Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.IC50 value: 4 ±1 nM (Ki) [1] Target: histamine H4 receptorin vitro: JNJ-7777120 prevents fibronectin-induced lung fibroblast migration, thus suggesting that H4R could represent an attractive target for the development of new drugs for lung fibrosis treatment .[2]in vivo: JNJ 7777120 blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. In addition, it can block the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. JNJ 7777120 significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model. [3]
LY-411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with IC50 of 0.39 nM.
Liriopesides B (Nolinospiroside F) is a steroidal saponin isolated from Ophiopogon japonicas. Liriopesides B has anti-oxidative and anti-aging effects[1].
Buformin (1-Butylbiguanide) is a potent and orally active biguanide antidiabetic agent, an AMPK activator. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al)[1].
(2S)-4'-Hydroxy-7-methoxyflavan is a Flavan. Flavan (4′-hydroxy-7-methoxyflavan) showed an important cytotoxic effect on human leukemic Molt 4 cells[1].
CJ-42794 is a selective prostaglandin E receptor subtype 4(EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).IC50 value: 8.5 (pKi ) [1]Target: EP4in vitro: CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor with a mean pA2 value of 8.6. PGE2 inhibits the lipopolysaccharide (LPS)-induced production of tumor necrosis factor α (TNFα) in human whole blood (HWB); CJ-042794 reverses the inhibitory effects of PGE2 on LPS-induced TNFα production in a concentration-dependent manner. [1]in vivo: CJ-42794 significantly delays the ulcer healing in rats and mice. The expression of VEGF in primary rat gastric fibroblasts was increased by PGE2 or AE1-329 (EP4 agonist), and these responses were both attenuated by coadministration of CJ-42794.[2]
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells[1][2][3][4].
Shancigusin I is a natural compound found in Cremastra appendiculata[1].
Arg-Trp is a dipeptide composed of arginine and tryptophan, and analogues of Arg-Trp-octyl ester show antibacterial activity[1].
Mocravimod is an oral activity amphematoshenol-1-1-phosphate receptor (S1PR) regulator, which can block the required signal from lymph organs to prevent the migration of effect cells from migrating to non-lymph hematopoietic tissue. Mocravimod can be used for cancer research[1].
A novel potent, selective Mcl-1 inhibitor with IC50 of <3 nM in FRET assays; displays >1,000-fold selectivity over Bcl-2 and Bcl-xL; induces cleaved caspase-3 in MV4-11 cells with IC50 of 3.78 uM.
Pantethine is a dimeric form of pantothenic acid, is an intermediate in the production of Coenzyme A, is available as a dietary supplement, and is used to treat acne and improve the blood-cholesterol profile.
HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors; displays a statistically significant higher affinity for receptors not containing the α1 subunit with a rank order of α5 (Ki=140nM) > α2 (Ki=269 nM) > α1 (Ki=382 nM); The Ki value of HZ166 for the α3β3γ2 combination (185± 47 nM) was statistically significantly lower than the Ki value observed for α1β3γ2 but not different from those of α2β3γ2 and α5β3γ2; HZ-166 is antihyperalgesic in mouse models of inflammatory and neuropathic pain.
Boc-β-(9-anthryl)-Ala-OH is an alanine derivative[1].
LL-37 GKE is an active domain of LL-37. LL-37 GKE has antibacterial activity and has potential applications in antibiotics[1][2].
Cordycepin, which is a nucleoside derivative isolated from Cordyceps, inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner.
Propargyl-PEG7-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Antistaphylococcal agent 3 is an antistaphylococcal therapeutic agent.
TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC. TX-1123 is a cyclo-oxygenase (COX) inhibitor with IC50 values of 1.16 μM and 15.7 μM for COX2 and COX1, respectively. TX-1123 has low mitochondrial toxicity. TX-1123 can be used in research of cancer[1][2].
15-Keto latanoprost is a metabolite of Latanoprost, which is an ocular hypotensive agent[1].
Deoxyribonuclease II (DNase II) is an endonuclease that hydrolyzes the phosphodiester bonds of deoxyribonucleotides in native and denatured DNA, producing 3' phosphate and 5'-hydroxyl termini. Deoxyribonuclease II works best at acidic pH and is commonly used in biochemical research[1].
Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
Capadenoson is a selective agonist of adenosine-A1 receptor.
Protease-Activated Receptor-3 (PAR-3) (1-6), human is a proteinase-activated receptor (PAR-3) agonist peptide[1].
6-(4-Methoxyphenyl)pyridazin-3-amine is an aminopyridazine derivative, and can be used for the synthesis of SR 95103. SR 95103 is a selective and competitive GABA-A receptor antagonist[1].
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells[1].
Lirentelimab (AK002) is a humanized IgG1 monoclonal antibody that targets sialic acid-binding Ig-like lectin 8 (SIGLEC8). Lirentelimab induces cell Apoptosis of IL-5-activated eosinophils and inhibits IgE-mediated mast cell activation. Lirentelimab can be used for the research of eosinophilic gastritis and duodenitis[1].
2-Fluoro-L-phenylalanine is a phenylalanine derivative[1].
N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitory activity against α-glucosidase (IC50 of 103.58 μM)[1].