Kanshone A is a sesquiterpene isolated from the roots of Nardostachys chinensis (Valerianaceae). Kanshone A shows cytotoxic with an IC50 value of 7.0 µg/ml in P388 cells[1][2].
Tyr0-Neurokinin A is a neuropeptide belongs to tachykinin peptide family. Tyr0-Neurokinin A is an agonist of Tacr2. Tyr0-Neurokinin A can be used in the research of insulin resistance, obesity, diabetes[1][2].
5α-Cholesta-7,24-dien-3β-ol, a sterol, can be found in hamster cauda epididymal mature spermatozoa[1].
CU06-1004 (Sac-1004) is an orally active endothelial dysfunction blocker. CU06-1004 ameliorates endothelial dysfunction by inhibiting hyperpermeability and inflammation, and is potent in inhibiting vascular leakage and inflammation in various animal models, such as diabetic retinopathy, stroke, cancer, and inflammatory bowel disease. CU06-1004 ameliorates CDAA-induced mouse model of NASH. CU06-1004 also improves cardiac function[1][2][3].
MNG-14a is an amphiphilic compound that can be used to aid the isolation of membrane proteins, and functional and structural determination of membrane proteins[1].
Fibracillin is a penicillin antibiotic.
Deruxtecan-d6 is the deuterium labeled Dehydroepiandrosterone sulfate (sodium hydrate)[1].
Dimethyl sulfoxide (DMSO) is an aprotic solvent that dissolves both polar and nonpolar compounds. Dimethyl sulfoxide has anti-freezing and bacteriostatic properties[1][2].
Roxithromycin is a semi-synthetic macrolide antibiotic.Target: AntibacterialRoxithromycin is a semi-synthetic macrolide antibiotic. It is used to treat respiratory tract, urinary and soft tissue infections. Roxithromycin is derived from erythromycin, containing the same 14-membered lactone ring. Roxithromycin prevents bacteria from growing, by interfering with their protein synthesis. Roxithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides. Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila. From Wikipedia.
N6-Ethyl-2’-O-methyladenosine 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].
1-O-trans-Cinnamoyl-β-D-glucopyranose is a nature product. 1-O-trans-Cinnamoyl-β-D-glucopyranose can be isolated from fruits[1].
Tetralysine is a cationic moietie that may be used in the construction of gene delivery vectors and DNA nanoparticles[1].
Obatoclax is an antagonist of the BCL-2 family proteins. It binds to BCL-2 with a Ki of 220 nM.
PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity[1].
Cidofovir diphosphate is an active intracellular metabolite of Cidofovir. Cidofovir diphosphate is a selective inhibitor of viral DNA polymerases with Ki values of 6.6, 0.86 and 1.4 μM for HCMV, HSV-1 and HSV-2 DNA polymerase, respectively[1][2].
11-Hydroxyrankinidine is an alkaloid compound isolated from the whole plant of Gelsemium elegans[1].
RG-101 is a hepatocyte targeted N-acetylgalactosamine conjugated oligonucleotide that antagonises miR-122. miR-122 is an important host factor for hepatitis C virus (HCV) replication[1].
Mca-Arg-Pro-Lys-Pro-Tyr-Ala-Nva-Trp-Met-Lys(Dnp)-NH2 is a biological active peptide. (MMP substrate)
Lei-Dab7 is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
Hexamethylphosphoramide-d18 is the deuterium labeled Hexamethylphosphoramide[1].
Bunazosin hydrochloride is a potent and selective α1-adrenoceptor antagonist. Bunazosin hydrochloride can be used for antihypertensive and ocular hypotensive research[1].
Fmoc-Trp(Boc)-Ser(psi(Me,Me)pro)-OH is a dipeptide.
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries. IC50 value: 3.4 nM [1]Target: HT2B receptorin vitro: PRX-08066 inhibits 5-HT-induced mitogen-activated protein kinase activation with IC50 of 12 nM and markedly reduces thymidine incorporation with IC50 of 3 nM in Chinese hamster ovary cells expressing the human 5-HT2BR, which suggests that PRX-08066 can potentially inhibit the pathologic 5-HT-induced vascular muscularization associated with PAH [1]. PRX-08066 inhibits cell proliferation with IC50 of 0.46 nM and with a maximum inhibition of 20% and 5-HT secretion with IC50 of 6.9 nM with a maximum inhibition of 30% in the 5-HT(2B) expressing SI-NET cell line, KRJ-I. PRX-08066 inhibits isoproterenol-stimulated 5-HT release with IC50 of 1.25 nM and a maximum inhibition of 60% in NCI-H720 cells. PRX-08066 (0.5 nM) significantly inhibits ERK phosphorylation in KRJ-I cells. PRX-08066 inhibits TGFβ1, CTGF and FGF2 transcription and secretion in KRJ-I cells. PRX-08066 decreases level of transcripts for Ki67 (84%) as well as Ki67 protein (36.8%) associated with an increase in caspase 3 transcript levels in KRJ-I cells. PRX-08066 decreases level of transcripts of TGFβ1, FGF2 and TPH1 in KRJ-I cells. PRX-08066 significantly increases the number of dead cells (34%) compared with untreated controls in KRJ-I cells. PRX-08066 causes a significant increase in dead/caspase 3 positive cells (76%) and caspase 3 activity (52%) in HEK293 cells [2].in vivo: PRX-08066 (100 mg/kg) treated groups demonstrates less right ventricular hypertrophy and septal flattening than the monocrotaline control group in rats. PRX-08066 significantly reduces peak pulmonary artery pressure at 50 mg/kg and 100 mg/kg compared with monocrotaline control rats. PRX-08066 also significantly reduces right ventricle (RV)/body weight and RV/left ventricle + septum, compared with MCT-treated rats. PRX-08066 significantly attenuates the elevation in pulmonary artery pressure and RV hypertrophy and maintains cardiac function. PRX-08066 significantly reduces the hypoxia-dependent increase in right ventricular systolic pressure in both rats and mice without affecting the systemic mean arterial pressure in the animals [1]. PRX-08066 (100 mg/kg) significantly inhibits both right ventricular systolic pressure and right ventricular/left ventricular +septum weight elevations in rats. PRX-08066 (30 mg/kg) inhibits right ventricular systolic pressure and monocrotaline-induced ERK phosphorylation in whole lung homogenates in rats [3].
CDK7-IN-5 is a CDK7 inhibitor with an IC50 value <100 nM. CDK7-IN-5 has anticancer effects. (WO2015154022A1 (Compound 104))[1].
2’,3’-Bis(O-t-butyldimethylsilyl)-2-thiouridine 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].
Febuxostat sec-butoxy acid is an impurity of Febuxostat. Febuxostat is selective xanthine oxidase inhibitor with a Ki of 0.6 nM[1].
Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
Methyl 5-hydroxypyridine-2-carboxylate is a phenolic acid that can found in the stems of Mahonia fortune. Methyl 5-hydroxypyridine-2-carboxylate exhibits NO inhibitory effects in vitro[1].
Ac-AAVALLPAVLLALLAP-YVAD-CHO is a cell-permeable caspase-1 inhibitor that has antitumor activity[1].
(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research[1].