Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities[1][2].
Socazolimab (ZKAB001) is an anti-PD-L1 monoclonal antibody. Socazolimab has lasting safety and efficacy in the treatment of recurrent or metastatic cervical cancer. Socazolimab also has potential applications in small cell lung cancer, esophageal squamous cell carcinoma (ESCC), advanced urothelial carcinoma and osteosarcoma[1][2][3][4][5].
17:0-18:1 PE-d5 is deuterium labeled 17:0-18:1 PE.
O-Linked GlcNAc transferase substrate is a biological active peptide. (A peptide substrate of O-linked GlcNAc transferase (OGT), a eukaryotic glycosyltransferase that uses UDP-GlcNAc as a glycosyl donor.)
Thifluzamide is a powerful and effective fungicide. When used safely and correctly it can be effective on rice and other crops because of improved water dispersal techniques. Thifluzamide is highly active against Basidiomycete fungi, in particular Rhizoctonia solani, primarily in rice, potatoes, and turf markets.
Bisacurone is a natural terpenoid, exhibits inhibitory activities on LPS-induced NO production with an IC50 of 29.8 μM[1].
ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3[1].
JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
Tris(4-aminophenyl)methane is a triphenylmethane dye. Tris(4-aminophenyl)methane is a weak HCV helicase inhibitor.
5-Benzylamino carbonyl-3’-O-acetyl-2’-O-methyl-5’-O-DMTr-uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
K02288 is a potent inhibitor of ALK, and inhibits ALK1/2/3/6 with IC50s of 1.8/1.1/34.4/6.3 nM; K02288 is less potent against ALK4/5, with IC50s of 302 nM and 321 nM.
Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease[1].
N,N'-DME-N-PEG2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
sulfo-SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4) via the sulfo-SPDB linker.
Cevipabulin fumarate (TTI-237 fumarate) is a microtubule-active, oral active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line[1][2].
(+)-Bicuculline is a light-sensitive competitive antagonist of GABA-A receptor.
3,4-Dibromo-Mal-PEG4-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ABT-670 is a selective, oral bioavailable agonist of dopamine D4 receptor, with EC50 of 89 nM, 160 nM, and 93 nM for human D4, ferret D4, and rat D4, respectively.
Platycoside E is a platycodigenin-type saponin isolated from the root of Platycodon grandiflorum with haemolytic activity and adjuvant potential. Platycoside E promotes the production of the sera OVA-specific IgG2a and IgG2b antibody in the ovalbumin (OVA)-immunized mice[1].
Goralatide TFA is an inhibitor of cell cycle progression. Goralatide TFA enhances selectivity of hyperthermic purging of human progenitor cells. Goralatide TFA has the potential for the research of leukemia[1].
p-NH2-CHX-A"-DTPA is a bifunctional chelating agent[1].
Naproxen sodium is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
Acacetin 7-O-β-D-glucuronopyranosyl-(1→2)[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside (compound 8) is a flavonoid glycoside that can be obtained from black locust (Leguminosae ) isolated from leaf extract[1].
Tolperisone is a centrally acting muscle relaxant, is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.
Balofloxacin is quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.Target: Antibacterial; DNA gyrase.Balofloxacin, an orally active fluoroquinolone antibiotic, has been developed by Choongwae Pharma in Korea, for the treatment of urinary tract infection (UTI). Chugai and Ciba were developing balofloxacin for respiratory tract infections (RTI) but discontinued development in 1995 due to changes in Chugai's R&D focus and a lack of efficacy of the drug. Following phase II trials, Choongwae bought the rights to develop balofloxacin in Korea from Chugai. Phase III trials for UTI were completed in early 2001. Balofloxacin was approved by the Korean FDA in December 2001 for UTI. In March 2002, phase II trials were underway for RTI.
eIF4A3-IN-10 (compound 58) is a silvestrol (HY-13251) analogue. eIF4A3-IN-10 interferes the assembling of eIF4F translation complex with EC50s of 35 and 100 nM for myc-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-10 can be used for the research of human cancer pathogenesis[1].
Deoxycholic acid (cholanoic acid) sodium hydrate，a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5[1][2].
Tuvirumab (OST 577; SDZ-OST 577) is a human IgG1 subclass monoclonal antibody directed against HBV surface antigen (HBsAg). Tuvirumab binds specifically and with high affinity (K=3.6 nM) to HBsAg. Tuvirumab has the potential for chronic hepatitis B research[1][2].
Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM[1].
BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 uM in ADP-Glo Assay.IC50 value: 37 uMTarget: ITPKA inhibitorBAMB-4 exhibit the lowest inhibition frequency among the InsP3-Kinase inhibitors. only in one from 42 targets tested,BAMB-4 showed an inhibitory effect. Noteworthy, in kinasescreens no targets of BAMB-4 were detected, indicating that thecompound does not belong to the typical kinase inhibitors. Thus,the relative high speci?city and the high cellular uptake ofBAMB-4 now for the ?rst provide the possibility to effectively inhibit InsP3kinase in vivo. e InsP3Kinase activity is essentially involved in ITPKA promoted metastasis of lung cancer cells, BAMB-4 is a promising therapeutic approach in lung cancertherapy.