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].
Fmoc-L-Val-OH-13C5,15N is a 15N-labeled and 13C-labled Pirimicarb. Pirimicarb is a fast-acting selective carbamate insecticide on a wide range of crops including cereals, sugar beet, potatoes, fruits and vegetables. Pirimicarb is an AChE inhibitor and an
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]
Podocarpusflavone B is a bisflavone that can be isolated from Padocarpus macraphylla[1].
LY243246 ((6S)-DDATHF), the 6S diastereomer of DDATHF, is a potent competitive inhibitor of 5’-phosphoribosylglycinamide formyltransferase (GAR transformylase). 6R- and 6S-diastereomers of DDATHF are remarkably similar and equiactive antimetabolites inhibitory to de novo purine synthesis[1].
GAC0001E5 is a novel LXR inverse agonist, functioning as LXR a degrader"
CP-135807 is an orally active and selective 5-HT1D agonist (IC50=3.1 nM), bovine). CP-135807 mediates central psychoactivity and can be used in antidepressant research[1][2].
TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM[1].
GSK 1562590 hydrochloride is a high affinity and selective antagonist of urotensin-II receptor (UT), with pKis of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native UT[1].
Antibacterial agent 116 is a benzophenone-containing salicylanilide compound. Antibacterial agent 116 has potent antibacterial activity by inhibiting the peptidoglycan formation. Antibacterial agent 116 is used as a photoaffinity probe to label Acinetobacter baumannii penicillin-binding protein (PBP1b), block the propagation pathway to disrupt the growth of peptidoglycan chain[1].
AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer[1].
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].
Bacitracin Zinc is a dephosphorylation of the C55-isoprenyl pyrophosphate interference for inhibition of cleavage of Tyr from Met-enkephalin with IC50 of 10 μM.Target: AntibacterialBacitracin is a mixture of related cyclic polypeptides produced by organisms of the licheniformis group of Bacillus subtilis var Tracy. Its unique name derives from the fact that the bacillus producing it was first isolated in 1943 from a knee scrape from a girl named Margaret Tracy. As a toxic and difficult-to-use antibiotic, bacitracin doesn't work well orally. However, it is very effective topically. Bacitracin is synthesised via the so-called nonribosomal peptide synthetases (NRPSs), which means that ribosomes are not involved in its synthesis [1, 2].
Agouti-Related Protein (25-51) (human) (AGRP (25-51) (human)) is an amino-terminal 25-51 fragment of agouti-related protein (AGRP)[1].
Pentosan Polysulfate is a semi-synthetic drug used to treat various medical conditions including thrombi and interstitial cystitis.
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).
HEPES-d18 is the deuterium labeled HEPES[1]. HEPES, a nonvolatile zwitterionic chemical buffering agent, is broadly applied in cell culture. HEPES is effective at pH 6.8 to 8.2. HEPES is also a potent inducer of lysosome biogenesis[2][3][4].
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].
SNX-5422 (PF-04929113), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
[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].
Amino-Tri-(m-PEG4-ethoxymethyl)-methane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[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].