ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-turmerone ((+)-ar-Turmerone) activates apoptotic protein in human lymphoma U937 cells[3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation and constitutes a promising therapeutic agent for various neurologic disorders[4][5].
Shinjulactone M is a quassinoid isolated from various parts of Ailanthus species. Ailanthus, an important genus of the Simaroubaceae family, can be used as an febrifuge (antimalarial) and anthelmintic, and is given for the research of chronic bronchitis, epilepsy and asthma[1].
Cap-dependent endonuclease-IN-22 is a potent cap-dependent endonuclease (CEN) inhibitor[1].
L-threo-PPMP is a GlcT (UDP-Glc: Ceramide β1,1glucosyltransferase) inhibitor. L-threo-PPMP inhibits glycosphingolipid biosynthesis and induces apoptosis. L-threo-PPMP has anti-cancer activity[1].
Benzyl-PEG6-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Selicrelumab is an agonist CD40 antibody, induces changes in the tumor microenvironment. Selicrelumab can be used for the research of pancreatic cance and neoadjuvant study[1].
L-Azidohomoalanine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent[1][2].
Recaticimab (SHR-1209) is a humanized monoclonal antibody that inhibits PCSK9. Receticimab mediates the degradation of PCSK9 by binding to PCSK9, increasing the level of low-density lipoprotein (LDL) receptors on the surface of hepatocytes, reducing the level of LDL in plasma, and achieving the goal of lowering blood lipids. Recaticimab has potential application in hypercholesterolemia[1][2].
L-NIO is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively[1][2]. L-NIO induces a consistentfocal ischemic infarctin rats[2].
PM-1, a derivative of Thioflavin-T (ThT; HY-D0218), is a small but highly specific plasma membrane (PM) fluorescent dye for specific and long-time membrane imaging of living and fixed cells. PM-1 is embedded directly into the cell membrane and exhibits a very long retention time on the plasma membrane with a half-life of approximately 15 h. PM-1 can be used in combination with protein labeling probes to study ectodomain shedding and endocytosis processes of cell surface proteins[1].
DOBAQ, a cationic lipid, is a pH-sensitive lipid. DOBAQ can be used for liposomes applied in drug delivery[1].
Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
Agrochelin, an alkaloid cytotoxic antibiotic, is produced by the fermentation of a marine Agrobacterium sp. Agrochelin has cytotoxic activity in tumor cell lines[1].
N,N'-Diacetylchitobiose is a dimer of β(1,4) linked N-acetyl-D glucosamine. N,N'-Diacetylchitobiose is the hydrolysate of chitin and can be used as alternative carbon source by E. coli[1].
GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase[1][2][3].
m-PEG3-Aminooxy is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Methoxycarbonyl-D-Nle-Gly-Arg-pNA is a synthetic trypsin that can serve as a substrate for coagulation factors IXa (FIXa) and Xa (FXa)[1][2][3].
Sparfosic acid trisodium, is a potent inhibitor of aspartate transcarbamoyl transferase, with anti-tumor and antimetabolite activity. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis[1][2].
Dicarbine blocks dopamine receptors in various brain parts and prevents the depression of the conditioned defence reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine could be used to treat patients with schizophrenia and alcoholic psychosis in clinical[1][2].
Nortrachelogenin-8'-O-β-glucoside is a natural product that can be isolated from the dried roots of Pulsatilla koreana. Nortrachelogenin-8'-O-β-glucoside inhibits cancer cell proliferation and reduces hormone dependence[1][2].
Bis-PEG7-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.IC50 value: 9 nM(VEGFR2); 15 nM(CSF1R); 80 nM (Kit activated) [1]Target: VEGFR2/Kit/CSF1Rin vitro: OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. Moreover, OSI-930 also induces apoptosis in HMC-1 cell line with EC50 of 34 nM [1]. A recent study shows that OSI-930 inactivates purified, recombinant cytochrome P450 (P450) 3A4 with a Ki of 24 μM in a time- and concentration-dependent mode [2].in vivo: OSI-930, administrated at the maximally efficacious dose of 200 mg/kg by oral gavage, exhibits potent antitumor activity in a broad range of preclinical xenograft models including HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models [1].
Dnp-PYAYWMR is a peptide substrate that selectively targets MMP3. Dnp-PYAYWMR is cleaved by MMP3 to produce Dnp-PYA (nonfluorescent) and YWMR (fluorophore detectable at 360 nm). After incubation of MMP3 with Dnp-PYAYWMR for 2 h, MMP3 fluorescence intensity was measured. Ex/Em=328/350 nm[1].
NM107 is a inhibitors of HCV RNA replication with IC50 of 7.0 μM in vitro.IC50 value: 7.0 μMTarget:HCV RNA replicationNM107 is a potent and selective inhibitor of flavi- and pesti-virus replication in cell culture, with inhibitory activity and cytotoxicity against HCV 1b replicon cells, IC50 is 1.13 μM. Intracellular HCV RNA in HCV-infected cells treated the HCV polymerase inhibitor NM107 shows a similar pattern of decline. NM107 are currently being investigated as additional therapeutic agents for HCV infection. NM107 inhibits bovine viral diarrhea virus (BVDV) replication (EC50 0.67 nM), eliminates persistent BVDV infection at nontoxic concentrations.
ANO1-IN-1 (Compound 9c) is a selective ANO1 channel blocker with an IC50 of 2.56 μM and 15.43 μM against ANO1 and ANO2, respectively. ANO1-IN-1 suppresses strongly proliferation of glioblastoma cells[1].
Dye 937, substituted unsymmetrical cyanine dyes with selected permeability, useful in the detection of DNA in electrophoretic gels.
PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.