GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors[1].
SB225002 is a potent and selective CXCR2 antagonist with an IC50 of 22 nM.
Flufenamic acid-13C6 is the 13C6 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.
Rubiadin is a dihydroxy anthraquinone isolated from Rubia cordifolia. Rubiadin has a potent antixidant activity[1].
CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity[1][2].
Butamirate is an orally active antitussive agent that acts centrally via receptors in the brainstem. Butamirate also reduces airway resistance[1].
Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1)[1][1].
[D-Trp8]-γ-MSH is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis[1][2].
5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC50s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders[1].
Flazin is a non-enzymatic protein glycation inhibitor, also inhibits peroxynitrite (ONOO-), with an IC50 value of 85.31 μM for bovine serum albumin (BSA) glycation and an EC50 value of 71.99 μM for ONOO-. Flazin can be used for researching diabetes and neuronal disorders. Flazin also can used as a lipid droplet (LD) regulator against lipid disorders, and a xanthine oxidase (XOD) inhibitor[1][2][3].
RP101442, an active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 2.6 nM and 171 nM for S1PR1 and S1PR5, respectively[1].
CTP-NBD is a cell permeable specific NFκB peptide inhibitor. CTP-NBD could be used in colitis study[1][2]
DHODH-IN-15 (Compound 7b) is a hydroxyfurazan analog of A771726. DHODH-IN-15 is a dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 11 μM for rat liver DHODH. DHODH-IN-15 can be used for rheumatoid arthritis[1].
2′-Hydroxygenistein is a natural product that can be isolated from Crotalaria pallida and C. assamica. 2′-Hydroxygenistein shows anti-inflammatory activity. 2′-Hydroxygenistein shows significant concentration-dependent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils, with IC50 values of 5.9 ± 1.4 and 9.7 ± 3.5 μM, respectively[1].
(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].
Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP).
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].
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
CL264 is a TLR7-specific agonist for innate immune signals research[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].
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.
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].
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.
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].
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].