COX-2/5-LOX-IN-1 (compound 3a) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-1 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-1 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 12.13, 0.4 and 4.96 μM, respectively[1].
Gelsevirine is the major alkaloid in Gelsemium elegans with potent anxiolytic effects. The anxiolytic mechanism of Gelsevirine may be involved in the agonist action of the glycine receptor in the brain. Gelsevirine has anti-proliferation activity with IC50 values of 1.41 mM and 1.22 mM for SW480 cells and MGC80-3 cells, respectively[1][2][3].
(S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH (VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH) is a E3 ligase ligand-linker conjugate that contains on one end a VHL ligand. (S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH is used in PROTAC technology[1].
Mal-AMCHC-N-Propargylamide is a click chemistry reagent containing an azide group. Mal-AMCHC-N-Propargylamide can be a bio-conjugation reagent for antibody-drug-conjugate synthesis using Click-Chemistry[1].
SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
ML355 is a potent and selective inhibitors of 12-Lipoxygenase(12-LOX) with IC50 of 0.34 μM, excellent selectivity over related lipoxygenases and cyclooxygenases, and possess favorable ADME properties.IC50 value: 0.34 μM [1]Target: 12-LOXML355 inhibits PAR-4 induced aggregation and calcium mobilization in human platelets and reduce 12-HETE in β-cells.
4-Nitrophenyl β-D-Cellobioside (p-Nitrophenyl β-D-cellobioside) is a cellotriose analog, a chromogenic substrate for the detection of cellulase activity. Exoglucanases, endoglucanases, and β-glucosidases hydrolyze 4-Nitrophenyl β-D-Cellobioside to yield p-nitrophenol (PNP)[1][2].
α-Glucosidase-IN-37 (Compound 11) moderately inhibits LPS-induced NO production with an IC50 value of 23.7 μM in macrophages. α-Glucosidase-IN-37 has weak inhibitory activity against α-Glucosidase[1].
Bifonazole is an imidazole antifungal drug.Target: AntifungalBifonazole, a new broad-spectrum antimycotic, interferes with sterol biosynthesis. In dermatophytes bifonazole additionally inhibits directly HMG-CoA-reductase. bifonazole possesses a sequential mode of action, namely inhibition of cytochrome P450-dependent C14-demethylation of sterols and direct inhibition of HMG-CoA-reductase. In vitro bifonazole shows a strongly pH-dependent efficacy. The uptake kinetics of bifonazole have been measured with different pathogens [1]. Bifonazole additionally leads to a generally decreased rate of sterol biosynthesis as compared to clotrimazole, due to a direct inhibition of microsomal HMG-CoA-reductase. The additional fungicidal effects of bifonazole are considered to originate from a sequential action by inhibition of HMG-CoA-reductase and of cytochrome P450 [2]. bifonazole were affected by choice of medium with Kimmig's agar generally giving the lowest MIC's. Bifonazole MICs were shown to vary with pH (maximal activity at pH 6 . 5) with selected yeasts when tested on Kimmig's agar [3].
Ecabet sodium (TA-2711) is currently applied to some clinical gastrointestinal disease by inhibiting the ROS production and improving Helicobacter pylori eradication[1]. Ecabet sodium reduces apoptosis[2]
GAC0001E5 is a novel LXR inverse agonist, functioning as LXR a degrader"
Desethylamiodarone (N-Deethylamiodarone) is the major metabolite of antiarrhythmic compound Amiodarone (HY-14187). Desethylamiodarone has antiarrhythmic activity. Desethylamiodaron also induces cancer cell apoptosis[1][2].
Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia)[1]. Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway[2].
LY2452473 is an orally bioavailable, selective androgen receptor modulator (SARM).
Magnesium stearate is a commonly used pharmaceutical lubricant. But Magnesium stearate leads to an adverse effect on bonding between particles. Magnesium stearate can be used as an excipient, such as lubricant. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1][2].
1-Hydroxy-9-methoxycanthin-6-one is a natural product that can be isolated from the roots of Eurycoma longifolia[1].
[D-Pro2,D-Phe7,D-Trp9] Substance P is a Substance P (HY-P0201) analogue. [D-Pro2,D-Phe7,D-Trp9] Substance P is an inhibitor of Substance P. [D-Pro2,D-Phe7,D-Trp9] Substance P contracts guinea-pig ileum (GPI) indirectly[1][2].
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo[1].
F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress[1].
Cytisine is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisine is a partial agonist of α4β2 nAChRs[1], and partial to full agonist at β4 containing receptors and α7 receptors[2]. has been used medically to help with smoking cessation[3].
Acetyl podocarpic acid anhydride is a potent, semisynthetic liver X receptor(LXR) agonist derived from extracts of the mayapple. Acetyl podocarpic acid anhydride has the potential to be useful for the prevention and treatment of atherosclerosis, especially in the context of low HDL levels[1].
CSF1R-IN-14 is an isoindolinone derivative compound. CSF1R-IN-14 is a potent inhibitor of CSF1R. Colony stimulating factor 1 (CSF-1, also known as macrophage colony stimulating factor, M-CSF) is an important growth factor that controls bone marrow progenitor cells, monocytes, macrophages, and giants. CSF1R-IN-14 has the potential for the research of cancer diseases (extracted from patent WO2019134662A1, compound 1)[1].
Luxabendazole-d3 is the deuterium labeled Luxabendazole.
SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model[1].
Daidzein-4',7-diglucoside is a natural product that can be isolated from Radix puerariae[1].
Azido-PEG5-S-methyl ethanethioate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tirofiban-d9 is deuterium labeled Tirofiban.
Dotriacontane-d66 is the deuterium labeled Dotriacontane[1].
Migrastatin is a typical Fascin1 inhibitor. Migrastatin is isolated from a cultured broth of Streptomyces sp. MK929-43F1. Migrastatin inhibits tumor cell migration[1][2].
RWJ 63556 is an orally active COX-2 selective/5-lipoxygenase inhibitor, with anti-inflammatory activities.