Amphotericin B methyl ester hydrochloride is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B methyl ester hydrochloride is the cholesterol-binding compound possesses significant antifungal activity. Amphotericin B methyl ester hydrochloride disrupts HIV-1 particle production and potently inhibits HIV-1 replication[1][2].
Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer[1].
Ardisiacrispin A (Deglucocyclamin) is a common triterpenoid saponin from Ardisia species. Ardisiacrispin A has similar biological properties with some triterpenoid saponins in A. crenata which is one of the species of genus Ardisia and exhibits cytotoxic effect on tumor cells, immunomodulatory and antiviral activities[1].
9-PAHPA is a fatty acid esters of hydroxy fatty acid (FAHFA). FAHFAs are a new family of endogenous lipids, have antidiabetic and anti-inflammatory effects[1].
JT001 (NLRP3-IN-19) is a potent, specific and orally active inhibitor of NLRP3. JT001 can inhibit NLRP3 inflammasome assembly, resulting in the inhibition of cytokine release and the prevention of pyroptosis. JT001 can be used for the research of nonalcoholic steatohepatitis and liver fibrosis[1].
Indican (Indoxyl-β-D-glucoside), a glycoside of indoxyl, is a precursor of the dyesindigo and indirubin. Indican has a major metabolite, indoxyl sulfate (IS). IS, an uremic toxin, is a substrate/inhibitor of organic anion transporter (OAT) 1, OAT 3 and multidrug resistance-associated protein (MRP) 4[1][2].
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy[3].
Digoxin is a potent inhibitor of Na+/K+-ATPase, clinically used to treat arrhythmia and heart failure.
Cyanine 3.5 (Cy3.5 NHS ester) chloride is an analog of Cy3.5 fluorophore. Cyanine 3.5 chloride is a reactive, red fluorescent dye. Cyanine 3.5 chloride is used for labeling of amino-groups in peptides, proteins, and oligonucleotides. (λex=591 nm, λem=604 nm)[1][2].
Ornipressin is a potent vasoconstrictor, hemostatic and renal agent. Sequence: Cys-Tyr-Phe-Gln-Asn-Cys-Pro-{Orn}-Gly-NH2 (Disulfide bridge: Cys1-Cys6).
N-Octyl 4-hydroxybenzoate-d4 is the deuterium labeled N-Octyl 4-hydroxybenzoate[1].
Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) agonist. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation[1].
Enpp-1-IN-6 is a potent inhibitor of ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1). The ENPP 1 has broad specificity and can cleave a variety of substrates, including phosphodiester bonds of nucleotides and nucleotide sugars and pyrophosphate bonds nucleotides and nucleotide sugars. Enpp-1-IN-6 has the potential for the research of cancer and infectious diseases (extracted from patent WO2021203772A1, compound 51)[1].
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
Aurein 5.2 is an antibiotic antimicrobial peptide[1].
Parasin I is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
Diprenorphine is a non-selective opioid antagonist with Ki values of 0.017, 0.072 and 0.23 nM against κ-, μ- and δ-opioid receptors, respectively[1]. Diprenorphine can be used for central poststroke pain (CPSP) research[1].
Dacomitinib is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection.
Anticancer agent 31 is a 1,3-diphenylurea quinoxaline derivative, and a anticancer agent. Anticancer agent 31 exhibits antitumor acitvity by arresting cell cycle at S phase and inducing apoptosis[1].
JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity[1].
Fuzapladib (IS-741) is a potent phospholipase A2 inhibitor. Fuzapladib can block the adhesion of inflammatory cells to microvascular endothelial cells, inhibit the infiltration of neutrophils into the pancreas or acute pancreatitis, and has anti-acute pancreatitis effects[1].
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors[1][2][3].
C-12 NBD cholesterol is a cholesterol derivative with a hydrophilic fluorophore tag (NBD: Ex=465 nm, Em=535 nm). C-12 NBD cholesterol can be used to study the utilization and metabolism of cholesterol[1].
2’,3’,5’-Tri-O-benzoyl-5-methoxyuridine 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].
(R)-VT104 is the R-enantiomer of VT104. (R)-VT104 shows an IC50 value of 0.1-1 μΜ for firefly luciferase. VT104 is an orally active and pan-TEAD auto-palmitoylation inhibitor[1].
N-(tert-Butoxycarbonyl)-O-(tetrahydro-2H-pyran-2-yl)-L-serine is a serine derivative[1].
Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.IC50 Value: 4 nM [1]Target: microtubulein vitro: Cytotoxic IC(50) values of CA-4 in human bladder cancer cells were below 4 nM. Analyses of cell-cycle distribution showed CA-4 obviously induced G(2)-M phase arrest with sub-G(1) formation. The analyses of apoptosis showed that CA-4 induced caspase-3 activation and decreased BubR1 and Bub3 in cancer cells [1]. The enhanced apoptosis induced by dasatinib plus CA-4 was accompanied by a greater extent of mitochondrial depolarization, caspase-3 activation and PARP cleavage in HO-8910 cells. Furthermore, elevated expression of Mcl-1 led to a reduced apoptosis induced by dasatinib plus CA-4, highlighting that downregulated Mcl-1 was necessary for the potentiating effect of dasatinib to CA-4-triggered apoptosis [2].in vivo: The increased anticancer efficacy of dasatinib combined with CA-4 was further validated in a human HO-8910 ovarian cancer xenograft model in nude mice [2]. There was a significant, concentration dependent increase in mean arterial blood pressure with a maximum increase of about 60% of the baseline MAP at 30 mg/kg of CA4P compared to the saline control. However, there was no significant increase in the cardiac troponin I level after CA4P injection [3].Clinical trial: A phase II trial of fosbretabulin in advanced anaplastic thyroid carcinoma and correlation of baseline serum-soluble intracellular adhesion molecule-1 with outcome [4].
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells[1].