Leupeptin Ac-LL is a protease inhibitor from actinomycetes. Leupeptin Ac-LL has antiplasmin activity[1].
L-Valyl-L-phenylalanine (Valylphenylalanine; H-VAL-PHE-OH) has been reported as biocompatible polymer.
Pde7-in-3 (example 2) is an inhibitor of the phosphodiesterase PDE7 with potential analgesic activity. PDE7-IN-3 can be used to study inflammatory, neuropathic, visceral and nociceptive pain[1].
Pimecrolimus hydrate (SDZ-ASM 981 hydrate) is a potent, nonsteroid and orally active calcineurin inhibitor. Pimecrolimus hydrate shows anti-inflammatory activity. Pimecrolimus hydrate has the potential for the research of atopic dermatitis and oral erosive lichen planus[1][2][3].
LY 178002 is a potent inhibitor of 5-lipoxygenase, phospholipase A2, with IC50 of 0.6 μM for 5-1ipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4[1].
JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTK inhibitor. JNJ-64264681 exhibits good pharmacokinetic characteristics and can be used for cancer and autoimmune diseases research[1].
Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity[1].
MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo[1].
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells[1][2].
Berteroin, a naturally occurring Sulforaphane analog, ia an antimetastatic agent. Berteroin has anti-inflammatory, antitumor and bactericidal effects[1][2].
Guaiacol-d4-1 is the deuterium labeled Guaiacol[1]. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[2].
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment [1]. Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex[2].
LDN 0088050 is selectivity adipocyte fatty acid binding protein (AFABP, FABP4) inhibitor with Ki values of 0.29 and 1.3 μM for FABP4 and FABP3, respectively. LDN 0088050 binds to FABP4 with a Kd of 2.05 μM[1].
α-Amyrin palmitate is isolated from Santalum album (sandalwood). α-Amyrin palmitate can be used for the study of arthritis in vivo[1].
Indinavir sulfate(MK-639 sulfate; L735524 sulfate ) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.Target: HIV ProteaseIndinavir(MK-639) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.MK-639 appears to have significant dose-related antiviral activity and is well tolerated [1]. Inhibition constants (K(i)) of the antiviral drug indinavir for the reaction catalyzed by the mutant enzymes were about threefold and 50-fold higher for PR(L24I) and PR(I50V), respectively, relative to PR and PR(G73S). The dimer dissociation constant (K(d)) was estimated to be approximately 20 nM for both PR(L24I) and PR(I50V), and below 5 nM for PR(G73S) and PR. Crystal structures of the mutants PR(L24I), PR(I50V) and PR(G73S) were determined in complexes with indinavir, or the p2/NC substrate analog at resolutions of 1.10-1.50 Angstrom [2].
Uridine 5'-diphosphate sodium salt is a potent, selective P2Y6 receptor native agonist (EC50=300 nM; pEC50=6.52) and a potent P2Y14 antagonist (pEC50=7.28). Uridine 5'-diphosphate sodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis[1][2].
Urease-IN-7 (Compound 5k) is a competitive Urease inhibitor (IC50: 3.33 μM, Ki: 3.62 μM). Urease-IN-7 can be used for research of peptic and gastric ulcers[1].
Sordarin is a potent diphthamide-dependent eEF2 inhibitor with antifungal properties. Sordarin targets eEF2 so as to inhibit protein translation by blocking eEF2-mediated translocation of tRNAs. Sordarin inhibits translation specifically in certain fungi (e.g. C. albicans, C. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae)[1][2].
Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties[1]. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research[2][3].
Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.
Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. IC50 value:Target: Histamine H1 receptorCetirizine crosses the blood-brain barrier only slightly, reducing the sedative side-effect common with older antihistamines. It has also been shown to inhibit eosinophil chemotaxis and LTB4 release. At a dosage of 20 mg, Boone et al. found that it inhibited the expression of VCAM-1 in patients with atopic dermatitis. The levorotary enantiomer of cetirizine, known as levocetirizine, is the more active form. From Wikipedia.
L-902688 is a potent, selective and orally active EP4 receptor agonist with a Ki of 0.38 nM and an EC50 of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors[1][2].
HPK1-IN-9 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-9 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 112) [1].
Pseudin-2, an AMP thast could be isolated from the skin of the South American paradoxical frog Pseudis paradoxa, exert a potent growth inhibitory effect against Gram-negative bacteria[1].
Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease[3].
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein[1][2].
(S)-4-Methoxydalbergione can be isolated from Dalbergia odorifera. (S)-4-Methoxydalbergione has anti-allergic and anti-inflammatory activity. (S)-4-Methoxydalbergione inhibits superoxide formation[1].
Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC50 of 36.5 nM for activation of the ERE tk-Luc.
Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].