URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets.IC50 value: 4.6 nM [1]Target: FAAH in vitro: URB597 binds in the hydrophobic pocket and catalytic core of FAAH that connects the active site residues to the membrane surface of FAAH [1]. URB597 reduces the expression of the LPS-induced enzymes cyclo-oxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS; NOS2) in primary rat microglial cell, with a concomitant reduction in the release of the inflammatory mediators prostaglandin E2 (PGE2) and (NO) nitric oxide [2]. in vivo: URB597 inhibits [3H]anandamide hydrolysis in rat brain membranes with a parallel increase in brain anandamide, OEA, and PEA content by inhibition of FAAH. URB597 enhances the hypothermia effect induced by ethanolamide by inhibiting FAAH [3]. When delivered intraperitonealy (0.3 mg/kg) URB597 reduces allodynia and hyperalgesia through cannabinoid CB1 and CB2 receptor-mediated analgesia in rats with inflammatory pain [4].
A potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays; shows no inhibitory activity against the closely related nuclear hormone receptors RORα or RORβ; attenuates expression of genes such as IL26, IL23R and CCR6 in primary human Th17 cells, attenuate the knee swelling response in an antigen-induced arthritis rat models and inhibits IL-17A cytokine production in ex vivo recall assays.
IDO-IN-8 (NLG-1487) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, compound 1487, has an IC50 of 1-10 μM.
1-Deazaadenosine is a potent Adenosine deaminase (ADA) inhibitor with a Ki value of 0.66 μM. 1-Deazaadenosine exhibits anti-cancer activities in vitro and has the potential to be a chemotherapy agent for lymphoproliferative disorders[1][2].
Statil (Ponalrestat) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Statil selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Statil inhibits the conversion of glucose to sorbitol[1][2][3].
Suc-Ala-Ala-Pro-Phe-SBzl can be used as the substrate of rat intestinal mast cell protease (RMCP I), rat skeletal muscle mast cell protease (RMCP II) and Chymotrypsin (HY-108910). Suc-Ala-Ala-Pro-Phe-SBzl can be hydrolyzed by glycine (R208G)[1][2].
HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level[1].
VTP-27999 is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.Ic50 value:Target: Renin
2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM[1][2][3].
Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.
hCAIX-IN-5 (compound 6b) is a potent and selective hCAIX inhibitor with KIs of >10000, >10000, 130.7, 829.1 nM for hCAI, hCAII, hCAIV, hCAIX, respectively[1].
Z-Leu-Leu-Tyr-COCHO is a potent chymotrypsin-like activity inhibitor with a Ki value of 3.0 nM[1].
Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively (patent WO2018064119A1, compound 405)[1].
Orismilast (LEO-32731) is a PDE4 inhibitor used for the research of inflammatory diseases[1].
Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.Target: CYP26in vitro: Talarozole R enantiomer treatment increased the mRNA expression of CRABP2, KRT4, CYP26A1 and CYP26B1 dose dependently, and decreased theexpression of KRT2 and IL-1alpha compared with vehicle-treated skin. No mRNA change in retinol-metabolizing enzymes was obtained. There was no induction of epidermal thickness or overt skin inflammation in talarozole-treated skin. Immunofluorescence analysis confirmed an upregulation of KRT4 protein, but no upregulation of CYP26A1 and CYP26B1 expression was detected [1] [2].in vivo: Talarozole R enantiomer slightly diffused into the skin only when dissolved in propylene glycol, isopropyl myristate or ethanol. Although only 0.1% of the dose applied was found in the skin itself after 12-24 h, this was sufficient to achieve local concentrations well above the half-maximal inhibitory concentration value for talarozole. The distribution of talarozole within the skin was investigated: 80% was located in the epidermis, while the remaining 20% was found in the dermis [3].
Z-Ala-Arg-Arg-AMC (Fluorogenic Proteasome Substrate) is a fluorogenic substrate for assaying trypsin-like activity of proteasome[1].
Palmitic acid-1-13C is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a Ki of <20 nM.
MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the expression of iNOS and p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity. MSU-42011 can be used for cancer research[1].
Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
Quizalofop-P is absorbed through weed stems and leaves, conducts upward and downward in plants, accumulates at the top and intermediate meristems, inhibits cellular fatty acid synthesis, and makes weeds necrotic. Quizalofop-P is highly selective between grass weeds and dicotyledonous crops[1].
4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a Ki of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC50= 1.71μM)[1][2].
Tetramisole hydrochloride is an inhibitor of alkaline phosphatases, is a high purity antiparasitic.
Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity[1].
FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease[1][2].
IDX184 is a potent and orally bioavailable inhibitor of HCV replication. IDX184 potently inhibits HCV polymerase (IC50=0.31 μM, Ki=52.3 nM)[1][2].
2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV Protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitory activity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells[1][2].
Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission[1].
IDO-IN-6 (NLG-1486) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, Compound 1486, has an IC50 of <1 μM.
MeOSuc-Ala-Ala-Pro-Met-AMC is a peptide substrate of elastases and chymotrypsin-like serine peptidases[1].