Temporin L is a potent antimicrobial peptide and is active against Gram-negative bacteria and yeast strains. Temporin L also has antiendotoxin properties[1][2].
1-Bromodecane-d21 is the deuterium labeled 1-Bromodecane[1].
Zomepirac-d4 sodium salt is the deuterium labeled Zomepirac sodium salt. Zomepirac sodium salt (McN-2783-21-98) is a potent prostaglandin biosynthesis inhibitor. Zomepirac sodium salt is a non-steroidal anti-inflammatory drug (NSAID). Zomepirac sodium salt can cause immune-mediated liver injury[1][2].
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[1][2][3][4].
Resorcinol monoacetate is an antiseptic and a disinfectant, is a chemical intermediate for the production of many other pharmaceuticals, and can be used to treat acne, seborrheic dermatitis, eczema, psoriasis, and other skin disorders.
Triptobenzene H (Hypoglic acid) significantly increases TNF-α and IL-1β mRNA levels in macrophages, causing indirect liver damage[1].
PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4[1][2].
(6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one (compound7) is a nature product isolated from rhizomes of Curcuma kwangsiensis. (6E)-1,7-Bis(4-hydroxyphenyl)-6-hepten-3-one has inhibitory effect on NO production induced by LPS in macrophages with an IC50 value of 8.93 μM[1].
NS1-IN-1 (compound 3) is a potent NS1 inhibitor. NS1 is a major influenza A virus virulence factor that inhibits host gene expression. NS1-IN-1 decreases viral protein levels, contributing to the reduction of virus replication. NS1-IN-1 shows antiviral activity by repressing the activity of mTORC1 in a TSC1-TSC2-dependent manner[1].
BL-918 is a small molecule activator of ULK1 with EC50 of 24 nM (243% kinase activity at 100 nM), induces autophagy via the ULK complex in SH-SY5Y cells; displays a cytoprotective effect on MPP+-treated SH-SY5Y cells, as well as protected against MPTP-induced motor dysfunction and loss of dopaminergic neurons by targeting ULK1-modulated autophagy in mouse models of PD.
γ-Secretase modulator 13 (compound 4) is a gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC50 value of 163 nM. γ-Secretase modulator 13 can be used in the study of Alzheimer's disease[1].
AHR agonist 3 is an aryl hydrocarbon receptor (AhR) agonist, that can induces cell cycle arrest or apoptosis via activation of tumor-suppressive transcriptional programs. AHR agonist 3 inhibits triple-negative breast cancer (TNBC) stem cell growth via AhR while exhibits minimal cytotoxicity against normal human primary cells and can be used for cancer research[1].
O-Nornuciferine, an aporphine-type alkaloid from lotus leaf, is a potent hERG channel inhibitor[1].
AZD7545 is a novel, selective small-molecule inhibitor of PDHK2 (PDH kinase2) with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2 respectively.IC50 Value: 36.8 nM (PDHK1); 6.4 nM (PDHK2) [1]Target: PDHK1/2in vitro: The IC50 values for inhibition of PDHK2 and PDHK1 by AZD7545 were 6.4 ± 2.2 nM (n = 6) and 36.8 ± 18 nM (n = 3) respectively. Other compounds in this series inhibited both PDHK1 and PDHK2 and a consistent trend of reduced potency (5-15-fold) towards PDHK1, as compared with PDHK2, was observed. In contrast, AZD7545 and related compounds failed to inhibit PDHK4 and paradoxically, at higher concentrations (>10 nM), AZD7545 stimulated PDHK4 activity [1]. In the presence of PDHK2, AZD7545 increased PDH activity with an EC(50) value of 5.2 nM. In rat hepatocytes, the rate of pyruvate oxidation was stimulated 2-fold (EC(50) 105 nM) [2].in vivo: A single dose of AZD7545 to Wistar rats increased the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner from 24.7 to 70.3% at 30 mg/kg; and in skeletal muscle from 21.1 to 53.3%. A single dose of 10 mg/kg also significantly elevated muscle PDH activity in obese Zucker (fa/fa) rats. Obese, insulin-resistant, Zucker rats show elevated postprandial glucose levels compared with their lean counterparts (8.7 versus 6.1 mM at 12 weeks old). AZD7545 (10 mg/kg) twice daily for 7 days markedly improved the 24-h glucose profile, by eliminating the postprandial elevation in blood glucose [2]. An interestingobservation is that administration of maximally effective doses of AZD7545 and related compounds to rats results in the near-complete activation of PDH activity in liver, where PDHK2 is the major isoenzyme, while only partial activation of PDH activity is achieved in skeletal muscle and heart, tissues which express high levels of PDHK4. For example, following administration of a maximally effective dose of compound K (30 mg/kg) the percentage of PDH present in the active (dephosphorylated) state in liver is elevated from 35.3 ± 4.0% to 90.2 ± 2.2% while in skeletal muscle and heart PDH activity plateaus at 64.3 ± 2.3% and 61.8 ± 4.3% respectively. Further evidence for a link between in vitro isoenzyme selectivity and in vivo activity comes from the observation that in fasted rats the ability of AZD7545 toelevate PDH activity in liver is intact, while the activation of skeletal muscle PDH activity in response to the compound is severely blunted [1].
BAY 41-2272 is a soluble guanylate cyclases (sGC) activator.Target: guanylate cyclaseBAY 41-2272 is a recently introduced novel orally available agent that directly stimulates soluble guanylate cyclase (sGC) and sensitizes it to its physiological stimulator, nitric oxide. BAY 41-2272 is a promising new therapeutic agent that goes beyond current therapeutic agents. BAY 41-2272 acts as an arterial vasodilator, resulting in a reduction of MAP and pulmonary artery pressure and a decrease in SVR and renal vascular resistance. BAY 41-2272 reduces pulmonary capillary wedge pressure in the absence of a decrease in right atrial pressure. [2]
Phosphatidylglycerol is a naturally occurring anionic phospholipid that is a component of plant, animal and bacterial cell membranes. It is present in prokaryotes and eukaryotes less than phosphatidylethanolamine, and in eukaryotes less than phosphatidylcholine. It is formed by the reaction between CDP-diglyceride and L-α-glycerol 3-phosphate followed by dephosphorylation and is the metabolic precursor of cardiolipin. Phosphatidylglycerols containing polyunsaturated and monounsaturated fatty acyl chains inhibit and promote the proliferation of murine keratinocytes, respectively. Phosphatidylglycerol is the second-largest lipid component of mammalian lung surfactant, accounting for 10% of lipids, and has reduced levels of pulmonary surfactant in infants with respiratory distress syndrome. Phosphatidylglycerol (egg) is a mixture of phosphatidylglycerols isolated from eggs with various fatty acyl groups at the sn-1 and sn-2 positions. References: [1]. Ohtsuka, T., Nishijima, M., and Akamatsu, Y. Phosphatidylglycerol phosphate synthase-deficient somatic mutants with impaired phosphatidylglycerol and cardiolipin biosynthesis J. Biol. Chemical. 268(30), 22908-22913 (1993).[2]. Furse, S. Are phosphatidylglycerols essential for terrestrial life? J. Chemistry. biology. 10(1), 1-9 (2016).[3]. Xie, D., Seremwe, M., Edwards, JG, et al. Different effects of different phosphatidylglycerols on the proliferation of mouse keratinocytes PLoS One 9(9), e107119 (2014).
2’,3’,5’-Tri-O-benzoyl-2’-β-C-methyl-3-deazauridine 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].
REV7/REV3L-IN-1 is a REV7/REV3L interaction inhibitor with an IC50 of 78 μM, which directly binds to REV7 in nuclear magnetic resonance analyses, and inhibits the reactivation of a reporter plasmid containing an interstrand crosslink (ICL) in between the promoter and reporter regions[1].
TRPV2-selective blocker 1 (compound IV2-1) is a selective TRPV2 channel blocker with an IC50 of 6.3 μM. TRPV2-selective blocker 1 does not affect TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 also inhibits TRPV2-mediated Ca2+ influx in macrophages, and inhibits macrophage phagocytosis[1].
Toltrazuril sulfone is an antiprotozoal agent that acts upon Coccidia parasites.IC50 Value:Target: AntiparasiticPonazuril (INN, Toltrazuril sulfone), sold by the Bayer Corporation under the trade name Marquis, is a drug currently approved for the treatment of equine protozoal myeloencephalitis in horses, caused by Sarcocystis neurona. More recently, veterinarians have been preparing a formulary version of the medication for use in small animals such as cats and dogs against coccidia, an intestinal parasite. Coccidia treatment is far shorter than treatment for EPM. Ponazuril (INN, Toltrazuril sulfone) is useful for Antiprotozoal.
HADA Hydrochloride is a blue fluorescent D-amino acid (FDAA). FDAAs are efficiently incorporated into the peptidoglycans (PGs) of diverse bacterial species at the sites of PG biosynthesis, allowing specific and covalent probing of bacterial growth with minimal perturbation[1].
DL-Norepinephrine hydrochloride is a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine．DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors, has an increasing effect on subendocardial oxygen tension[1].
Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.
SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM[1][2].
Diclofenac-13C6 is the 13C6 labeled Diclofenac. Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
Sodium Propionate-d3 is the deuterium labeled Sodium Propionate[1].
Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases[1][2].
γ-Glutamyl-S-allylcysteine (L-γ-Glutamyl-(S)-Allyl-Cysteine) is a naturally occurring organosulfur compound found in garlic. γ-Glutamyl-S-allylcysteine has antiglycative effect and shows radical-scavenging and metal-chelating capacities[1][2].
Tubulin polymerization-IN-47 (Compound 4h) is a tubulin polymerization inhibitor and mitotic inhibitor. Tubulin polymerization-IN-47 inhibits neuroblastoma cancer cell proliferation, with IC50s of 7 and 12 nM for Chp-134 and Kelly cell line[1].
BODIPY 576/589 is a long wavelength biological labeled dye[1].