Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
Daphylloside is an iridoid isolated from the aerial parts of Galium verum.
Ceratotoxin-2 (CcoTx2) is a voltage-gated sodium channel blocker with IC50s of 8 nM and 88 nM against Nav1.2/β1 and Nav1.3/β1, respectively[1].
pTH (1-38) (human) is a biologically active peptide.
(-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity[1]. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[2].
1,7-Dihydroxyacridone is a natural product that can be isolated from Boronia lanceolata[1].
Ornidazole diol (Ro 11-2616) is a diol produced by ornidazole rapidly hydrolysing in basic solutions[1].
Morusinol is a flavonoid isolated from Morus alba root bark. Morusinol has an antiplatelet activity and significantly inhibits arterial thrombosis in vivo[1].
MOBS is an amphoteric buffer, a butane analogue of the Good buffers MOPS [3-(N-morpholino) propanesulfonic acid] and MES [2-(N-morpholino) ethanesulfonic acid][1].
Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer[1][2][3].
7-Deaza-2′-deoxyguanosine 5′-triphosphate (7-Deaza-2'-dGTP), a nucleotide analogue, is a telomerase inhibitor (IC50: 11 μM)[1].
C188-9 is a Stat3 inhibitor, with a Kd of 4.7 nM.
PPARγ-IN-2 (Compound 5a) is a PPARγ inhibitor. PPARγ-IN-2 inhibits TG accumulation in 3T3-L1 preadipocytes (EC50: 0.106 μM). PPARγ-IN-2 inhibits high-cholesterol diet (HFC)-induced obesity and related metabolic syndrome, and reduces lipid accumulation in adipose tissue[1].
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.IC50 value: 3.2 pM [1]Target: PDE4Bin vitro: GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 × 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 × 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity [1].in vivo: GSK256066 inhibits the LPS-induced pulmonary neutrophilia with an ED50 of 1.1 μg/kg, achieving maximal inhibition of 72% at 30 μg/kg when given in the aqueous suspension. GSK256066 inhibits the LPS-induced pulmonary neutrophilia with ED50 of 2.9 μg/kg, achieving maximal inhibition of 62% when given in the dry powder formulation. GSK256066 shows a moderate plasma clearance of 39 ml/min/kg, a moderate volume of distribution of 0.8 L/kg, and a relatively short half-life of 1.1 hour in the male CD rat [1]. GSK256066 sustains at a high lung concentration of 2.6 μg/g after intra-tracheal administration as an aqueous suspension at a dose of 30 μg/kg in rats [2]. GSK256066 (10 μg/kg) is administered intratracheally at different times (2, 6, 12, 18, 24, and 36 hours) before LPS administration, inhibiting LPS-Induced Pulmonary Neutrophilia in rat lipopolysaccharide (LPS)-induced models of acute pulmonary inflammation. GSK256066 (0.3–100 μg/kg) inhibits LPS-induced increases in exhaled nitric oxide with ED50 of 35 μg/kg in rat. GSK256066 (10 μg/kg) is administered half a hour before OVA administration in rat, inhibiting OVA-induced pulmonary eosinophilia with ED50 of 0.4 μg/kg. GSK256066 administered intratracheally as a dry powder blended in respiratory-grade lactose at doses of 3 to 100 μg/kg 2 hours before inhaled LPS challenge in ferrets, inhibiting LPS-induced pulmonary neutrophilia with ED50 of 18 μg/kg without inducing emetic episodes [3].
Benzyl 4-hydroxybenzoate-d4 is the deuterium labeled Benzyl 4-hydroxybenzoate[1].
Aminooxy-PEG3-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
Elamipretide is a cardiolipin peroxidase inhibitor and mitochondria-targeting peptide.
QX77 is a chaperone-mediated autophagy (CMA) activator.
Gedunin is a limonoid with anti-cancer, anti-viral, anti-inflammatory and insecticidal activities. Gedunin acts as a potent Hsp90 inhibitor and induces the degradation of Hsp90-dependent client proteins. Geduni may obstructs the entry of SARS-CoV-2 virus into human host cells and can be used for COVID-19 research[3].
Thalidomide-NH-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
LY 97241 accelerates the apparent rate of inactivation of transient outward K current. LY 97241 is an antiarrhythmic drug[1].
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively[1].
Estrogen receptor antagonist 2 is a potent and orally active estrogen receptor (ER) antagonist, example 17, extracted from patent US20180111931A1. Estrogen receptor antagonist 2 is used for the study of breast cancer[1].
APPA is an aldose reductase inhibitor. APPA can effectively prevent apoptosis and the symptoms of Streptozotocin (HY-13753)-induced diabetes by inhibiting the polyol pathway in rats. APPA has the potential for diabetic nephropathy (DN) research[1].
2,3-Diphenylmaleic anhydride is an analogue of cis-Stilbene[1].
White mineral oil is the highly refined mineral oil, and is composed of saturated aliphatic and alicyclic nonpolar hydrocarbons. White mineral oil is biologically and chemically stable, and doesn’t support pathogenic bacterial growth. White mineral oil can resist moisture, extend, soften, smoothen, and lubricate[1].
Thalidomide-5-PEG2-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-PEG2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].
(±)-WS75624B is an endothelin converting enzyme (ECE) inhibitor with an IC50 of 0.03 μg/mL.
H-Val-Gln-OH is a biologically active peptide.