Boc-(R)-3-thienylglycine is a Glycine (HY-Y0966) derivative[1].
Sulfo-NHS-Acetate sodium is an alkyl chain-based PROTAC linker. Sulfo-NHS-Acetate sodium can be used in the synthesis of PROTACs[1].
Sodium hexadecyl sulfate-d33 is the deuterium labeled Sodium hexadecyl sulfate[1].
2,7-Bis(alloxycarbonylamino)-9-chloroacridine can be used as a fluorescent label.
endo-BCN-PEG3-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Fenbufen-d9 (CL-82204-d9) is the deuterium labeled Fenbufen. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor[1][2][3][4][5].
Boc-D-Trp(For)-OH, containing the amino acid tryptophan, is synthesized by the ammonolysis of Boc-protected D-alanine, followed by cyclization to form a dipeptide with ninhydrin. Boc-D-Trp(For)-OH has pharmacological properties, including inhibition of growth hormone release, induction of sleep and antiinflammatory[1][2].
meso-CF3-BODIPY 2 (CF3-substituted Tetramethyl BODIPY) is a fluorescent dye with the absorption wavelength (λabs) of 553 nm and emission wavelength (λem) of 622 nm. meso-CF3-BODIPY 2 can be used in labeling reagents and photodynamic therapy[1][2].
GP1a is a potent agonist of cannabinoid receptor 2 (CB2). Gp1a is beneficial to skin wound healing. GP1a inhibits inflammation and fibrogenesis while promoting re-epithelialization[1].
Syk-IN-1 (compound 4) is a potent Syk inhibitor, with an IC50 of 35 nM[1].
Anticancer agent 103 (Compound 2k) is a potent anticancer agent[1].
Boc-C16-COOH is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Boc-C16-COOH is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]
Ezetimibe-d4 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
Copeptin (human) is a diagnostic and prognostic biomarker for cardiovascular disease (CVD). Copeptin (human) is also the carboxyl terminus of the arginine vasopressin (AVP) precursor peptide. Copeptin (human) can be used in the study of cardiovascular disease[1].
SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
O-Desmethylangolensin is a metabolite of soy isoflavone, daidzein metabolized by gut microbiota. O-Desmethylangolensin possesses antioxidant activity[1][2].
HJB97 is a high-affinity BET inhibitor with Kis of 0.9±0.2 nM (BRD2 BD1), 0.27±0.09 nM (BRD2 BD2), 0.18±0.01 nM (BRD3 BD1), 0.21±0.03 nM (BRD3 BD2), 0.5±0.2 nM (BRD4 BD1), 1.0±0.1 nM (BRD4 BD2), respectively. HJB97 is a PROTAC BET degrader. Antitumor activity[1].
Azido-PEG5-CH2CO2-PFP is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs[1].
Ethylenediaminetetraacetic acid (EDTA) disodium dihydrate is a chelating agent used as a protease inhibitor and metal ion scavenger. Ethylenediaminetetraacetic acid disodium dihydrate is used extensively during protein purification. Ethylenediaminetetraacetic acid disodium dihydrate has been shown to be a noneffective molecule on cellulase activity. Ethylenediaminetetraacetic acid disodium dihydrate binds to metals including calcium and facilitates their excretion[1][2].
Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
APS-2-79 behaves as a kinase suppressor of Ras (KSR)-dependent antagonist of RAF-mediated MEK phosphorylation. APS-2-79 binds directly to KSR2 within the KSR2-MEK1 complex with an IC 50 of 120±23 nM for KSR2.
1,1-Dimethylurea-d6 is the deuterium labeled 1,1-Dimethylurea[1].
1,3,5,6-Tetrahydroxyxanthone is a natural xanthone that can be isolated from Garcinia achachairu Rusby (Clusiaceae) branches. 1,3,5,6-Tetrahydroxyxanthone induces diuresis and saluresis in normotensive and hypertensive rats[1].
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately[1].
Solifenacin is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration[1].
N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 140 nM[1].
PD-1/PD-L1-IN-22 (Example 2) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-22 blocks PD-1/PD-L1 with the IC50 of 0.732 μM. PD-1/PD-L1-IN-22 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
Rubrofusarin 6-O-β-D-glucopyranoside, the glycoside of Rubrofusarin, is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with the IC50 of 87.36 μM. Rubrofusarin 6-O-β-D-glucopyranoside can be used for the research of comorbid diabetes and depression[1].
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile[1].