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].
trans-Isoferulic acid-d3 is the deuterium labeled trans-Isoferulic acid[1]. trans-Isoferulic acid (trans-3-Hydroxy-4-methoxycinnamic acid) is an aromatic acid isolated from the roots of Clematis florida var. plena. trans-Isoferulic acid exhibits anti-inflammatory activity[2].trans-isoferulic acid suppresses NO and PGE2 production through the induction of Nrf2-dependent heme oxygenase-1 (HO-1)[3].
Toxicarol isoflavone is an isoflavone extracted from Millettia brandisiana.
Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly[1][2].
SARS-CoV-2-IN-66 (1), a vitaminK derivative, is a SARS-CoV-2 inhibitor, with an EC50 of 70.8 μM in VeroE6/TMPRSS2 cells[1].
AUTAC2 is a FKBP12-targeting autophagy-mediated degrader (AUTAC). AUTAC2 contains an FBnG (p-Fluorobenzyl Guanine) and an SLF (c ligand of FKBP) moiety. SLF binds non-covalently to FKBP12[1].
NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells[1].
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.
Chlorthenoxazine is a nonsteroidal anti-inflammatory drug.
Zaloglanstat (ISC-27864) is the inhibitor of the microsomal prostaglandin E synthase-1 (mPGES-1), and can be used to study asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases, etc[1].
MSA-2 is an orally available non-nucleotide STING agonist, with EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 shows antitumor activity and stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models[1].
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].
Rosenonolactone shows inhibitory activity against prolyl endopeptidase and thrombin and cholesterol ester transfer protein[1][2][3].
Plerixafor octahydrochloride is a selective CXCR4 antagonist with an IC50 of 44 nM.
Altromycin D is a Gram-positive antibiotic[1].
Ditryptophenaline ((-)-Ditryptophenaline) is the metabolites of Aspergillus flavus. Ditryptophenaline inhibits substance P receptor and has anti-inflammatory activity[1].
Bulbocapnine hydrochloride, an aporphine alkaloid, is a dopamine receptor inhibitor. Bulbocapnine hydrochloride inhibits dopamine synthesis. Bulbocapnine hydrochloride also has neuroleptic-like, anticonvulsant and antinociceptive effects[1][2][3].
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].
Kv3 modulator 4 is a Kv3.1 (pEC50=5.45) and Kv3.2 modulator extracted from patent WO2018020263A1, Cyclobutyl structure[1].
Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody targets the p19 subunit of interleukin 23. Mirikizumab can be used for the research of ulcerative colitis[1].
Monomethyl fumarate-d5 is deuterium labeled Monomethyl fumarate. Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease[1][2][3].
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.
3-pyridine toxoflavin is an impurity of toxoflavin.
GB-88 is a selective, orally PAR2 antagonist, inhibits PAR2 activates Ca(2+) release with an IC 50 of 2 µM[1].
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].
Tripelennamine, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine lessens the allergic response of the organism caused by histamine. Tripelennamine can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions[1][2][3].
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].