Demeclocycline is an orally active tetracycline antibiotic. Demeclocycline impairs protein synthesis by binding to the 30S ribosomal subunit to inhibit binding of aminoacyl tRNA. Demeclocycline shows anti-bacterial activitise to a wide variety of bacterial infections[1][2].
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM[2]. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay[1]. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway[4]. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease[5].
IKK2-IN-4 (compound 4) is a potent IKK-2 inhibitor, with an IC50 of 25 nM. IKK2-IN-4 can inhibit the LPS-induced production of TNFα in PBMCs[1].
Methylenedihydrotanshinquinone is a natural product that can be isolated from the dried root of S. miltiorrhiza. Methylenedihydrotanshinquinone has anti-inflammatory effect by inhibiting expression of TNF-α, IL-1β, and IL-8[1].
CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 blocks the binding of TCDD to AhR with an IC50 of 0.03 µM.
Atinvicitinib is a kind of pyrazole compound. Atinvicitinib has the potential for the research of atopic dermatitis (extracted from patent WO2021123094A1)[1].
Thromboxane A2 (TXA2) is a prostanoid mediator produced by the metabolism of Arachidonic acid (HY-109590) through the cyclooxygenase pathway. Thromboxane A2 activates the thromboxane-prostanoid (TP) receptors. Thromboxane A2 is a potent vasoconstrictor eicosanoid. Thromboxane A2 (TXA2) leads to potent vasoconstriction by stimulation of smooth muscle cells. Thromboxane A2 acts as s tonic immunoregulator to regulate adaptive immune responses[1][2].
Beinaglutide is a recombinant human GLP-1 (rhGLP-1) that shares almost 100% homology with human GLP-1 (7–36). Beinaglutide displays does-dependent effects in glycemic control, inhibiting food intake and gastric empty and promoting weight loss. Beinaglutide has the potential for the research of overweight/obesity and nonalcoholic steatohepatitis (NASH)[1][2].
UTL-5g (GBL-5g), an anti-inflammatory TNF-α inhibitor, has chemoprotective and liver radioprotective effects. UTL-5g lowers hepatotoxicity, nephrotoxicity, and myelotoxicity induced by Cisplatin through TNF-α inhibition among other factors[1][2].
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity[1].
Cajucarinolide is anti-Inflammatory diterpene that can be isolated from Croton cajucara[1].
Hesperidin methylchalcone (Hesperidin methyl chalcone) inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone inhibits inflammation and pain. Hesperidin methylchalcone exhibits vasoprotective activity[1].
trans-3,5-Dimethoxystilbene (cis-Pinosylvin dimethyl ether) is a natural product that has been isolated from the benzene extract of the bark of jack pine (Pinus bunksiuna)[1].
The compound 7,4'-Di-O-methylapigenin may be partly responsible for the reported antifungal activity of C. zeyheri, and may serve as a potential source of lead compounds that can be developed as antifungal phytomedicines.And it also showed inhibition of the drug efflux pumps (with IC50 = 51.64 μg/ml).IC50:51.64 μg/ml(Candida albicans drug efflux pumps)[2]In vitro: The isolated 7,4'-Di-O-methylapigenin was further investigated for its inhibitory activity on ABC drug efflux pumps in C. albicans by monitoring an increase in ciprofloxacin, assessing the level of its accumulation, in response to reserpine. There was a higher accumulation of ciprofloxacin in Candida cells in the presence of 7,4'-Di-O-methylapigenin than with reserpine. The compound 7,4'-Di-O-methylapigenine demonstrated the activity in a dose-dependent manner with IC50 value of 51.64 μg/ml. These results support those obtained from synergism assays where by the underlying synergistic antifungal mechanisms could be due to blockage of ABC efflux pumps and increasing the susceptibility of Candida to miconazole.[2]In vivo: In searching for natural products as potential anti-inflammatory agents, 7,4'-Di-O-methylapigenin wasn't evaluated in vivo for its ability to inhibit acute inflammation.[1]
Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
Parimifasor is an immunomodulator, with anti-inflammatory activity.
trans-urocanic acid (trans-UCA), a natural epidermal constituent, inhibits human natural killer cell (NK) activity in vitro. trans-urocanic acid is active in regulating an immune function[1].
IDR-1 is an antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria. IDR-1 counters infection by selective modulation of innate immunity without obvious toxicities. IDR-1 has anti-inflammatory and anti-infective properties, enhances the levels of monocyte chemokines, and attenuates pro-inflammatory cytokine release[1][2].
Manitimus is an inhibitor of dehydroorotate dehydrogenase, and a potent immunosuppressive drug.
CCG-2046 is a RGS4 inhibitor with an IC50 of 4.3 μM against RGS4-Gαo interaction signal[1].
A small molecule inhibitor of the NF-κB family member c-Rel with IC50 of 3 uM in EMSA assays; inhibits human diffuse large B-cell lymphoma (DLBCL) cell line with IC50 of 18 uM, binds c-Rel directly and changes the conformation of the protein, inhibiting DNA binding and transcriptional activity.
Urease-IN-8 (Compound 5e) is a competitive Urease inhibitor (IC50: 3.51 μM, Ki: 3.11 μM). Urease-IN-8 can be used for research of peptic and gastric ulcers[1].
GSK-843 is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM[1].
ENMD-1068 hydrobromide is a potent PAR2 antagonist. ENMD-1068 hydrobromide attenuates joint inflammation in a dose-dependent manner. ENMD-1068 hydrobromide can be used in research of joint inflammation[1].
Diammonium Glycyrrhizinate, isolated from the licorice root, is a widely used anti-inflammatory agent[1].
GPR84 antagonist 8 is a selective GPR84 antagonist.
Balstilimab (AGEN2034) is a fully human monoclonal IgG4 antibody against PD-1[1].
XMP-629 (XOMA-629), a cationic α-helical peptide, is a potent endotoxin inhibitor. XMP-629 exhibits broad-spectrum antimicrobial activity via an immunomodulatory mechanism. XOMA 629 has antimicrobial activity against Propionibacterium acnes, Staphylococcus aureus and Streptococcus pyogenesand[1][2].
Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity[1].
(Z)-Lafutidine ((Z)-FRG-8813) is a potent histamine H2 receptor antagonist. (Z)-Lafutidine shows anti-secretory and gastroprotective activities[1].