RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α[1].
Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice[1].
Propionyl-DL-carnitine chloride is a carnitine derivative. Propionyl-DL-carnitine chloride can be used for the research of inflammation[1][2][3][4].
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.
Spinoxin isolated from the venom of scorpion Heterometrus spinifer, is a 34-residue peptide neurotoxin cross-linked by four disulfide bridges. Spinoxin is a potent inhibitor of Kv1.3 potassium channel (IC50 = 63 nM), considering to be valid molecular targets in the diagnostics and therapy of various autoimmune disorders and cancers[1].
Difloxacin is an antimicrobial agent[1].
Curcumin D6 (Diferuloylmethane D6) is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
Saikosaponin A is an active component of Bupleurum falcatum, up-regulates LXRα expression, with potent anti-inflammatory activity[1].
Zafirlukast-d7 (ICI 204219-d7) is the deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects[1][2].
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
Tomatidine acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling.
Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research[1][2][3].
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].
Germination-IN-1 (compound 11) is a potent germination inhibitor with an IC50 of 4 µM. Germination-IN-2 shows anti-germination activity with 14% germination rate[1].
DHODH-IN-4 (compound 17) is a human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitor, with IC50 values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity[1].
Cl-amidine (hydrochloride) is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.
Cergutuzumab amunaleukin (CEA-IL2v) is a monomeric carcinoembryonic antigen (CEA)-targeted IL-2 variant-based immunocytokine. Cergutuzumab amunaleukin has immunostimulating and antineoplastic activities[1].
Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.IC50 Value: 7 nM [1]Target: Lckin vitro: Lck Inhibitor (compound 25) exhibited good potency in the T-cell receptor-induced IL-2 secretion assay (IL- 2) and also inhibited subsequent T-cell proliferation (T-cell prolif.) in the same human T -cells.in vivo: A once daily dose of 25was administered orally at 10, 30, and 60 mg/kg from day 9 today 17. Paw volume was measured daily from day 9 through day 18. The compound showed a dose-dependent inhibition of arthritis, with an ED50 estimated at 24 mg/kg (Figure 6). Based on the measured plasma levels from the three dose groups, the exposure of 25 at the ED50 was estimated to be 2.7 μM·h (Cmax≈ 0.7 μM) [1].Clinical trial: N/A
RS4317 is a topically effective 5-lipoxygenase (5-LO) inhibitor.
Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B[1]. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM)[2].
Fenoprofen Calcium is a nonsteroidal, anti-inflammatory antiarthritic agent.Target: Prostaglandin G/H synthase 1Fenoprofen is a non-steroidal anti-inflammatory, antipyretic, analgesic agent advocated for use in rheumatoid arthritis, degenerative joint disease, ankylosing spondylitis and gout. Fenoprofen has a serum half-life of about 150 to 180 minutes and is at least 99% bound to plasma proteins. It is extensively metabolised after oral administration, the main metabolites being fenoprofen glucuronide and 4-hydroxy-fenoprofen glucuronide [1]. Fenoprofen calcium is revealed for relief of mild to moderate pain in adults and for relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis. In patients with osteoarthritis, the anti-inflammatory and analgesic effects of fenoprofen calcium have been demonstrated by decrease in tenderness as a response to pressure and reduction in night pain, stiffness, swelling, and overall disease activity. These effects have also been demonstrated by attenuation of pain with motion and at rest and increased range of motion in involved joints [2].
MF-766 (MF766) is a highly potent and selective EP(4) antagonist with binding Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay; exhibits blockade of inhibition of TNFa-induced IP10 release by the specific EP4 agonist L-000902688 (IC50=9.5 nM); demonstrates potency and efficacy of in the rat AIA model measuring inhibition of paw swelling.
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].
Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research[1][2].
PDE IV-IN-1 is an inhibitor of phosphodiesterase IV, used for the research of asthma, COPD or other inflammatory diseases.
Vobarilizumab (ALX-0061) is an anti-IL-6R monoclonal antibody (mAb) (Kd: 0.19 pM). Vobarilizumab consists of an anti-IL-6R domain and an anti-human serum albumin domain. Vobarilizumab can be used in the research of inflammatory autoimmune diseases, such as rheumatoid arthritis[1][2][3].
TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide[1].
Rabeprazole Sulfide is an active metabolite of Rabeprazole. Rabeprazole is a proton pump inhibitor that suppresses gastric acid secretion through an interaction with (H+/K+)-ATPase in gastric parietal cells. Rabeprazole markedly inhibits the motility of H. pylori. Rabeprazole has the potential for various peptic diseases treatment[1][2].
Geissoschizoline ((+)-Geissoschizoline) is a potent inhibitor of human AChE/BChE, with IC50s of 20.40 µM and 10.21 µM, respectively. Geissoschizoline emerges as a possible multi-target prototype that can be very useful in studies of preventing neurodegeneration and restoring neurotransmission. Geissoschizoline aiso is a potent anti-inflammatory agent[1].
Empasiprubart (ARGX-117) a humanized inhibitory monoclonal antibody against complement C2. Empasiprubart prevents the formation of the C3 proconvertase and inhibits classical and lectin pathway activation upstream of C3 activation through binding to the Sushi-2 domain of C2. Empasiprubart exhibits pH- and calcium-dependent target binding. Empasiprubart prevents complement-mediated cytotoxicity in in vitro models for autoimmune hemolytic anemia and antibody-mediated rejection of organ transplants[1].