CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs)[1].
Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research[1][2].
Toxicarol isoflavone is an isoflavone extracted from Millettia brandisiana.
SMN-C2 is a close analogs of RG-7916 act as selective RNA-binding ligands that modulate pre-mRNA splicing; directly binds to the AGGAAG motif on exon 7 of the SMN2 pre-mRNA, and promotes a conformational change in two to three unpaired nucleotides at the junction of intron 6 and exon 7 in both in vitro and in-cell models; increases binding of the splicing modulators, far upstream element binding protein 1 (FUBP1) and its homolog, KH-type splicing regulatory protein (KHSRP), to the SMN-C2/C3-SMN2 pre-mRNA complex and enhances SMN2 splicing.
BT424 is a specific HCK inhibitor. BT424 can regulate macrophage activation and autophagy in vitro. BT424 ameliorates inflammation and kidney fibrosis in UUO model[1].
HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 104 times more active than histamine in H2-mediated effects in natural suppressor cells[1].
ODN 1826, a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. CpG ODN 1826 is an excellent immunostimulator that induces NO and iNOS production in the murine model. CpG ODN 1826 enhances cell apoptosis. ODN 1826 sequence: 5’-tccatgacgttcctgacgtt-3’[1][2][3].
Ginsenoside Rb3 is extracted from steamed Panax notoginseng. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
Comanthoside B is a flavonoid glycoside isolated from the aerial portions of Ruellia tuberosa L. Comanthoside B has anti-inflammatory and antiseptic activities[1].
Corynoline, isolated from Corydalis incise (Papaveraceae), is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM[1]. Corynoline exhibits anti-inflammatory activity by activating Nrf2[2].
Frunevetmab (NV-02) is a felinized anti-nerve growth factor (NGF) monoclonal antibody with a Kd of 20 pM. Frunevetmab can effectively decrease osteoarthritis (OA) pain in cats[1][2].
Chloranthalactone E (compound 6), a labdane diterpene, can be isolated from the aerial parts of Chloranthus serratus. Chloranthalactone E inhibits NO production in LPS-activated RAW 264.7 macrophages[1].
J-113863 is a potentand selective CCR1 antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 has no active against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect[1][2][3].
Phostriecin is an antitumor antibiotic produced by Streptomyces pulveraceus. Phostriecin is a strong inhibitor of type 2A (PP2A) and a weak inhibitor of type 1 (PP1) serine/threonine protein phosphatases with IC50s of 3.2 nM and 131 μM, respectively. Phostriecin has the potential for the research of cancer[1].
N4-Acetylcytidine triphosphate is a endogenous nucleoside metabolite from the degradation of tRNA, primes and activates NLRP3 inflammation by inducing HMGB1 expression[1].
TLR7 agonist 7 (compound IIb-26) is an TLR7 agonist with an EC50 value of ~4 nM[1].
BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research[1].
Quercetin 3-O-neohesperidoside, a flavonoid glycoside, has anti-inflammatory activity[1].
Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.
ODN 6016 is a CpG-A oligonucleotides. ODN 6016 can induce IFN-α production, can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G[1][2].
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.
HA Peptide (HA tag) is a nine amino acids peptide derived from the human influenza hemagglutinin (HA). It is extensively used to isolate, purify, detect, and track the protein of interest in cell biology and biochemistry.
CCP peptide is a synthetic cyclic citrullinated peptide (CCP) and used as the substrate for detecting anti-CCP antibodies serologically. CCP peptide functions as a target for autoantibodies with a very high specificity for rheumatoid arthritis (RA)[1][2].
Zedoalactone B is an anti-Babesial agent with an IC50 of 1.6 μg/mL against Babesia gibsoni. Zedoalactone B inhibits NO production with an IC50 of 23.8 μM[1][2].
Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor[1].
RXFP1 receptor agonist-2 (Example 124) is a RXFP1 receptor agonist. RXFP1 receptor agonist-2 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1 nM[1].
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative isolated from plants of the Genus Daphne, is a protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively[1][2]. Daphnetin (7,8-dihydroxycoumarin) is a secondary metabolite of plants used in folk medicine to counter inflammatory and allergic diseases, also has been clinically used in the treatment of coagulation disorders, rheumatoid arthritis with anti-malarian and anti-pyretic properties[3].
Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic, and also a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide employs in traditional Chinese medicine for many ailments, mainly to improve the microcirculation in states of shock, and also in organophosphate poisoning[1].
Timolol is a β-blocker available for both topical and systemic administration. Topical Timolol is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension. Timolol can also be used for the research of infantile hemangiomas, hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation.Timolol also has cardioprotective effect[1][2].
Copper tripeptide (GHK-Cu), a naturally occurring tripeptide, is first isolated from human plasma, but can be found in saliva and urine. During wound healing, Copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a Natural Modulator of Multiple Cellular Pathways in Skin Regeneration[1].