Cynatratoside D is a oligoglycoside isolated from the root of Cynanchum atratum Bunge (Asclepiadaceae)[1].
LDH-IN-2, a salicylic acid derivative, is an inhibitor of glycolate oxidase (GO). LDH-IN-2 decreases oxalate output in hyperoxaluric hepatocytes. LDH-IN-2 can be used for research of primary hyperoxaluria type 1 (PH1)[1].
Defensin HNP-3 human is a cytotoxic antibiotic peptide known as "defensin". Defensin HNP-3 human has inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Defensin HNP-3 human is initially synthesized as the 94 amino acids preproHNP(1-94), which is hydrolyzed to proHNP(20-94) and converted to mature HNP(65-94) after the removal of anion precursors[1][2].
SSI-4 is an inhibitor of Stearoyl CoA desaturase 1 (SCD1) , which can be modified with 11C, used as a ligand to in vivo small animal PET/CT imaging of SCD1[1].
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition[1].
14-Deoxy-17-hydroxyandrographolide is an ent-labdane diterpenoid compound isolated from the aerial parts of Andrographis paniculate[1].
7,3'-Dihydroxy-5'-methoxyisoflavone (Pterosonin E) is an arylcoumarin. 7,3'-Dihydroxy-5'-methoxyisoflavone can be used for various biochemical studies[1].
Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].
Isospaglumic acid is a neuropeptide found in millimolar concentrations in brain.
Neotame is a derivative of Aspartame and is a low-caloric and high-intensity artificial sweetener that is 7000-13,000 times sweeter than sugar. Neotame is a non-nutritive sweetener and flavor enhancer that can be used in a variety of foods[1][2].
Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) is a somatostatin agonist that can be used in cancer research[1].
Tildipirosin, a long-acting macrolide, has antibiotic activity.
(R)-3-Amino-4-hydroxybutanoic acid is a serine derivative[1].
Pomalidomide-amino-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Camelliaside A is a flavonoid from the methanol extract of tea (Camellia oleifera) seed pomace[1].
Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib is a drug for the treatment of ER-positive and HER2-negative breast cancer.
LDN-27219 is a potent inhibitor of hTGase(Tissue transglutaminase) with an IC50 of 0.6 uM.IC50 value: 0.6 uM [1]Target: hTGase inhibitorLDN-27219 is a potent inhibitor of the enzyme(hTGase), producing 100% inhibition at the screening concentration of 10 uM. To examine the enzyme selectivity of LDN-27219, it was tested as an inhibitor of coagulation Factor XIIIa and caspase 3. At concentrations as high as 50 íM, the compound had no effect on the activities of either of these enzymes. LDN-27219 was found to be nontoxic at concentrations as high as 100 íM in an assay that measures the viability of HT1080 cells, a fibrosarcoma tumor cell line.
Milbemycin oxime is a veterinary drug from the group of milbemycins, used as a broad spectrum antiparasitic.
Irpagratinib (ABSK011) is an orally active inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinase, targeting to FGFR4 (IC50<10 nM). Irpagratinib inhibits the auto-phosphorylation of FGFR4 and blocks signal transduction from FGFR4 to downstream pathway activation. Irpagratinib exhibits high exposure in PK study in mouse, rat and dog, and also shows antineoplastic/anti-tumor activity in subcutaneous xenograft tumor models[1].
Tetrabutylammonium acetate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.
Isoapetalic acid (compound 4) is a potent anti-HIV agent[1].
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
1-(3’-O-[4,4’-Dimethoxytrityl]-alpha-L-threofuranosyl)-thymine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
E3 ligase Ligand-Linker Conjugates 5 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.
Poziotinib(NOV120101; HM781-36B) is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.IC50 value: 3/5/23 nM(HER1/HER2/HER4) [1]Target: pan-HER inhibitorin vitro: The IC50 levels of HM781-36B for N87 and SNU216 were 0.001 and 0.004 μmol/L, respectively, which was 10–1000 fold lower than the IC50 levels of other HER family TKIs. HM781-36B more potently inhibited the phosphorylation of HER family and downstream proteins, and induced apoptosis and G1 arrest compared to gefitinib or lapatinib [1]. HM781-36B is a potent inhibitor of EGFR in vitro, including the EGFR-acquired resistance mutation (T790M), as well as HER-2 and HER-4, compared with other EGFR tyrosine kinases inhibitors (erlotinib, lapatinib and BIBW2992). HM781-36B treatment of EGFR DelE746_A750-harboring erlotinib-sensitive HCC827 and EGFR L858R/T790M-harboring erlotinib-resistant NCI-H1975 NSCLC cells results in the inhibition of EGFR phosphorylation and the subsequent deactivation of downstream signaling proteins [2]. The addition of HM781-36B induced potent growth inhibition in both DiFi cells with EGFR overexpression and SNU-175 cells (IC50 = 0.003 and 0.005 μM, respectively). Furthermore, HM781-36B induced G1 arrest of the cell cycle and apoptosis, and reduced the levels of HER family and downstream signaling molecules, pERK and pAKT, as well as nonreceptor/cytoplasmic tyrosine kinase, BMX [3].in vivo: The growth of tumors in mice treated with HM781-36B alone or in combination with 5-FU was significantly inhibited compared with control mice, and tumor volume in mice receiving coadministraion of HM781-36B and 5-FU was smaller than tumor volume in mice receiving HM781-36B only [1].
USP1-IN-6 (compound 11) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM[1].
Stigmasterol is a plant sterol which has been focused on the cholesterol-lowering activity and is valued as an anti-stiffness factor in the therapy of rheumatic diseases.
A-1293102 is a potent and selective BCL-XL inhibitor that kills BCL-XL-dependent tumor cells[1].