BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM.
Ethyl red (1,1'-Diethyl-2,4'-cyanine) iodide is an azo dye and acid–base indicator[1][2].
Lycoclavanol is a serratane-type triterpenoid, which can be isolated from the dried whole plants of Lycopodium japonicum[1].
CP-640186 is an isozyme-nonselective acetyl-CoA carboxylase (ACCase) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively; with improved metabolic stability vs CP-610431.IC50 value: 53 nM/61 nM (rat liver ACC1/skeletal muscle ACC2) [1]Target: acetyl-CoA carboxylasein vitro: CP-640186, also inhibited both isozymes with IC50s of ~55 nM but was 2–3 times more potent than CP-610431 in inhibiting HepG2 cell fatty acid and TG synthesis. CP-640186 also stimulated fatty acid oxidation in C2C12 cells (ACC2) and in rat epitrochlearis muscle strips with EC50s of 57 nM and 1.3 uM [1]. in vivo: In rats, CP-640186 lowered hepatic, soleus muscle,quadriceps muscle, and cardiac muscle malonyl-CoAwith ED50s of 55, 6, 15, and 8 mg/kg. Consequently, CP-640186 inhibited fatty acid synthesis in rats, CD1 mice,and ob/ob mice with ED50s of 13, 11, and 4 mg/kg, andstimulated rat whole body fatty acid oxidation with anED50 of ~30 mg/kg [1].
25-O-Methylalisol A is a protostane triterpenoids isolated from Alisma orientale. The dried rhizomes of the aquatic plant Alisma orientale known as Rhizoma Alismatis is a common traditional Chinese medicine used for diuretic, anti-inflammatory, and hypolipidemic purposes, as well as the treatment of diabetes[1].
Gly-Pro-Glu is a neuroactive peptide with a potent action on acetylcholine release. Gly-Pro-Glu is the N-terminal tripeptide of insulin-like growth factor-I. Gly-Pro-Glu inhibits glutamate binds to N-methyl-D-aspartate (NMDA) receptor with an IC50 value of 14.7 μM. Gly-Pro-Glu can be used for the research of neuroprotection [1][2].
Bis(2,5-dioxopyrrolidin-1-yl) octadecanedioate is a linking reagent used in organic synthesis[1].
Endothelin 1 (swine, human) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ETA and ETB.
Scopolamine Methyl Nitrate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
1,2-Distearoyl-sn-glycero-3-phosphate-d70 (sodium) is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphate.
Z-Lys(Z)-OSu is a lysine derivative[1].
G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER) antagonist with a Ki of 20 nM[1][2].
Schisandrin has various therapeutic effects on a range of medical conditions such as anti-asthmatic, anti-cancer, and anti-inflammatory effects.IC50 value:Target:in vitro: Sch inhibited the pro-fibrotic activity of TGF-β1 in AML12 cells; thus, it suppressed the accumulation of ECM proteins. Also, Sch inhibited the EMT as assessed by reduced expression of vimentin and fibronectin, and increased E-cadherin and ZO-1 in TGF-β1 induced AML12 cells. Sch reduced TGF-β1-mediated phosphorylation of Smad2/3 and Smad3/4 DNA binding activity. On the other hand, Sch reduced TGF-β1-induced ERK1/2 and PI3K/Akt phosphorylation in the non-Smad pathway [1]. the anti-inflammatory properties of schisandrin result from the inhibition of nitric oxide (NO) production, prostaglandin E(2) (PGE(2)) release, cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression, which in turn results from the inhibition of nuclear factor-kappaB (NF-kappaB), c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (MAPK) activities in a RAW 264.7 macrophage cell line [2].
1-Chloro-4-methoxybenzene-d4 is the deuterium labeled 1-Chloro-4-methoxybenzene[1].
GF 15 is a potent inhibitor of centrosomal clustering in tumor cells.
2-Amino-6-chloro-9-(3-deoxy-3-fluoro-beta-D-ribofuranosyl)-9H-purine ((2R,3S,4S,5R)-2-(2-Amino-6-chloro-9H-purin-9-yl)-4-fluoro-5-(hydroxymethyl)tetrahydrofuran-3-ol) is a purine nucleoside analogue. 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].
Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle[1].
Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor.
APOBEC3G-IN-1 (MN136.0185) is a potent HIV inhibitor, targeting APOBEC3G[1].
Z62954982 is a potent, specific Rac1 inhibitor, reduces the intracellular levels of Rac1-GTP in a concentration-dependent manner with IC50 of 12 uM, 4 times more effective than NSC23766 (IC50=50 uM); causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC.
Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the treatment of infections caused by a diverse group of bacterial species[1][2][3].
FLT3-IN-16 is a potent FLT3 inhibitor with an IC50 of 1.1 μM. FLT3-IN-16 can be used for researching acute myeloid leukemia[1].
Helioxanthin 8-1 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV/HCV/HSV-1/HIV activity with EC50 of >5/10/1.4/15 uM.IC50 value: >5/10/1.4/15 uM(HBV/HCV/HSV-1/HIV) [1]Target: Antiviral agentThe cyclic hydrazide 28(Helioxanthin 8-1) showed the most potent antiHBV activity among those helioxanthin analogues tested. In addition, compound 28 exhibited moderately potent activity against HIV. It would therefore be promising to study helioxanthin analogues that contain a six-membered ring instead of the five-membered ring found in the lactam [1]. 8-1 exhibited effective inhibition on DHBV replication. The combination of 8-1 with 3TC resulted in additional anti-DHBV activity. Viral induced cells displayed higher susceptibility to 8-1 treatment than non-induced cells. HBV X protein might not be an essential factor in the initiation of the biological activity of 8-1, as demonstrated by its absence in DHBV [2].
TAS0728 is a potent, selective, oral active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity[1].
Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor, plays an important role in the regulation of the inflammatory response and the progression of some cancers[1].
3-Methylpyrazole is used as a nitrification inhibitor of nitrification in soil[1].
α-Cyanopyridine-d4 is the deuterium labeled α-Cyanopyridine[1].
Carbaryl-d3 is the deuterium labeled N6-(carboxymethyl)-L-lysine[1].
LY 292728 is a potent leukotriene B4 (LTB4) receptor antagonist. LY 292728 binds to human neutrophils with a Ki of 0.47 nM and binds to guinea pig lung membranes with a Ki of 0.04 nM[1].
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist[1][2].