18-hr 250 nM pretreatment) and D2.A1 growth in 3D cultures (by 54% at 100 nM) without affecting EGF-dependent Erk phosphorylation or 3D growth of NMuMG murine mammary epithelial cells. Oral administration (25 mg/kg q.o.d.) is efficacious in suppressing the growths of tumors-derived from murine mammary carcinoma 4T1 lung metastases and patient TNBC brain metastases xenografts in mice in vivo with good pharmacokinetics (Tmax = 0.5 hr, T1/2 = 2.4 hr, AUC = 935 h·ng/mL; 10 mg/kg p.o.) and without overt toxicity to the animals.
 
SML0876   Filastatin ≥98% (HPLC) Filastatin blocks the ability of Candida albicans, and other Candida sp. to bind to polystyrene, and human A549 cell monolayers. Filastatin also blocks biofilm formation and yeast-to-hyphal morphologic transition through inhibition of the hyphal-specific promoter HWP1.
 
PZ0030   Filibuvir ≥98% (HPLC) Filibuvir is an orally available, potent and selective inhibitor of the hepatitis C virus (HCV) nonstructural 5B (NS5B) RNA-dependent RNA polymerase that exhibits potent antiviral activity against subgenomic HCV replicons in cell culture assays. Also, Filibuvir potently inhibits viral replication in infected patients. Filibuvir interacts with the thumb site II of the viral polymerase.
 
SML1740   FIN56 ≥98% (HPLC) FIN56 is a specific inducer of ferroptosis, a non-apoptotic form of cell death characterized by iron-dependent accumulation of lipid peroxidation products and lethal reactive oxygen species (ROS). FIN56 has an EC50 value of 240 nM, and is believed to act though two separate pathways. The first requires the enzymatic activity of acetyl-CoA carboxylase (ACC),and results in degradation of glutathione peroxidase 4 (GPX4), which acts as a negative regulator of ferroptosis by reducing lipid hydroperoxides. The second pathway involves FIN56 binding to and activing squalene synthase, which leads to coenzyme Q10 depletion.
Ferroptosis inducer 56 (FIN56) is a member of the class 3 ferroptosis inducers.
 
SML2134 Finafloxacin ≥95% (HPLC) Finafloxacin is a fluoroquinolone antibiotic approved by the FDA in 2014 for treating swimmer′s ear. Its mechanism of action involves the inhibition of bacterial type II topoisomerase enzymes, DNA gyrase and topoisomerase IV
 
F1293 Finasteride ≥98% (HPLC), powder Finasteride can reduce serum and scalp dihydrotestosterone (DHT) by preventing the transformation of testosterone to DHT. It is usually used to manage benign prostate hyperplasia and pattern hair loss in male. Finasteride possesses androgen-distracting properties.
Selective 5α-reductase inhibitor; antiandrogen.
human ... HSD3B1(3283), SRD5A1(6715), SRD5A2(6716)
rat ... Hsd3b1(360348), Srd5a1(24950), Srd5a2(64677)
SML1733 FINDY ≥98% (HPLC) FINDY is a cell-permeable thioxothiazolidinone derivative that specifically targets newly synthesized cellular DYRK1A, but not DYRK1B or DYRK2, for proteasomal degradation by suppressing DYKR1A intramolecular Ser97 autophosphorylation, a necessary event for folding/maturation of newly translated DYRK1A. Unlike INDY and other ATP-competitive DYRK inhibitors, FINDY is ineffective against the kinase activity of DYRK1A, DYRK1B, DYRK2, or DYRK3 (IC50 >10 μM) and inhibits only five kinases (GSK3β, MARK4, PIM1, PIM3, PLK3) by over 75% at 10 μM among a panel of 271 other kinases. FINDY (2.5 μM) is shown to selectively rescue the developmental defect of Xenopus embryos induced by the overexpression of DYRK1A, but not DYRK1B, while INDY prodrug (2.5 μM) treatment indiscriminately prevents defect caused by both DYRK1A and DYRK1B expression.
 
F5807 FIPI hydrochloride hydrate ≥98% (HPLC), powder FIPI is a potent Phospholipase D (PLD) inhibitor. The signaling enzyme Phospholipase D (PLD) and the lipid second messenger phosphatidic acid (PA) generated by PLD are implicated in many cell biological processes including Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a potent in vivo inhibitor of both PLD1 and PLD2, setting the stage for a new era of exploration and validation of cell biological roles for mammalian PLD. It rapidly blocks in vivo PA production with sub-nM potency. FIPI inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis, indicating potential utility for it as a therapeutic for autoimmunity and cancer metastasis. It does not affect PLD subcellular localization, PIP2 availability, the actin stress fiber network in resting CHO cells, or selected signaling events proximal to PLD activation.
FIPI is a potent phospholipase D (PLD) inhibitor effective at sub-nM levels. Phospholipase D (PLD) and the lipid second messenger phosphatidic acid (PA) generated by PLD are implicated in many cell biological processes including Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI inhibits both PLD1 and PLD2, rapidly blocking in vivo PA production. FIPI inhibits PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis, suggesting potential as a therapeutic for autoimmune diseases and cancer metastasis.
 
F4679 FK-506 monohydrate ≥98% (HPLC) FK-506 also appears to inhibit Na+/Ca2+ exchange. FK-506 and its derivatives demonstrate significant neurodegenerative activity. This property seems to arise via different mechanisms. FK-506 is also useful in treating ophthalmologic complications such as corneal graft rejection, uveoretinitis and allergen induced conjunctivitis.
FK-506 is a potent immunosuppressant, neuroprotective and neuroregenerative, and in vitro T cell proliferation blocker. FK-506 disrupts calcineurin-mediated signal transduction in T lymphocytes and interacts with its FK-506-binding protein-12 (FKBP12).
human ... FKBP1A(2280)
F8557   FK866 hydrochloride hydrate ≥98% (HPLC) FK866 is a potent inhibitor of NAD biosynthesis, and a specific inhibitor of NAMPT (Nicotinamide Phosphoribosyltransferase, visfatin, PBEF). NAMPT functions as an intra-cellular and extra-cellular NAD biosynthetic enzyme that is important for regulating metabolism and stress resistance through sirtuins and other NAD-consuming regulators. NAMPT also acts as a cytokine independent of its enzymatic activity, playing a major part in regulating immune responses.
 
F1183 FK888 hydrate Selective, high affinity tachykinin NK1 receptor antagonist.
 
SML0707   FKGK11 ≥98% (GC) FKGK11 is a potent inhibitor of GVIA iPLA2 with little or no inhibition against GIVA cPLA2 (XI(50) = 0.0073 and >0.91, respectively). The compound displays a slight inhibition against GVsPLA2. FKGK11 potently inhibited the progression and severity in a murine experimental autoimmune encephalomyelitis (EAE) model.
 
F3055 Flavopiridol hydrochloride hydrate ≥98% (HPLC), powder Flavopiridol hydrochloride is a potent CDK (cyclin-dependent kinase), and a CDC25 phosphatase family inhibitor.
 
F8304 Flavoxate hydrochloride ≥98% (HPLC), solid L-type Ca2+ (Cav1.2) channel inhibitor
 
F6777 Flecainide acetate salt Class IC antiarrhythmic agent; sodium channel blocker
 
SML0975   FLI-06 ≥98% (HPLC) FLI-06 is an inhibitor of Notch signaling. FLI-06 acts upstream of α-secretase and β-secretase cleavage, disrupting intracellular trafficking and processing of the Notch signaling pathway and inhibiting general secretion at a step before exit from the endoplasmic reticulum (ER). This inhibition is accompanied by a tubule-to-sheet morphological transition of the ER. FLI-06 does not act on the cytoskeleton, but causes a complete disruption of the Golgi in a manner different from that of Brefeldin A or Golgicide A. FLI-06 is the first compound acting that early in the secretory pathway.
 
SML0797   Flibanserin ≥98% (HPLC) Flibanserin is a 5-HT1A receptor agonist and 5-HT2A receptor antagonist. Flibanserin has high affinity for human 5-HT1A receptors (Ki = 1 nm) and lower affinity for 5-HT2A (Ki = 49 nm) and D4 (Ki = 4–24 nm) receptors, and negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin was investigated as a novel, non-hormonal treatment for pre-menopausal women with Hypoactive Sexual Desire Disorder (HSDD). Flibanserin. Recently, Flibanserin was found to reduce L-DOPA-induced dyskinesia in a model of Parkinson′s Disease.
 
F9057 FLLL31 ≥98% (HPLC) FLLL31 selectively binds to Janus kinase 2 and the STAT3 Src homology-2 (SH2) domain, effective inhibitors of STAT3 phosphorylation. STAT3 plays a critical role in early embryogenesis, but is largely dispensable in normal adult cells and tissues. On the other hand the JAK2/STAT3 signaling pathway is persistently activated in great number of human solid and blood cancers. Such activation is commonly associated with a worse prognosis. FLLL31 is a curcumin derivative locked in diketone-tautomeric form, which supposedly improves binding to SH2 domain. The compound inhibits JAK2 kinase activity and prevents STAT3 phosphorylation. FLLK31 is a potent and selective inhibitor of the STAT3 signaling pathway.
 
SML1023   Flucloxacillin sodium ≥95% (HPLC) Flucloxacillin is a narrow-spectrum β-lactam antibiotic used to treat Gram-positive bacterial infections. Flucloxacillin induces cholestatic liver damage.
 
F8929 Fluconazole ≥98% (HPLC), powder Fluconazole is an antifungal agent. It is highly selective inhibitor of fungal cytochrome P-450 sterol C-14 α-demethyllation. Fluconazole is a potent inhibitor of CYP2C9. Fluconazole interferes with fungal ergosterol synthesis and downregulates the metallothionein gene.
human ... CYP1A2(1544)
F6127 Fludrocortisone acetate ≥98% Fludrocortisone acetate is a synthetic corticosteroid with more mineralocorticoid than glucocorticoid activity.
 
F6300 Flumazenil >99% (HPLC), solid Highly specific benzodiazepine receptor antagonist.
human ... BZRAP1(9256), GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA5(2558), GABRA6(2559), GABRG2(2566)
rat ... Gabra2(29706), Gabrg1(140674)
F8257 Flunarizine dihydrochloride ≥98% (TLC) Blocks T-type Ca2+/Na+ channels; inhibits K+-induced catecholamine release from chromaffin cells
 
F5021 Flunisolide ≥97%    
F9261 Flunitrazepam Hypnotic; anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA5(2558), GABRA6(2559)
rat ... Gabra2(29706)
F0429 Flunixin meglumine ≥98% (HPLC) COX1, COX2 and PLA2 inhibitor non-narcotic analgesic, anti-pyretic, anti-inflammatory.
 
SML0099 Fluocinonide ≥98% (HPLC) Flucinonide is a fluorinated glucocorticid that is used as a topical anti-inflammatory agent. Recently, flucinonide and other fluorinated glucocorticolids were identified as smoothend agonists. Flucinonide induces expression of Gli-reporter luciferase in Shh-LIGHT2 cells.
Fluocinonide has been used to study its effect on T-cell proliferation.
Fluocinonide is shown to be effective in the treatment of atopic dermatitis and oral lichen planus (OLP).
 
SML0155   Fluorescent Adenosine receptor Agonist (A-633-AG) synthetic    
SML0156   Fluorescent Adenosine receptor Antagonist (A-633-AN) synthetic The SML0156 ligand was shown to antagonize the activity of the adenosine receptor agonist adenosine-5’-N-ethyluronamide (NECA), in three separate recombinant CHO cell lines expressing the human A1, A2A or A3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.
 
SML0158   Fluorescent β2 adrenoceptor Agonist (β2-633-AG) synthetic The SML0158 agonist was shown to induce a reporter gene response, in two separate recombinant CHO cell lines expressing either the human β1 or β2 adrenoceptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene. This response was antagonized by either the ?1-selective antagonist CGP 20712A in the human β1 cell line, or the ?2-selective antagonist ICI 118551 in the human β2 cell line, respectively.
 
SML0160   Fluorescent Beta-2 Adrenoceptor Antagonist (β2-633-AN) synthetic The SML0160 ligand was shown to antagonize the activity of the non-selective β agonist, isoprenaline, in three separate recombinant CHO cell lines expressing either the human β1, β2 or β3 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.
 
SML0159   Fluorescent Beta-2 Adrenoceptor Antagonist (β3-633-AN3) synthetic The SML0159 ligand is an antagonist at β2, β1 and β3 adrenoceptors (in rank order of affinity).
 
SML0162   Fluorescent Beta-2 Adrenoceptor Antagonist (β3-633-AN4) synthetic The SML0162 ligand is an antagonist at β2, β1 and β3 adrenoceptors (in rank order of affinity).
 
SML0164   Fluorescent Dopamine D1 receptor Antagonist (D1-633-AN2) synthetic The SML0164 ligand was shown to antagonize the activity of the D1 agonist, SKF 83566, in a recombinant CHO cell line expressing the human D1 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.
 
SML0165   Fluorescent GABA-B receptor Antagonist (GB-633-AN) synthetic The SML0165 ligand was shown to antagonize the activity of the GABA-B agonist, GABA, in a recombinant CHO cell line expressing the human GABA-B1 and GABA-B2 receptors and a serum-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.
 
SML0167   Fluorescent Histamine H2 receptor Antagonist (H2-633-AN) synthetic The SML0167 ligand was shown to antagonize the activity of the H2 agonist, histamine, in a recombinant CHO cell line expressing the human H2 receptor and a cyclic AMP-responsive secreted placental alkaline phosphatase (SPAP) reporter gene, and in a similar cell line expressing the human H3 receptor.
 
SML0168   Fluorescent Histamine H3/H4 receptor Antagonist (H3-633-AN) synthetic The SML0168 ligand was shown to antagonize the activity of the histamine agonist, histamine, in two separate recombinant CHO cell lines expressing either the human H2 or H3-receptor and a cyclic-AMP responsive secreted placental alkaline phosphatase (SPAP) reporter gene.
 
SML0169   Fluorescent Muscarinic M3 receptor Antagonist (M3-633-AN synthetic The SML0169 ligand was shown to antagonize the activity of the muscarinic agonist, carbachol, in a recombinant CHO cell line expressing the human M3 receptor and a serum-responsive secreted placental alkaline phosphatase (SPAP) reporter gene.
 
SML0170   Fluorescent 5HT-1A receptor Antagonist (5HT1A-633-AN2) synthetic The SML0170 ligand was shown to antagonize the activity of the 5 HT1A agonist, 5-HT, in the ChanTest CHO cell line expressing the human 5-HT1A receptor, using the Ca++ sensitive fluorescent indicator, Fura-2 AM.
 
SML0754   3-Fluoroamphetamine hydrochloride ≥98% (HPLC) 3-Fluoroamphetamine hydrochloride is a monoamine releaser and potential designer drug derivative of amphetamine.
 
F2927 1-(4-Fluorobenzyl)-5-methoxy-2-methylindole-3-acetic acid ≥98% (HPLC), solid Putative inhibitor of multidrug resistance-associated protein 1 (MRP1).
human ... ABCC1(4363)
F6301 Fluorocurarine chloride ≥97% (TLC), from Vinca erecta, solid Short-acting selective sympathetic ganglioblocker with weak antagonist activity on the nicotinic receptor at the neuromuscular junction; hypotensive.
 
F5307 5−Fluoro−2′−deoxycytidine ≥98% (HPLC), powder 5-Fluoro-2′-deoxycytidine is a mechanism based DNMT (DNA cytosine-5 methyltransferase) inhibitor, that forms a covalent link with the cysteine residue in the active site of DNMT.
 
F8791 5-Fluoro-5′-deoxyuridine Doxifluridine is an antitumor agent efficient in tumors, cell lines or in fibroblasts transformed by H-ras or trk oncogenes. Possesses anticachectic activity which is independent of its antiproliferative activity.
 
H127 p-Fluorohexahydro-sila-difenidol hydrochloride powder, ≥98% (HPLC) High affinity M3 muscarinic acetylcholine receptor antagonist.
human ... CHRM3(1131)
F2929 6-Fluoromevalonate ≥90% (GC), viscous liquid Mevalonate-pyrophosphate decarboxylase inhibitor
 
SML1162 5-Fluoro-1-propargyl-uracil ≥98% (HPLC) 5-Fluoro-1-propargyl-uracil is a biologically inert precursor, a prodrug that can be bioorthogonally activated to 5-fluorouracil iside a tumor that has a previously implanted palladium catalyst. Preliminary tests with pancreatic and colorectal cancer cells resulted in the death of than 80% of the malignant cells.
 
F132 Fluoxetine hydrochloride solid Fluoxetine hydrochloride is a selective serotonin reuptake inhibitor and functions as an antidepressant. This drug works at presynaptic terminals where it prevents the reuptake of serotonin, resulting in the accumulation of serotonin in extracellular fluid at synapses.
Selective serotonin reuptake inhibitor; antidepressant.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
F1678 R-(−)-Fluoxetine hydrochloride >98% (HPLC), solid Selective serotonin reuptake inhibitor.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
F1553 S-(+)-Fluoxetine hydrochloride ≥98% (HPLC), solid Fluoxetine hcl (hydrochloride) is a selective serotonin reuptake inhibitor and functions as an antidepressant. This drug works at presynaptic terminals where it prevents the reuptake of serotonin, resulting in the accumulation of serotonin in extracellular fluid at synapses.
Selective serotonin reuptake inhibitor.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
F4765 Fluphenazine dihydrochloride D1/D2 dopamine receptor antagonist; phenothiazine antipsychotic; H1 histamine receptor antagonist.
human ... DRD1(1812), DRD2(1813), HRH1(3269)
F8927 Flupirtine maleate salt ≥98% (HPLC) Flupirtine is commercially available as maleate salt. It exists in two polymorphs : flupirtine maleate A and B. Flupirtine is useful in treating muscular spasm, muscle tension and muscle stiffness. It is known to be effective in relieving back pain. Along with cytoprotection, flupirtine also offers protection against neurodegenerative disorders such as multiple sclerosis, amyotrophic lateral sclerosis, Alzheimer′s disease, Parkinson′s disease, Huntington′s chorea and AID (acquired immunodeficiency) associated encephalopathy. Flupirtine is found to be a potential drug for eye-related problems like maculopathy including diabetic retinopathy, retinitis pigmentosa and glaucoma. It is also proved to be helpful in preventing cardiac associated disorders such as myocardial ischemia and infarction, cerebral ischemia and infarction. Hepatitis is also prevented by the use of flupirtine.
Non-opioid analgesic; cytoprotective versus PrP fragment 106-126
 
F8549 Fluprostenol 10 mg/mL in ethanol, 98%    
F2427 Fluprostenol isopropyl ester ≥98%, ethanol solution Potent FP prostanoid receptor agonist used in animal models for glaucoma.
 
F100 Fluspirilene Dopamine receptor antagonist; antipsychotic; calcium channel blocker.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
F9397 Flutamide Flutamide is a non-steroidal anti-androgen.
human ... AR(367)
mouse ... Ar(11835)
rat ... Ar(24208)
F9428 Fluticasone propionate ≥98% (HPLC), powder Fluticasone propionate is a second generation glucocorticoid. Used as an anti-inflammatory agent for asthma. Shown to enhance eosinophil apoptosis in a concentration-dependent manner via the glucocorticoid receptor.
 
SML0038 Fluvastatin sodium hydrate ≥98% (HPLC) Fluvastatin has antifungal activity.
Fluvastatin is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Fluvastatin is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
 
F2802 Fluvoxamine maleate solid Selective serotonin reuptake inhibitor; antidepressant.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
F8807 FM19G11 ≥98% (HPLC) FM19G11 is an inhibitor of Hypoxia Inducible Factors α (HIFα), reported to affect self-renewal and differentiation of stem cells. Hypoxia-inducible factors (HIFs) are transcription factors that respond to changes in available oxygen in the cellular environment. Among other functions (like angiogenesis), HIFα proteins affect the self-renewal and the differentiation processes of stem cells. FM19G11 inhibits the HIFα proteins that repress the target genes of the two α subunits, in various tumor cell lines as well as in adult and embryonic stem cell (ESC) models.
 
SML1979 FM-381 ≥98% (HPLC) FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor (IC50 = 127 pM/JAK3, 52 nM/JAK1, 346 nM/JAK2, 459 nM/TYK2 by radiometric assay; [ATP] = 10 μM) that targets JAK3 gatekeeper (GK) Cys909 for a reversible covalent interaction, exhibiting much reduced or little potency against a panel of 409 other kinases. FM-381 is >3-fold more potent than the JAK1/3 inhibitor Tofacitinib (IC50 = 292 pM/JAK3, 496 pM/JAK1, 2.2 nM/JAK2, 8.9 nM/TYK2 by radiometric assay; [ATP] = 10 μM) in blocking JAK1/JAK3-mediated STAT5 phosphorylation in human CD4+ T-cells upon IL-2 stimulation (ECmax ∼100 nM with FM-381), while being ineffective (up to 1 μM) against JAK3-independent STAT1/3 phosphorylation following IL-6 or TNFα stimulation. For characterization details of FM-381, please visit the FM-381 probe summary on the Structural Genomics Consortium (SGC) website.

FM-479 is the negative control for the active probe, FM-381. FM-479 is available from Sigma. To learn more about and purchase FM-479, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc
 
SML1992 FM-479 ≥98% (HPLC) FM-479 is an FM-381 structural analog that exhibits no inhibitory potency against JAK3 or other kinases when used at the FM-381 effective dosing range of 100-300 nM. For characterization details of the active probe, FM-381, please visit the FM-381 probe summary on the Structural Genomics Consortium (SGC) website.

FM-381, the active probe, is available from Sigma. To learn more about and purchase FM-381, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc
 
SML0380 FMP-API-1 ≥98% (HPLC) FMP-API-1 is an inhibitor of AKAP-PKA interactions in vitro and in cultured cardiac myocytes that activates PKA. Apparently, FMP-API-1 binds to a novel allosteric regulatory site.
 
SML1240   Fondaparinux sodium ≥95% (HPLC) Fondaparinux sodium is an antithrombotic anticoagulant, a Factor Xa inhibitor. Fondaparinux sodium is chemically related to low molecular weight heparins. Its pentasaccharide structure corresponds to the antithrombin III (ATIII) binding site of heparin. Fondaparinux sodium binding at this site potentiates the natural inhibitory effect of ATIII against factor Xa by a factor of approximately 300, which results in inhibition of thrombin generation.
 
F9552 Formoterol fumarate dihydrate >98% (HPLC) β2-Adrenoreceptor agonist.
Formoterol fumarate dihydrate can be used along with budesonide to treat asthma.
human ... ADRB2(154)
F6886 Forskolin from Coleus forskohlii, ≥98% (HPLC), powder Cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties. Many of its biological effects are due to its activation of adenylyl cyclase and the resulting increase in intracellular cAMP concentration. Forskolin effects calcium currents and inhibits MAP kinase.
human ... OPRK1(4986), SLC2A10(81031), TNF(7124)
SML2101 Fosamprenavir calcium ≥98% (HPLC) Fosamprenavir calcium is an HIV protease inhibitor anti-retroviral. It is a water soluble phosphate ester prodrug of amprenavir, the active agent.
 
SML2228 Fosaprepitant dimeglumine ≥98% (HPLC) Fosaprepitant dimeglumine is a Substance P/neurokinin-1 (NK1) receptor antagonist. It is a water soluble prodrug of the antiemetic drug aprepitant.
 
F1308 Fosinopril sodium ≥98% (HPLC), powder Fosinopril is an angiotensin converting enzyme (ACE) inhibitor. Fosinopril is also known to inhibit the activity of the peptide transporter PEPT2.
 
F8682 Fosmidomycin sodium salt hydrate ≥95% (NMR) Fosmidomycin is an inhibitor of 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR) (MEP synthase): an antimalarial compound. 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR) is an enzyme involved in the first step in the nonmevalonate pathway for isoprenoid biosynthesis in Gram-negative, Gram-positive bacteria, plants, and the parasite causing the most virulent form of malaria, Plasmodium falciparum (Mammals produce isoprenoids via the mevalonate pathway).
 
SML0117 Fosphenytoin disodium salt hydrate ≥98% (HPLC) Fosphenytoin is a water soluble phenytoin prodrug.
 
F4425 Fostriecin sodium salt from Streptomyces pulveraceus ≥98% (HPLC) Fostriecin was discovered as an anti-tumor antibiotic isolated from the fermentation beer of Streptomyces pulveraceus (subspecies fostreus). Fostriecin has antitumor activity against a wide spectrum of tumor cells in vitro and excellent activity against P388 and L1210 leukemias in vivo. The antitumor activity of fostriecin originates from its ability to interfere with the reversible phosphorylation of proteins that are critical for progression through the cell cycle.
 
F7307 Fotemustine ≥98% (HPLC) Fotemustine is a third generation nitrosourea, chloroethylating agent used in the treatment of glioma and malignant melanoma.
 
SML0827   FPH1 ≥98% (HPLC) FPH1 (BRD-6125) induces functional proliferation of primary human hepatocytes in vitro. Human induced pluripotent stem (iPS) cells can be differentiated toward hepatocyte-like (iHep) cells, but replication is not great, and cells typically show an immature hepatic phenotype and have limited use as a renewable source of functional human hepatocytes. FPH1 induced hepatocyte colonies were used in conjunction with FH1 (BRD-K4477) to induce a more mature phenotype. Cultures treated with both FH1 and FPH1 contained larger colonies of hepatocyte-like (iHep) cells, which showed more pronounced hepatocyte morphologies with a more mature phenotype than previously obtainable.
 
SML0828   FPH2 ≥98% (HPLC) FPH2 (BRD-9424) induced functional proliferation of primary human hepatocytes in vitro. Human induced pluripotent stem (iPS) cells can be differentiated toward hepatocyte-like (iHep) cells, but replication is not great, and cells typically show an immature hepatic phenotype and have limited use as a renewable source of functional human hepatocytes. FPH2 induced hepatocyte doublings at a rate consistent with reported liver regeneration kinetics. FPH2 can be used in conjunction with FH1 (BRD-K4477), which induces a more mature phenotype.
 
F1179 FPL-55712 ≥97% (HPLC), solid CysLT1 leukotriene receptor antagonist.
 
F131 FPL 64176 ≥98% (HPLC), powder Potent Ca2+ channel (L-type) activator.
rat ... Cacnb3(25297)
SML1943 FPMINT ≥98% (HPLC) FPMINT is a potent, irreversible and non-competitive inhibitor of equilibrative nucleoside transporters ENT1 and ENT2. FPMINT is more selective for ENT2 than ENT1.
 
SML0413 FQI1 ≥98% (HPLC) FQI1 inhibits the DNA-binding activity of LSF, a ubiquitous transcription factor that is up regulated in many hepatocellular carcinomas (HCC). FQI1 inhibits LSF-dependent luciferase reporter expression, blocks proliferation in cancer cell lines, and induces apoptosis in liver cancer cells but is not toxic to primary hepatocytes. FQI1 also inhibits tumor growth in a mouse HCC xenograft model.
 
F7553 FR 122047 hydrochloride ≥98% (HPLC), powder Selective cyclooxgenase-1 (COX-1) inhibitor.
 
SML0028 FR-171113 ≥98% (HPLC) FR171113 was the first non-peptide antagonist of the Protease Activated Receptor-1 (PAR1), also termed thrombin receptor. FR171113 inhibits either thrombin or TRAP-6-induced platelet aggregation (IC50 = 290 and 150 nM, respectively). The compound does not affect the protease activity of thrombin or clotting time.
 
SML0320 FR180204 ≥98% (HPLC) FR180204 is a potent, cell-permeable, ATP-competitive inhibitor of ERK1 and ERK2 (mitogen-activated protein kinase (MAPK)/extracellular-signal-regulated kinases (ERK) 1/2).
 
SML2113 FR194921 ≥98% (HPLC) FR194921 is a blood-brain barrier-permeable A1R adenosine receptor antagonist. The measured Ki values of FR194921 for the human adenosine A1 receptors have been in the low nM range with no binding affinity for A2A and A3 receptors up to 1μM. It is orally active and has good bioavailability. FR194921 was used in a recent study to restore auditory cortex plasticity. Paired with sound exposure, FR194921 resulted in cortical map plasticity and improved auditory perception in adult mice.
 
F8307 FR-900098 monosodium salt ≥97% (NMR) 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR) is an enzyme involved in the first step in the nonmevalonate pathway for isoprenoid biosynthesis in Gram-negative, Gram-positive bacteria, plants, and the parasite causing the most virulent form of malaria, Plasmodium falciparum (Mammals produce isoprenoids via the mevalonate pathway). Inhibiton of the enzyme provides alternative to traditional antimalaria therapy. FR-900098 is twice more effective than fosmidomycin against various strains of P. falciparum in vitro and the closely related P. vinckei in mice.
 
SML2270 FRAX486 ≥98% (HPLC) FRAX486 is a potent, group I-selective p21-activated kinase (PAK) inhibitor (PAK1/2/3 IC50 = 8.25/39.5/55.3 nM; group II PAK4 IC50 = 779 nM). FRAX486 effectively inhibits PAK-mediated PKD1 Ser203 phosphorylation and PAK1/2 Ser144/141 autophosphorylation upon angiotensin II (ANGII) stimulation of rat IEC-18 cells (IC50 ∼0.5 μM) and exhibits in vivo efficacy in rescuing the autism-like phenotypes among Fmr1 knockout fragile syndrome (FXS) mice (20 mg/kg s.c.) as well as in ameliorating schizophrenia-associated dendritic spine deterioration among Disc1 knockdown mice (10 μg/g or 10 mg/kg i.p.) with good pharmacokinetic properties and blood–brain barrier (BBB) permeability.
 
SML1291 Frovatriptan succinate monohydrate ≥97% (HPLC) During migraine condition, frovatriptan succinate monohydrate acts on extra cerebral, intracranial arteries and prevent excessive dilation of these vessels.
Frovatriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine. Frovatriptan has high affinity for the 5-HT(1B) and 5-HT(1D) receptors while affinity for 5-HT receptors other than 5-HT(1B/1D) is substantially lower with a pEC50 value of 8.2 for the 5-HT1B receptor, compared to a pEC50 value of 6.2 for the 5-HT7 receptor.
 
SML1420   FSL-1 ≥80% (HPLC) FSL-1 (Pam2CGDPKHPKSF) is a synthetic lipoprotein that acts as a Toll-like Receptor 2/6 (TLR2/6) agonist and activator of nuclear transcription factor NF-KB. FSL-1 is based on the N-terminal part of the 44-kDa lipoprotein LP44 of Mycoplasma salivarium. FSL-1 showed higher stimulatory activity than MALP-2 in its ability to induce TNF-α production in macrophages and NF-κB in TLR2/TLR6 transfected HEK293 cells.
 
SML0714   FSLLRY-NH2 trifluoroacetate salt ≥98% (HPLC) FSLLRY-NH2 is a peptide antagonist of the protease activated receptor 2 (PAR2). The peptide blocks agonist induced itching in rodent models. In cell based assays, the peptide inhibits agonist-induced cardiocyte remodeling, and production of cytokines by endothelial cells.
 
SML2242 FTBMT ≥98% (HPLC) FTBMT is an orally available, selective and potent agonist of GPR52. It exhibits antipsychotic and procognitive properties without causing catalepsy in rodents. FTBMT improves recognition memory in a novel object recognition test and mitigates MK-801-induced working memory deficits in a radial arm maze test in rats.
 
F9553 FTI-276 trifluoroacetate salt ≥95% (HPLC) FTI-276 is a highly potent RasCAAX peptidomimetic. FTI-276 antagonizes both H and K-Ras oncogenic signaling. It is an inhibitor of farnesyltransferase (Ftase) in vitro with an IC50 of 500 pM and is an anti-cancer agent.
 
F9803 FTI-277 trifluoroacetate salt ≥95% (HPLC), film Farnesyltransferase inhibitor 277 (FTI-277) mediates apoptosis in multiple myeloma and is regarded as a potential therapeutic agent.
Highly potent (pM/nM) Ras CAAX peptidomimetic which antagonizes both H and K-Ras oncogenic signaling. Inhibitor of farnesyltransferase (Ftase) IC50 = 50 nM.
 
SML0700   FTY720 ≥98% (HPLC) FTY720 is an immunomodulating drug and sphingosine 1-phosphate (S1P) receptor modulator. Phosphorylation of FTY270 by sphingosine kinase causes S1P1R internalization, which sequesters lymphocytes in lymph nodes, preventing them from taking part in an autoimmune response. Clinically, it has been approved for the treatment of multiple sclerosis (MS). It has also been shown to block and reverse paclitaxel-induced chemotherapy induced peripheral neuropathy (CIPN) through S1PR inhibition as well as inhibit the activity of histone deacetylases in the hippocampus of mouse brains, thereby modulating memory.
 
SML0377   (S)-FTY720 phosphate ≥94% (HPLC) FTY20 phosphate (FTY720-P) is a sphingosine 1-phosphate (S1PR) receptor agonist and immunomodulatory agent, the active metabolite of FTY720. FTY720P acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5), with IC50 values of 0.2-6 nM.
 
F5379 Fucosterol ≥93%    
I4409 Fulvestrant >98% (HPLC) Fulvestrant (ICI 182,780) is a selective estrogen receptor down-regulator (SERD). Fulvestrant is a high affinity estrogen receptor antagonist. IC50 = 0.29 nM. Fulvestrant is the first "pure" antiestrogen with no agonistic activity both in vitro and in vivo.
Fulvestrant is a 7α-alkylsulphinyl analog of 17β-oestradiol and is structurally different compared to other selective estrogen receptor (ER) modulators (SERMs). It reduces dimerization and nuclear localization of the estrogen receptor (ER). Fulvestrant lowers the level of ER protein in human breast cancer cells. Fulvestrant is preferred for the treatment of women at their menopause having hormone-sensitive advanced breast cancer.
 
F6771 Fumagillin from Aspergillus fumigatus ≥90%, powder Methionine aminopeptidase-2 (MetAP-2) inhibitor; inhibits endothelial cell proliferation and angiogenesis.
 
F9054 Fumitremorgin C from Neosartorya fischeri, film Fumitremorgin C (FTC) is a fungal toxin of the diketopiperazines family of compounds. In mammalian cells, FTC is tremorgenic and causes cell cycle arrest. Fumitremorgin C has been shown to reverse resistance to doxorubicin, mitoxantrane, and topotecan in non-Pgp (P-glyco­protein), non-MRP (multidrug resistance protein) multidrug-resistance (MDR) cells. This reversal of resistance is associated with an increase in drug accumulation. Fumitremorgin C is a specific, selective, and potent inhibitor at micromolar concentrations of the breast cancer resistant protein (BCRP/ABCG2), an ABC transporter associated with chemotherapy resistance. FTC, in combination with mitoxantrone, can be used for the detection of ABCG2 functional activity in several cell lines.
 
O003 β-Funaltrexamine hydrochloride solid Selective irreversible μ opioid receptor antagonist that is also a κ opioid receptor agonist.
 
F124 Furafylline ≥98% (HPLC) Furafylline is a methyl xanthine derivative with longer duration of action than theophylline and an inhibitor of cytochrome P4501A2.
human ... CYP1A2(1544)
F9130 Furaltadone    
F9380 Furaltadone (+)-tartrate salt    
SML1559   Furamidine dihydrochloride ≥98% (HPLC) Furamidine (DB75) binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine was originally developed as an anti-parasitic compound for a variety of diseases including Chagas′ disease. Furamidine targets AT rich sequences in trypanosome kinetoplast minicircle DNA (kDNA), resulting in subsequent destruction of the kinetoplast and cell death. Furamidine has also been found to inihbit tyrosyl-DNA phosphodiesterase (Tdp1) and act as a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4μM.
 
F4381 Furosemide "High ceiling" diuretic that strongly affects renal tubular action by increasing renal blood flow; antihypertensive.
Furosemide can block the Na+/K+/2Cl- co-transporter in the ascending thick loop of Henle. It can enhance the synthesis of intrarenal prostaglandin. It enhances its ototoxicity in animals when used along with kanamycin. Furosemide is linked with thiamine insufficiency in individuals with heart failure.
Inhibits ion co-transport in the kidney.
human ... ALB(213), CYP1A2(1544), SLC12A1(6557)
F6513 Fusaric acid from Gibberella fujikuroi Dopamine β-hydroxylase inhibitor.
human ... DBH(1621)
F0756 Fusidic acid Suppresses nitric oxide lysis of pancreatic islet cells. Inhibits protein synthesis in prokaryotes by inhibiting the ribosome-dependent activity of G factor and translocation of peptidyl-tRNA.
 
F0881 Fusidic acid sodium salt ≥98% (TLC) Suppresses nitric oxide lysis of pancreatic islet cells. Inhibits protein synthesis in prokaryotes by inhibiting the ribosome-dependent activity of G factor and translocation of peptidyl-tRNA.
 
SML2074   FX1 ≥98% (HPLC) FX1 is a BCL6 inhibitor that effectively blocks BCL6 N-terminal BTB domain-mediated corepressors chromosome recruitment (by 61-87%/SMRT and 67-82%/BCOR; 50 μM FX1 for 30 min) and selectively suppresses BCL6-depenent growth (GI50 16-54 μM; >125 μM against BCL6-independent cells) in diffuse large B cell lymphoma (DLBCL) cultures, exhibiting greater affinity than its structure analog 79-6 or BCL6 corepressor SMRT for BTB domain (KD = 7 μM/FX1, 30 μM/SMRT, 129 μM/79-6). FX1 shows greater efficacy than 79-6 in reversing BCL6/corepressors-mediated target genes repression in vitro (IC50 = 35 μM vs. 318 μM with 79-6 by HEK293T-based reporter assay) and in suppressing OCI-Ly7 DLBCL xenograft tumor growth mice in vivo (100% vs. 45% suppression with respective compound via 25 mg/kg/day i.p.).
 
SML1481 FzM1 ≥98% (HPLC) FzM1 is an allosteric ligand of the Frizzled4 (Fz4) receptor and a Wnt/β-catenin pathway inhibitor, found by a screen for pharmacological chaperones for a misfolded mutant of the Frizzled4 (Fz4) receptor. FzM1 is believed to induce conformational changes in Fz4 by interacting with the third intracellular loop, ICL3, inhibiting binding of dishevelled (Dsh) and hampering the formation of the Fz4-Dsh complex that is necessary for β-catenin nuclear transport and ultimately transcription of TCF/LEF-regulated genes. FzM1 was tested on two tumor cell lines. U87MG glioblastoma cells acquired a more differentiated phenotype on application. FzM1 and FzM1alk also sped up the differentiation of Caco-2 cells. FzM1 has a log EC50 value of 5.74 for inhibition of Wnt antagonism.