S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
Odatroltide, as a nanoscale P-selectin inhibitor, is a nano-delivery system of 6,7-dihydroxyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and KPAK to target the thrombus[1].
Poststerone is a nature product. Poststerone is a metabolite of insect metamorphosing substances from Cyathula capata[1].
SHP2-IN-20 (compound 193) is a SHP2 inhibitor with an IC50 value of 3 nM. SHP2-IN-20 can be used for glioblastoma research[1].
OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.
Forsythoside H, a caffeoyl phenylethanoid glycoside (CPG) isolated from the fruits of Forsythia suspense (Thunb.) Vahl, may possesses anti-inflammatory activities[1].
D-Xylofuranose, 1,2,3,5-tetraacetate is the raw material for nucleotides synthesis[1].
RS Domain derived peptide is a biological active peptide. (This peptide is a substrate for Clk/Sty and is phosphorylated by Clk/Sty protein kinase (Km=102 microM).)
CY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity[1].
L-Methionine-13C5 is the 13C-labeled L-Methionine. L-Methionine is the L-isomer of Methionine, an essential amino acid for human development. Methionine acts as a hepatoprotectant.
IKarisoside A(Icarisoside-A) is a natural compound isolated from Epimedium koreanum (Berberidaceae); has anti-inflammatory properties.IC50 value:Target: in vitro: Ikarisoside A inhibited the expression of LPS-stimulated inducible nitric oxide synthase (iNOS) and the production of nitric oxide (NO) in LPS-stimulated RAW 264.7 cells and mouse bone marrow-derived macrophages (BMMs) in a concentration-dependent manner. In addition, Ikarisoside A reduced the release of pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1 beta). Furthermore, Ikarisoside A inhibited the activity of p38 kinase and nuclear factor-kappaB (NF-kappaB) [1]. Ikarisoside A is a potent inhibitor of osteoclastogenesis in RANKL-stimulated RAW 264.7 cells as well as in bone marrow-derived macrophages.The inhibitory effect of Ikarisoside A resulted in decrease of osteoclast-specific genes like matrix metalloproteinase 9 (MMP9), tartrate-resistant acid phosphatase (TRAP), receptor activator of NF-kappaB (RANK), and cathepsin K. Moreover, Ikarisoside A blocked the resorbing capacity of RAW 264.7 cells on calcium phosphate-coated plates. Ikarisoside A also has inhibitory effects on the RANKL-mediated activation of NF-kappaB, JNK, and Akt [2].
Folinic acid is an adjuvant used in cancer chemotherapy involving the drug methotrexate.Target: AntifolateFolinic acid is a 5-formyl derivative of tetrahydrofolic acid. It is readily converted to other reduced folic acid derivatives (e.g., tetrahydrofolate), and, thus, has vitamin activity that is equivalent to that of folic acid. Since it does not require the action of dihydrofolate reductase for its conversion, its function as a vitamin is unaffected by inhibition of this enzyme by drugs such as methotrexate. In 1980s, however, folinic acid was found to reactivate the dihydrofolate reductase itself even when methotrexate exists. Although the mechanism is not very clear, the polyglutamylation of methotrexate and dihydrofolate in malignant cells is considered to play an important role in the selective reactivation of dihydrofolate reductase by folinic acid in normal cells [1]. Folinic acid is generally administered along with MTX as a rescue agent to decrease MTX-induced toxicity. However, information regarding the inhibitory effect of folinic acid against cytogenetic damage caused by MTX is limited. This study was conducted to assess the cytogenetic effect of MTX and its inhibition by folinic acid (FA) using the micronucleus and chromosomal aberration assays concurrently [2].
KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases[1].
D-Ribofuranose (D-Ribose) is an endogenous metabolite present in Cerebrospinal_Fluid that can be used for the research of Ribose 5 Phosphate Isomerase Deficiency and Medium Chain Acyl Co A Dehydrogenase Deficiency[1][2].
Pomalidomide-C11-NH2 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-C11-NH2 can be connected to the ligand for protein by a linker to form PROTAC[1].
Tamsulosin-d4 (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
(Ethoxymethyl)benzene is an endogenous metabolite.
Metixene (Piperidine) is an anticholinergic and antiparkinsonian agent. Metixene potently inhibits binding of quinuclidinyl benzilate (QNB) with the muscarinic receptor, IC50 and Ki values of 55 nM and 15 nM, respectively. Metixene can be used for the research of parkinsonian[1][2][3].
Anthracene-9-carboxylic acid (9-Anthracenecarboxylic acid) is an anthracene derivative traditionally used to block and identify Ca2+-activated Cl- currents (CaCCs) in various cell types, like diverse smooth muscle cells, epithelial cells and salivary gland cells[1].
Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active[1][2].
Eflornithine hydrochloride, hydrate is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.
2-Deoxy-D-glucose-13C-1 is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
Royal Jelly acid (Queen Bee Acid) is a fatty acid constituent of royal jelly, promotes the growth and protection of neurons, reduces anxiety-like phenotypes[1].
Aprophen (Aprofene) is an antimuscarinic inhibitor. Aprophen can be used for the research of central nervous system[1].
Nortrachelogenin 4'-O-β-gentiobioside (compound 20) is a lignan isolated from the aerial parts of Trachelospermius[1].
WAY-304671 is an active molecule and a potential ubiquitin ligase inhibitor.
Mal-amido-PEG3-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
L-Allooctopine is a competitive inhibitor of D-octopine[1].