(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.8)[1].
ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.
Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP).
Sirt2-IN-1 (Compound 9) is a sirtuin 2 (Sirt2) inhibitor with an IC50 of 163 nM[1].
Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l[1][2][3].
COX-2-IN-28 is a potent and selective COX-2 inhibitor with IC50 values of 0.054, 2.14, 13.21 µM for COX-2, 15-LOX, COX-1,respectively[1].
Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, with an EC50 of 190 nM in T84 cells. Plecanatide acetate shows anti-inflammatory activity in models of murine colitis[1].
A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.IC50 value: 147 nMTarget: Lck
L 601920-0 is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
CL264 is a TLR7-specific agonist for innate immune signals research[1].
Benzoylgomisin O isolated from Schisandra rubriflora, has inhibitory activity against 15-LOX, COX-1 and COX-2 enzymes and anti-inflammatory activity[1].
NPC-567 is a bradykinin B2 receptor antagonist. NPC-567 is effective in inhibiting the acute response to allergen in the airways[1][2].
Giripladib (PLA-695) is a indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). Giripladib can be used for osteoarthritis and breast cancer research[1][2].
Fasinumab (Anti-Human NGF) is a human IgG1k monoclonal antibody to nerve growth factor (NGF). Fasinumab can be used in acute sciatica and knee osteoarthritis (OA) studies[1].
6-Thioguanine is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
Ayanin is a bioflavonoid isolated from Croton schiedeanus Schlecht. Ayanin is a non-selective phosphodiesterase1-4 inhibitor and can be used for the study of respiratory disease,such as allergic asthma et al[1].
Kebuzone is a non-steroidal anti-inflammatory substance that may be studied in inflammatory diseases such as thrombophlebitis and rheumatoid arthritis[1].
N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
Tomentin is a compound isolated from Sphaeralcea angustifolia. Tomentin inhibits the formation of λ-carrageenan footpad edema at 58 %. Tomentin inhibits the phorbol ester-induced auricular edema formation by 57 %[1].
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition[1].
ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with an IC50 value of 3.2 nM.
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Antibacterial agent 129, an oxetanyl-quinoline derivative, has shown good antibacterial activity against P. mirabilis and B. subtilis with MICs of 31.25 μM and 31.5 μM and . Antibacterial agent 129 shows good antifungal activity against A. niger with a MIC of 31.25 μM. Antibacterial agent 129 shows excellent antimycobacterial activity with MIC 57.73 μM for M. tuberculosis H37Rv[1].
Stigmasterol is a plant sterol which has been focused on the cholesterol-lowering activity and is valued as an anti-stiffness factor in the therapy of rheumatic diseases.
EIPA is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].
Filipin III is the major component of Filipin, a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure[1].
STAMBP-IN-1 is a small-molecule inhibitor of STAMBP deubiquitinase, and interrupts STAMBP-Ub-NALP7 interaction. STAMBP-IN-1 decreases protein level of its inflammasome substrate NALP7 and suppresses IL-1b release after Toll-like receptor (TLR) agonism. STAMBP-IN-1 inhibits the activity of STAMBP to cleave recombinant di-Ub with an IC50 value of 0.33 mM[1].
Anti-inflammatory agent 30 (Compound 5) is an anti-inflammatory agent with hepatoprotective activity[1].
Taurodeoxycholate-d6 (sodium salt) is the deuterium labeled Taurodeoxycholate sodium salt[1]. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses[2]. [2][3].