Benzylthiouracil is an active pharmaceutical ingredient against hyperthyroidism[1].
Nile Blue Methacrylamide is a Nile Blue-based nanosized pH densor that can be used for simultaneous far-red and near-infrared live bioimaging[1].
IL-17 modulator 4 is a prodrug of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator[1].
Picarbutrazox is a potent pesticide and fungicide. Picarbutrazox can be used for corn and soybean to control Pythium and Phytophthora. Picarbutrazox can be used in agricultural production and control[1][2].
Oligo-1,6-glucosidase belongs to the α-amylase family that catalyzes the exo hydrolysis of α-1,6-glucoside bonds from the nonreducing ends of panose, palatinose, α-limit dextrins, and isomaltooligosaccharides[1].
Pyraflufen-ethyl is a phenylpyrazole herbicide for control of annual and perennial broadleaf weeds[1].
Tenofovir Disoproxil Fumarate is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic Hepatitis B.
SR 142948 is an orally active, potent and selective non-peptide neurotensin receptor (NT1R) antagonist. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT 29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability, can be used in study of psychiatric disorders[1][2].
Fulzerasib is a potent KRAS inhibitor[1].
PRMT5-IN-32 is an inhibitor of PRMT5. PRMT5-IN-32 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM[1].
Ibutilide Fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm.Target: Calcium ChannelIbutilide is the first 'pure' class III antiarrhythmic drug to become available. Its predominant action is prolongation of the myocardial action potential duration. Intravenous ibutilide 0.01 to 0.025 mg/kg or 1 to 2 mg successfully converted atrial flutter or fibrillation to sinus rhythm in 33 to 49% of patients in 2 placebo-controlled trials involving 439 patients with sustained arrhythmia [1]. Ibutilide appears to be an effective alternative method for rapid conversion of recent-onset AF or AFl. The drug may be particularly useful in patients who have undergone recent cardiac surgery or those who are not ideal candidates for DCC [2].
Z-D-Lys-OH is a lysine derivative[1].
Butoconazole nitrate is an anti-fungal agent.Target: Antifungalbutoconazole 1-BSR is an effective and safe alternative to longer-term therapy with miconazole nitrate (seven days) for vulvovaginal candidiasis [1]. A sustained-release (SR) bioadhesive vaginal cream (2% butoconazole nitrate) has incorporated VagiSite technology, a topical drug delivery system that allows SR of the drug [2].
Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras)[1].
Diphemanil methylsulfate is a quaternary ammonium anticholinergic. It binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stomach acids as well as saliva and sweat.IC50 value: Target: mAChRDiphemanil Methylsulfate exerts its action by primarily binding the muscarinic M3 receptor. M3 receptors are located in the smooth muscles of the blood vessels, as well as in the lungs. This means they cause vasodilation and bronchoconstriction. They are also in the smooth muscles of the gastrointestinal tract (GIT), which help in increasing intestinal motility and dilating sphincters. The M3 receptors are also located in many glands which help to stimulate secretion in salivary glands and other glands of the body.
LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM[1].
Acetyl-pepstatin is a high affinity aspartic protease inhibitor. Acetyl-pepstatin inhibits HIV-1 protease (Ki=20 nM at pH 4.7) and HIV-2 protease (Ki= 5 nM at pH 4.7). Antiviral.
L-Methionine γ-lyase (Methionine lyase) is a multifunctional enzyme, which belongs to the γ-family of pyridoxal-5’-phosphate (PLP) dependent enzyme. L-Methionine γ-lyase can catylyse α, γ-elimunation of L-methionine and homocysteine. L-Methionine γ-lyase has anticancer and anti-infectious activity, and also can be used for homocysteinemia study[1][2][3].
Lademirsen (SAR339375; RG-012) is a highly specific antisense oligonucleotide (ASO) targeting miR-21. Lademirsen has the potential for Alport nephropathy research[1][2].
Monobehenin has a strong inhibitory activity toward bacterial biofilm formation.
Sulfamethomidine is an antibacterial agent[1].
MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
Silver sulfadiazine (AgSD), a sulfonamide antibiotic, effects a dual inhibitory action on bacterial growth by its sulfa moiety (SD-SDZ) that prevents bacterial folate absorption and subsequent DNA synthesis. The silver that is released from Silver sulfadiazine binds and disrupts the DNA structure, precluding bacterial DNA replication[1].
Boc-NH-PEG2-C2-NHS ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ono 3403 is a synthetic serine protease inhibitor. Ono 3403 inhibits lipopolysaccharide-induced tumor necrosis factor-alpha and nitric oxide production. ONO-3403 also has an antitumor effect on malignant tumors.
(+)-Ketoconazole is an imidazole anti-fungal agent, a CYP3A4 inhibitor.Target: CYP3A4 (+)-Ketoconazole, an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections [1]. (+)-Ketoconazole also is a cytochrome P450 inhibitor [2].(+)-Ketoconazole (KTZ), on the antischistosomal potential of these quinolines against Schistosoma mansoni infection by evaluating parasitological, histopathological, and biochemical parameters. Mice were classified into 7 groups: uninfected untreated (I), infected untreated (II), infected treated orally with PZQ (1,000 mg/kg) (III), QN (400 mg/kg) (IV), KTZ (10 mg/kg)+QN as group IV (V), HF (400 mg/kg) (VI), and KTZ (as group V)+HF (as group VI) (VII). KTZ plus QN or HF produced more inhibition (P<0.05) in hepatic CYP450 (85.7% and 83.8%) and CYT b5 (75.5% and 73.5%) activities, respectively, than in groups treated with QN or HF alone. This was accompanied with more reduction in female (89.0% and 79.3%), total worms (81.4% and 70.3%), and eggs burden (hepatic; 83.8%, 66.0% and intestinal; 68%, 64.5%), respectively, and encountering the granulomatous reaction to parasite eggs trapped in the liver [3].Clinical indications: Candida infection; Dermatophytosis; Folliculitis FDA Approved Date: Toxicity: teratogenesis; liver injuries; adrenal gland problems
MitoBloCK-11 (MB-11) is a s mall molecule inhibitor of mitochondrial protein import possibly acts through transport protein Seo1, but not Tom70 or Tom20; inhibits precursor proteins that contain hydrophobic segments, confers growth in media lacking uracil in a specific manner and affects zebrafish development.
MeOSuc-Ala-Phe-Lys-AMC TFA is a peptide substrate of plasmin[1].