Copanlisib (BAY 80-6946) is a selective and ATP-competitive class-I PI3 kinases inhibitor, with IC50s of 0.5, 0.7, 3.7 and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively.
YM-264 is a selective, potent and orally active platelet-activating factor (PAF) antagonist with a pKi value of 8.85 for rabbit platelet membranes.
KDU731, an orally active C. parvum PI4K inhibitor with an IC50 value of 25 nM, blocks Cryptosporidium infection in vitro and in vivo[1][2]. KDU731 is a promising drug candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety[2].
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs[1][2].
Plumbagin (2-Methyljuglone) is a naphthoquinone isolated from Plumbago zeylanica L, exhibits anticancer and antiproliferative activities[1].
4-Isothiocyanatophenyl α-D-Mannopyranoside, an organic isothiocyanate, is a building block and reagent which is used for preparing neoglycoproteins[1].
cis-Ferulic acid 4-O-β-D-glucopyranoside (compound 7) is a phenolic glycosid, which can be isolated from Nitraria sibirica.. cis-Ferulic acid 4-O-β-D-glucopyranoside exhibits antioxidant activity and potent inhibitory effect on Phosphatase PTP1B[1].
DBCO-NHCO-PEG4-amine is a cleavable ADC linker used to conjugate MMAE (HY-15162) and antibody (e.g., DBCO-VCpAB−MMAE and DBCO-TRX−MMAE with EC50s of 280 nM and 22 nM in SKBR3 cells, respectively)[1].
Finasteride (acetate) is an orally active testosterone 5-alpha-reductase inhibitor. Target: 5-alpha ReductaseApproved: 1992Finasteride (acetate) is the acetate salt of finasteride which is a synthetic 4-azasteroid antiandrogen compound, is a specific inhibitor of steroid Type II 5α-reductase, an intracellular enzyme that converts the androgen testosterone into 5α-dihydrotestosterone (DHT). Finasteride is used in the treatment of prostate cancer, benign prostatic hyperplasia, and androgenetic alopecia (male pattern baldness). In benign prostatic hyperplasia, finasteride inhibits 5alpha-reductase activity in epithelium for Ki of 10nM, significantly lower than in stroma (Ki = 33nM) [1].
Kras4B G12D-IN-1 is a Kras4B G12D inhibitor with anticancer effects. Kras4B G12D-IN-1 decreases Kras protein expression in mouse embryonic fibroblasts (MEF) expressing Kras4B G12D (WO2016179558A1, Comp 994566)[1].
Lampalizumab (RG 7417) is a humanised monoclonal antibody targeting complement Factor D in the alternative complement pathway. Lampalizumab binds an exosite and sterically blocks Factor B access to the active site. Lampalizumab can be used for age-related macular degeneration (AMD) research[1][2].
WAY-351783 is an active molecule.
Afloqualone is a agonist of GABA receptor .Target: GABA Receptorin vitro: Afloqualone is a quinazolinone family GABAergic drug.Afloqualone is an analogue of methaqualone. It has sedative and muscle-relaxant effects, resulting from its agonist activity at the β subtype of the GABAa receptor.in vivo: Afloqualone slightly increased the response during the alarm period in one out of 3 rats at 5, 10, and 20 mg/kg p.o., respectively.
OG 488, acid, a fluorescent pH indicator, has many applications in biochemistry and neurosciences[1].
Arginine vasopressin (AVP, also known as antidiuretic hormone (ADH)) is a 9 amino acid neuropeptide secreted by the posterior pituitary. AVP can regulate the biological effects of fluid balance, osmolality and cardiovascular through three separate G-protein coupled receptors (GPCRs), namely Avpr1a (V1a), Avpr1b (V1b) and Avpr2 (V2). AVP also have potentially important effects on centrally regulated metabolic processes[1].
HO-PEG10-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
NMDA receptor modulator 2 (Compound 1) is a potent NMDA receptor modulator. NMDA receptor modulator 2 can be used for neurological disorder research[1].
Angiotensin II 5-valine is an agonist of angiotensin receptor.
WAY-207024 (dihydrochloride) is a potent and orally active GnRH antagonist that reduces leuteinizing hormone (LH) levels in plasma[1].
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM)[1][2].
Vitamin K5 (Synkamin) is a photosensitizer and a antimicrobial agent. Vitamin K5 is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 induces apoptosis of colon 26 cells. Vitamin K5 can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages[1][2][3].
Tyr-Tyr-Tyr-Tyr-Tyr-Tyr is a tyrosine derivative[1].
SALMF amide 2, a neuropeptide S2 from the starfish Asterias rubens, is involved in the regulation of eversion of the cardiac stomach in starfish[1].
Methyl 1,2,3,4-tetrahydro-α-hydroxy-2,4-dioxo-1-β-D-ribofuranosyl-5-pyrimidineacetate is a pyrimidine nucleoside analog. Pyrimidine nucleoside analogs have a wide range of biochemical and anticancer activities. These include DNA synthesis inhibition, RNA synthesis inhibition, antiviral effects, and immunomodulatory effects[1].
IQB-782 is a cysteine derivative. IQB-782 has inhibition for thrombin activatable fibrinolysis inhibitor (TAFI), with an Ki(app) of 0.14 μM. IQB-782 shows a potent mucolytic-expectorant activity[1][2].
TCO-PEG8-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Sotetsuflavone is a potent inhibitor of DENV-NS5 RdRp (Dengue virus NS5 RNA-dependent RNA polymerase) with an IC50 of 0.16 uM, is the most active compound of this series .
diSulfo-Cy3 alkyne is a water-soluble dye and a Click Chemistry reagent containing an azide group. Absorbance and emission of the dye are identical to Cy3 fluorophore. diSulfo-Cy3 alkyne can be used for the labeling of proteins, and even intact biological objects in water phase[1].
(1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor[1].
Tipepidine hydrochloride reversibly inhibits on dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) to activate VTA dopamine neuron, with an IC50 of 7.0 μM[1]. Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect[2].