ChemR23-IN-2 is a potent and orally efficacious ChemR23 inhibitor with an IC50 value of 3.2 nM.
Carbocisteine, a mucolytic agent, can be used for the research of chronic obstructive pulmonary disease (COPD)[1].
Eflepedocokin alfa is a recombinant fusion protein with potential cell protective activity. Eflepedocokin alfa consists of human IL-22 fused to human IgG2-Fc domain. Eflepedocokin alfa leads to the activation of IL-22/IL-22R-mediated signal transduction pathways as well as STAT3. Eflepedocokin alfa plays a role in immune response and bacterial infection, enhancing intestinal barrier function, intestinal immunity, and tissue repair[1].
Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin[1].
Ac2-12, an annexin/lipocortin 1 (LC1)-mimetic peptide, inhibit neutrophil extravasation. Ac2-12 has antimigratory action and inhibits recruitment of neutrophils in experimental inflammation models[1][2].
Mecysteine hydrochloride is an antitussive, and an expectorant agent, used to relieve breathing difficulties caused by mucus.
(S)-Thalidomide ((S)-(-)-Thalidomide) is the S-enantiomer of Thalidomide. (S)-Thalidomide has immunomodulatory, anti-inflammatory, antiangiogenic and pro-apoptotic effects[1][2][3]. (S)-Thalidomide induces teratogenic effects by binding to cereblon (CRBN) [4].
BVT 2733 is a new, small molecule, non-steroidal, isoform-selective inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1).IC50 value:Target: 11β-HSD1 inhibitorin vitro: in vivo: BVT 2733 lowered hepatic PEPCK and glucose-6-phosphatase mRNA, blood glucose and serum insulin concentrations compared with vehicle treated mice [1]. CIA mice were treated with BVT-2733 (100 mg/kg, orally) or vehicle twice daily for 2 weeks. BVT-2733 treatment attenuated the arthritis severity and anti-CII level in CIA mice. BVT-2733 also decreased the levels of serum TNF-α, IL-1β, IL-6 and IL-17. BVT-2733 treatment also significantly reduced synovial inflammation and joint destruction [2]. Mice receiving BVT 2733 treatment exhibited decreased body weight and enhanced glucose tolerance and insulin sensitivity compared to control mice. BVT 2733 also down-regulated the expression of inflammation-related genes including monocyte chemoattractant protein 1 (MCP-1), tumor necrosis factor alpha (TNF-α) and the number of infiltrated macrophages within the adipose tissue in vivo [3].
SDZ 224-015 is an orally active inhibitor of the interleukin-1 beta (IL-1β) converting enzyme and caspase-1. SDZ 224-015 possesses anti-COVID-19 activity, targeting Mpro (IC50 of 30 nM)[1][2].
Rebamipide D4 (OPC12759 D4) is deuterium labeled Rebamipide. Rebamipide is a mucoprotective agent. Rebamipide induces COX-2 expression, increases PGE2 levels, and enhances gastric mucosal defense in a COX-2-dependent manner[1].
AUDA (compound 43) is a potent soluble epoxide hydrolase (sEH) inhibitor with IC50s of 18 and 69 nM for the mouse and human sEH, respectively[1]. AUDA has anti-inflammatory activity[2].
Stephanine ((-)-Stephanine) is an isoquinoline aporphine-type alkaloid. Stephanine induce apoptosis through the reverse of mitotic exit. Stephanine exhibits Antiplasmodial activity. Stephanine can be used for the research of stomach pain, abdominal pain, arthritis and cancer[1][2].
3β-Acetoxy-hop-22(29)-ene (compound 1) is a potent anti-inflammatory agent. 3β-Acetoxy-hop-22(29)-ene shows high inhibitory activity of yeast α-glucosidase, with an IC50 of 5.74 μM. 3β-Acetoxy-hop-22(29)-ene inhibits MPO (myeloperoxidase) activity in a dose-dependent manner in mouse ear edema model induced by 12-O-tetradecanoylphorbol acetate (TPA), with an IC50 of 0.23 μmol/ear[1].
Tyk2-IN-3 is a Tyk2 pseudokinase inhibitor, with an IC50 of 485 nM.
Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research[1][2][3].
2-[(4-Oxo-1,2,3-benzotriazin-3-yl)oxy]acetic acid (HBA) is a hapten with a carboxyl group at the end of its spacer arm, suitable for reacting with free amine groups of proteins. 2-[(4-Oxo-1,2,3-benzotriazin-3-yl)oxy]acetic acid can be combined with carrier proteins and used in antigen design[1].
Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication[1]. Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation [2].
Dichotomine B, a β-Carboline alkaloid, attenuates neuroinflammatory responses in LPS/ATP-induced BV2 microglia[1].
K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.IC50 value:Target: GATA-specific inhibitorin vitro: K-7174 inhibited the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either tumor necrosis factor alpha or interleukin-1beta, without affecting the induction of intercellular adhesion molecule-1 or E-selectin. K-7174 had no effect on the stability of VCAM-1 mRNA.K-7174 did not influence the binding to any of the following binding motifs: octamer binding protein, AP-1, SP-1, ets, NFkappaB, or interferon regulatory factor [1]. Addition of 10 microM K-7174 rescued these inhibitions of Epo protein production and promoter activity induced by IL-1beta, TNF-alpha, or L-NMMA, respectively [2]. K-7174 had the potential to induce endoplasmic reticulum (ER) stress evidenced by induction of GRP78 and CHOP.Other inducers of ER stress completely reproduced the effects of K-7174 including suppression of lipid accumulation, blockade of induction of adiponection and PPARgamma and maintenance of MCP-1 expression [3].in vivo: K-7174, one of proteasome inhibitory homopiperazine derivatives, exhibits a therapeutic effect, which is stronger when administered orally than intravenously, without obvious side effects in a murine myeloma model. Moreover, K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib [4].
Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19[1][2][3].
Irisflorentin, a naturally occurring isoflavone, is an abundant active constituent in Rhizoma Belamcandae. Irisflorentin markedly reduces the transcriptional and translational levels of inducible nitric oxide synthase (iNOS) as well as the production of NO. Anti-inflammatory activity[1].
Anti-osteoporosis agent-3 (Compound 11), a PMSA derivative, is an anti-osteoporosis agent. Anti-osteoporosis agent-3 inhibits osteoclastogenesis with an IC50 value of 322.9 nM in vitro. Anti-osteoporosis agent-3 also blocks the formation of F-action belts and bone resorption[1].
Ruplizumab (BG 9588) is a humanized monoclonal anti-CD40L (TNF Receptor) IgG1κ antibody. Ruplizumab has the potential for systemic lupus erythematosus disease research[1].
Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively IC50 Value: 13 nM(Lck) [1]Target: Src family kinaseLck inhibitor 2(Compound 9) inhibited 48 kinases with %control < 1 (33 of them tyrosine kinases, almost half of the 71 tyrosine kinases in the panel). A further 27 kinases were bound with %control < 10. Kd values for 16 kinases were determined and found to be below 100 nM. These included TXK (10 nM)[2].
Esculentic acid is a selective COX-2 inhibitor and has anti-inflammatory effect. Esculentic acid is a pentacyclic triterpenoid that can be extracted from the Chinese herb Phytolacca esculenta[1][2].
Navarixin is a potent, allosteric antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.
BMS-1166 hydrochloride is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
Sodium lauroyl glutamate is an anionic amino acid surfactant. Sodium lauroyl glutamate has the irritant contact dermatitis potential, and possible anti-irritating potential in a surfactant mixture on human skin[1].
BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.
NTU281 is a potent transglutaminase-2 inhibitor. NTU281 can reduce the increases in serum creatinine and albuminuria in diabetic rats. NTU281 can also reduce glomerular collagen I accumulation, Hic-5 and α-SMA expression, and apoptosis. NTU281 can be used for researching glomerulosclerosis caused by diabetes[1][2].