BU09059 is a potent, selective, short-acting kappa-opioid receptor antagonist with Ki of 1.72 nM, displays 15- and 616-fold selectivity over μ- and δ-receptors respectively; BU09059 is a potent and selective κ-antagonist with pA2 of 8.62, significantly blocks U50,488-induced antinociception in vivo (3 and 10 mg/kg), demonstrates a shorter duration of κ-antagonist action in vivo.
Norethindrone acetate is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Homocapsaicin II is a pungent compound, that can be isolated from fruits of Capsicum annuum L[1].
LCMV gp33-41 is the H-2Db restricted epitope derived from the lymphocytic choreomeningitis virus (LCMV) glycoprotein gp 33; residues 33 to 41.
1-O-Galloyl-2-O-cinnamoyl-glucose is a natural compound that could be found in R. palmatum L.[1].
Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12[1].
BAPTA tetrapotassium is a non-permeable, selective extracellular calcium chelator, with 105-fold greater affinity for Ca2+ than Mg2+. BAPTA tetrapotassium is a valuable tool to study the role of calcium in cell signaling[1][2].
Viscidulin II (FL6) is a flavone. Viscidulin II can be isolated from the root of Scutellaria baicalensis. Viscidulin II significantly suppresses P. acnes-induced IL-8 and IL-1β production in THP-1 cells[1].
Clobutinol is a compound that has anti-tussive effects. Clobutinol affects heart rate and blood pressure, it can be used for cough related research[1][2][3].
MSG606 is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 exhibits binding affinity for A375 melanoma cells in vitro. MSG606 reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.
UAMC-00050 is a potent trypsin-like serine protease inhibitor. UAMC-00050 can be used in research of dry eye syndrome and ocular inflammation[1].
HDAC ligand-1 is a HDAC ligand that can be used to synthesize PROTAC HDAC degraders[1].
(-)-Ketoconazole is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
2,3,4,6-Tetra-o-acetyl-alpha-galactosylpyranosyl bromide is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
N2-iso-Butyroyl-5'-O-DMT-3'-deoxy-3'-fluoroguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
BTdCPU is a potent heme-regulated eIF2α kinase (HRI) activator. BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell[1].
HCAIX-IN-2 (compound 9d) is a selective carbonic anhydrase inhibitor with the Ki values of 24.6 nM and 45.3 nM for hCA IX and hCA XII, respectively[1].
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia[1].
Farrerol is a bioactive constituent of Rhododendron, with broad activities such as anti-oxidative, anti-inflammatory, anti-tumor, neuroprotective and hepatoprotective effects[1][2][3][4][5][6].
SCO-PEG8-NHS SCO is a PROTAC linker and belongs to the PEG class. SCO-PEG8-NHS SCO contains SCO and NHS esters that can be covalently bound to amino groups, respectively. SCO is often used to react with amino acid residues of proteins or peptides, particularly lysine.
Fluconazole (hydrate) is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.Target: AntifungalFluconazole (hydrate) is the hydrate salt form of fluconazole, which is a triazole antifungal intended for oral treatment of superficial and systemic mycoses. In tests done in standard mycological media, the compound had minimal inhibitory concentrations against pathogenic Candida species that were usually in excess of 100 mg/l. Fluconazole inhibited branching and hyphal development in C. albicans at concentrations as low as 10(-6) M (0.3 mg/l), but miconazole and ketoconazole were still active in these tests at concentrations 100 times lower than this [1]. Oral fluconazole was not associated with a significantly increased risk of birth defects overall or of 14 of the 15 specific birth defects of previous concern. Fluconazole exposure may confer an increased risk of tetralogy of Fallot [2]. Fluconazole is predicted to be ineffective against Cryptococcus gattii in the koala as a sole therapeutic agent administered at 10 mg/kg p.o. every 12 h [3].Clinical indications: Balanitis; Candida infection; Cryptococcus infection; Cryptococcus neoformans meningitis; Dermatomycosis; Female genital tract infection; Fungal infection; Fungal respiratory tract infection; Fungal urinary tract infection; Prophylaxis; Tinea capitis; Tinea corporis; Tinea cruris; Tinea pedis .Toxicity: Symptoms of overdose include hallucinations and paranoid behavior.
Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD[1][2][3].
5-Pyrrolidinomethyluridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Alterbrassicene B is isolated from Alternaria brassicicola. Alterbrassicene B has cytotoxicity against cancer cell lines OVCAR and MDA-MB-231 with IC50s of 19.25 μM and 31.22 μM[1].
Chromoionophore I (ETH 5294) is a hydrophobic pH indicator. Chromoionophore I is used as a transmissive or fluorescent probe molecule in many types of hydrophobic sensor membranes. Chromoionophore I is oil-soluble[1].
Tubulin polymerization-IN-36 is a tubulin polymerization inhibitor (IC50: 2.8 μΜ). Tubulin polymerization-IN-36 binds to the colchicine site of tubulin and inhibits colchicine binding. Tubulin polymerization-IN-36 can be used in the research of cancers, such as lymphomas[1].
GS39783 is a positive allosteric modulator (PAM) of GABABR. Positive modulation of the GABABR can be used for the research of Nicotine addiction[1].
a-Hydroxymetoprolol is a metabolite of metoprolol. The adrenoreceptor blocking effect of a-Hydroxymetoprolol on metoprolol is almost zero[1].
FLT3-IN-2 is a FLT3 inhibitor with IC50 of ＜ 1 μM, detailed information refer to WO 2012158957 A2 and WO 2007013896.
Trimetazidine dihydrochloride is a drug for angina pectoris. Trimetazidine is the first cytoprotective anti-ischemic agent , which improves myocardial glucose utilization through inhibition of fatty acid metabolism.