Kobusin is a bisepoxylignan isolated from the Pnonobio biondii Pamp. Kobusin is an activator of CFTR and CaCCgie chloride channels and a inhibitor of ANO1/CaCC (calcium-activated chloride channel) channel[1][2].
Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
ASB 14780 (ASB14780, ASB-14780) is a potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM; displays excellen selectivity over other known secreted phospholipase A2s (sPLA2s), such as sPLA2-IA, sPLA2-IIA, sPLA2-III, and sPLA2-IB; markedly ameliorates liver injury and hepatic fibrosis, attenuates the CCl4-induced expression of α-SMA protein and the mRNA expression of collagen 1a2, α-SMA, and TGF-β1 in the liver, and inhibits the expression of monocyte/macrophage markers, CD11b and MCP-1 in vivo, while preventing the recruitment of monocytes/macrophages to the liver.
Momordicoside G (Momordicacoside G) is an orally active cucurbitane-type triterpene glycoside. Momordicoside G selectively induces apoptosis of M1-like macrophages, without affecting M2-like macrophages. Momordicoside G reduces intracellular ROS levels and promotes autophagy. Momordicoside G also has anticancer activity, inhibiting the growth of cancer cell lines. Momordicoside G stimulates M2-associated lung injury repair and prevents inflammatory lung cancer injury[1].
Bifarcept is a recombinant antibody of interferon receptor type I (IFN-RI). Bifarcept can bind IFN-β and prolong its serum half-life[1].
ZINC49534341 is a MRGPRX2 antagonist, with a Ki of 32 nM[1].
Thonzylamine is an orally active H1 histamine receptor antagonist, exhibits good antihistaminic and antianaphylactic properties. Thonzylamine can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases[1][2].
PTPN22-IN-1 is a potent PTPN22 inhibitor (IC50=1.4 µM; Ki=0.50 µM). PTPN22-IN-1 exhibits >7-10 fold selectivity for PTPN22 over similar phosphatases. PTPN22-IN-1 augments antitumor immune responses[1]. From WO2021007491A1 compound L-1.
Valziflocept (BAX1810; TAK-752) is a recombinant soluble human FcγRIIb receptor that targets Fc and FcγR. FcγRs bind and neutralize pathogenic IgG, thus forming a "decoy" or "scavenger" receptor that can reduce the severity of autoimmune diseases. Valziflocept can be used in studies of autoimmune diseases such as systemic lupus erythematosus (SLE)[1].
CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity[1].
Plonmarlimab (TJ003234) is an anti-GM-CSF monoclonal antibody. Plonmarlimab can be used for research of rheumatoid arthritis and COVID-19[1][2].
SR-31747 is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase[1][2].
TP-064 is a potent, selective, and cell-active inhibitor of PRMT4 with IC50 of <10 nM and Kd of 7.1 nM, shows high selectivity (>100-fold) for PRMT4 over other PRMTs; reduces dimethylation of BAF155 (IC50=340±30 nM) and MED12 (IC50=43±10 nM) in a dose-dependent manner in cell-baed assays; inhibits the proliferation of a subset of multiple myeloma cell lines (NCI-H929, RPMI8226, Cell IC50 of 379 and 886 nM, respectively) with affected cells arrested in G1 phase of the cell cycle, but has no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines.
Ro 31-9790 is a synthetic metalloproteinase (MMP) inhibitor.
Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis. Sulfasalazine is reported to suppress NF-κB activity.
Dihydrolipoic Acid (DHLA) is an excellent antioxidant capable of scavenging almost any oxygen-centered radical[1]. Dihydrolipoic acid exhibits anti-inflammatory properties in various diseases. Dihydrolipoic Acid exerts a preventive effect via ERK/Nrf2/HO-1/ROS/NLRP3 pathway in LPS-induced sickness behavior rats. Dihydrolipoic Acid can be used for the reaserch of depression[2].
6,6'-Di-O-sinapoylsucrose is a sucrose ester hat can be found in cynanchum amplexicaule[1].
5-desmethylsinensetin, isolated from Stevia satureiifolia var. satureiifolia, possesses antiprotozoal activity. 5-desmethylsinensetin shows IC50 values of 0.4 μg/mL on T. cruzi epimastigotes and 75.1 μg/mL on trypomastigotes, respectively[1].
Diayangambin (Syringaresinol dimethyl ether; Lirioresinol C dimethyl ether) is a cell proliferation inhibitor with an IC50 value of 1.5 μM against human monocytes. Diayangambin also has immunosuppressive and anti-inflammatory effects[1].
BTK-IN-5 is a covalent BTK inhibitor for treating medical conditions such as cardiovascular diseases, respiratory diseases, inflammation, and diabetes.
Fludroxycortide is a synthetic topical steroid and is used as an anti-inflammatory treatment for use on skin irritations.
Carbomycin B is a macrolide antibiotic[1].
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect[1].
Lacto-N-tetraose is the significant core structure of human milk oligosaccharides (HMOs) naturally existing in human milk. Lacto-N-tetraose is consist of galactose, N-acetylglucosamine, and glucose moieties. Lacto-N-tetraose has prebiotic effect, immune regulatory effect, anti-inflammatory effects, intestinal cell responses regulatory effect, antibacterial activity and antiviral activity. Lacto-N-tetraose has been widely added to infant formula[1].
Methyl syringate-d6 is the deuterium labeled Methyl syringate[1]. Methyl syringate, a chemical marker of asphodel monofloral honey, is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a TRPA1 agonist[2][3][4].
EGTA is a specific calcium ion chelator. EGTA has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca2+ over Mg2+ (Mg2+ Kd 1-10 mM). EGTA significantly inhibited the substrate adherence capacity of inflammatory macrophages[1][2].
Tafasitamab is an Fc-modified, humanized monoclonal antibody that binds to the human B-cell surface antigenCD19[1][2].
URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout[1].
Relfovetmab is an anti-NGF monoclonal antibody (mAb)[1].
Mavrilimumab (CAM 3001) is a monoclonal antibody that binds to the α subunit of the granulocyte-macrophage colony stimulating factor (GM-CSF) receptor and blocks intracellular signalling downstream of GM-CSF. GM-CSF might be a mediator of the hyperactive inflammatory response associated with respiratory failure and death[1].