Aminooxy-PEG3-C2-thiol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tacalcitol monohydrate (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) promotes normal bone development by regulating calcium.IC50 value:Target: Tacalcitol modulates immunological and inflammatory processes. Tacalcitol induces nerve growth factor production in epidermal keratinocytes.
Quercetin-3-O-D-glucosyl]-(1-2)-L-rhamnoside is main antioxidant from Shuxuening, an herbal medicines injection[1].
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo[1][2].
Magnocurarine a natural compound isolated from Tiliacora racemosa[1].
CalFluor 488 Azide is a water-soluble fluorogenic azide probe. CalFluor 488 Azide is activated by Cu-catalyzed or metal-free click reaction. CalFluor 488 Azide is not fluorescent until it is reacted with alkynes[1][2].
Macropa-NH2, a H2macropa derivative with an macrocyclic core of macropa, can be used in targeted cancer therapy research[1].
Boc-Ala-Ala-Asp-pNA is a chromogenic substrate of granzyme B. Boc-Ala-Ala-Asp-pNA can be used to test functional activity of granzyme B[1].
Cyclohexyl [3,5-bis(methylthio)-4-isothiazolyl]carbamate is a compound that can be used for altering the lifespan of eukaryotic organisms[1].
AZD-4818 is a potent antagonist of chemokine CCR1. AZD-4818 can be used for the treatment of chronic obstructive pulmonary disease (COPD) [1].
Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
Gal-C4-Chol is a glycosylated cholesterol derivative. Gal-C4-Chol can be used as a ligand for asialoglycoprotein receptors (ASGPR) to prepare Galactosylated (Gal) liposomes. Gal-C4-Chol can be used to prepare simple lipid-based nanoparticles[1][2][3].
Calystegine A3 is a natural product that can be isolated from Calystegia sepium[1].
ML-099 (CID-888706) is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, Rab7, and Rab-2A[1].
GSK3735967 is a potent, selective, non-nucleoside inhibitor of DNMT1 with IC50 of 40 nM.
Syringetin-3-O-glucosid (Syringetin 3-O-β-D-glucoside), a flavonol glycoside, shows relatively weak DPPH and ABTS radical scavenging activity[1].
cis-11-Methyl-2-dodecenoic acid is a quorum sensing (QS) signal that acts as a diffusion signaling factor (DSF) in extracellular microbial and fungal communication systems. DSF is involved in the regulation of virulence and biofilm formation of a variety of bacterial pathogens[1].
Phosphodiesterase II, namely phosphodiesterase 2, is mainly involved in the hydrolysis of the important second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), and is often used in biochemical research. Phosphodiesterase II is expressed in a variety of tissues, such as the adrenal medulla, brain, heart, platelets, macrophages and endothelial cells, and is involved in the regulation of many different intracellular processes[1].
SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
L-Serine isopropyl ester hydrochloride is a serine derivative[1].
Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects[1][2].
Tyrphostin A1(AG9) inhibits CD40L-stimulated IL-12 production in macrophage cultures and antigen-induced generation of Th1 cells.IC50 value: Target: IL-12 production inhibitorAddition of increasing concentration of A1 resulted in a dose dependent decrease of IL-12 p40, with maximal inhibition (62.5%) occurring at a dose of 10 μM. tyrphostin A1 blocks CD40L-induced translocation of NF-κB to the nucleus, and reduces the activation of IL-12 p40 gene. In vivo therapy with A1 leads to decrease in generation of myelin basic protein (MBP) specific encephalitogenic T cells. In addition, treatment of SJL/J mice with A1 results in attenuation of experimental allergic encephalomyelitis (EAE) [1]. Tyrphostin A1 is a much weaker inhibitor of TK than other tyrphostins (IC50>1250 μM for epidermal growth factor receptor (EGFR) kinase), and therefore often used to differentiate TK-mediated effects of tyrphostins from other non-specific effects [2].
Griffonilide is a butenolide, isolated from the roots of Semiaquilegia adoxoides, and often occurs alongside lithospermoside[1][2].
Ro 363 is a potent and highly selective β1-adrenoceptor agonist. RO 363 is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility[1][2][3].
VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104 decreased the levels of palmitoylated TEAD3 and TEAD4 and increased the levels of unpalmitoylated TEAD3 and TEAD4 in the human mesothelioma cell line NCI-H2373.VT104 exhibited inhibitory activity in more mesothelioma cell lines than the TEAD1-selective inhibitor VT103.VT104 (oral administration of 10 and 3 mg/kg) has very strong antitumor efficacy in the human mesothelioma NCI-H226 CDX model, with no effect on body weight gain.
ATPγS (tetralithium salt) is a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A[1].
Proprotogracillin is a steroidal glycoside isolated from the bulbs of lilium speciosum[1].
Chlormadinone acetate is a steroidal progestin, with antiandrogen and antiestrogenic effects.
N-Nitrosodiethylamine is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity[1].