TCO-PEG3-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Tuvirumab (OST 577; SDZ-OST 577) is a human IgG1 subclass monoclonal antibody directed against HBV surface antigen (HBsAg). Tuvirumab binds specifically and with high affinity (K=3.6 nM) to HBsAg. Tuvirumab has the potential for chronic hepatitis B research[1][2].
Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM[1].
BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 uM in ADP-Glo Assay.IC50 value: 37 uMTarget: ITPKA inhibitorBAMB-4 exhibit the lowest inhibition frequency among the InsP3-Kinase inhibitors. only in one from 42 targets tested,BAMB-4 showed an inhibitory effect. Noteworthy, in kinasescreens no targets of BAMB-4 were detected, indicating that thecompound does not belong to the typical kinase inhibitors. Thus,the relative high speci?city and the high cellular uptake ofBAMB-4 now for the ?rst provide the possibility to effectively inhibit InsP3kinase in vivo. e InsP3Kinase activity is essentially involved in ITPKA promoted metastasis of lung cancer cells, BAMB-4 is a promising therapeutic approach in lung cancertherapy.
(Lys7)-Phalloidin is a biologically active peptide.
ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell[1].
Ethyl 3-hydroxybutyrate is a fragrance found in wine and Tribolium castaneum[1][2].
Thalidomide-5-CH2-NH2 (hydrochloride) is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-CH2-NH2 (hydrochloride) can be connected to the ligand for protein by a linker to form PROTACs[1].
Monensin is a lipid-soluble naturally occurring bioactive ionophore produced by Streptomyces spp. Monensin can bind protons and monovalent cations. Monensin exhibits a broad spectrum activity against opportunistic pathogens of humans in both drug sensitive and resistant strains. Monensin also induces apoptosis in multiple cancer cell lines[1][2].
3’-Deoxy-3’-flluoro-3-deazauridine is a purine nucleoside analog. 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].
SCH-23390-d3 (R-(+)-SCH-23390-d3) hydrochloride is the deuterium labeled SCH-23390 hydrochloride. SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM[1][2][3].
CAY10410 (11-Oxo-prosta-5Z), a 15d-PGJ2 analog, is a potent PPARγ agonist. CAY10410 has the ability to activate PPARγ in human B cells without killing B lymphocytes[1].
Arecoline Hydrobromide is a muscarinic acetylcholine receptor agonist. Target: mAChRArecoline is an alkaloid found in the areca nut. Arecoline. a drug obtained from the Areca Catechu L., induced a dose-dependent antinociception (0.3-1 mg kg(-1) i.p.) which was prevented by the muscarinic antagonists pirenzepine (0.1 microg per mouse i.c.v.) and S-(-)-ET-126 (0.01 microg per mouse i.c.v.) [1]. Arecoline exerts its excitatory actions by binding to M2-muscarinic receptors on the cell membrane of neurons of the locus coeruleus [2]. Arecoline (1 nM - 1 microM) produced a concentration-dependent contraction in both the longitudinal and the circular smooth muscle of rabbit colon. Atropine (10 microM) abolished the arecoline (80 nM)--induced contraction. M3 receptor antagonist, 4 - DAMP (0.4 microM), abolished the arecoline (80 nM)--related response, whereas M2 receptor antagonist, gallamine (0.4 microM), did not affect the effect of arecoline. These results suggest that arecoline excites the colonic motility via M3 receptor in rabbits [3].
Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling[1].
UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5[1].
Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.
Fentonium bromide is an anti-ulcerogenic, anticholinergic and antispasmodic agent. Fentonium bromide can be used in the research of neurological conditions[1][2][3].
Supercinnamaldehyde is a potent transient receptor potential ankyrin 1 (TRPA1) activator with an EC50 value of 0.8 μM. Supercinnamaldehyde activates TRPA1 ion channels through covalent modification of cysteines[1].
CGP36216 (Compound 9) is a GABAB receptor antagonist. CGP36216 binds to GABAB receptor with a Ki value of 0.3 μM. CGP36216 can be used for research of anxiety and trauma-related disorders[1][2].
α-Methyl-p-tyrosine is a competitive inhibitor of the enzyme tyrosine hydroxylase, which converts tyrosine to Levodopa (DOPA). α-Methyl-p-tyrosine is an orally active inhibitor of catecholamine synthesis which inhibits the hydroxylation of tyrosine to DOPA[1].
Berninamycin D is a cyclic peptide fungal metabolite isolated from ermentation of Streptomyces bernensis[1].
trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations[1].
4-Chlorobenzaldehyde-2,3,5,6-d4 is the deuterium labeled 4-Chlorobenzaldehyde[1].
2’-Deoxy-N3-methylcytidine hydriodide is a purine nucleoside analog. 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].
[Arg6]-β-Amyloid (1-40), england mutation is a biological active peptide. (Several mutations in the beta amyloid precursor gene cause autosomal dominant Alzheimer's Disease in a number of kindreds. Among them, the English mutation, with His at position 6 replaced with Arg, was reported to accelerate the kinetics of oligomers formation which act as fibril seeds and are more toxic to cultured neuronal cells.)
Agelastatin A ((-)-Agelastatin A; AglA), a tetracyclic alkaloid isolated from the sponge Agelas dendromorpha, induces apoptosis and arrests cells in the G2/M phase of the cell cycle, exhibiting antitumor activity[1].
OSIP-486823 is a novel microtubule-interfering agent with distinct biological effects on both protein kinase G (PKG) and microtubules.
Aminooxy-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential[1].
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes[1][2][3][4].