RIPK2 inhibitor OD36 is a potent, specific, ATP-competitive inhibitor of RIPK2 with IC50 of 5.3 nM, inhibits Tyr and Ser/Thr-directed activities of RIPK2; inhibits both RIPK2 tyrosine autophosphorylation as well as downstream NF-κB and MAPK signaling induced by MDP, downregulates a panel of RIPK2 kinase-dependent genes; reduces cellular infiltration in an in vivo MDP-induced peritonitis model; also shows high affinity for cyclin G-associated kinase (GAK) with Ki of 3.8 nM.
Auraptene is the most abundant naturally occurring geranyloxycoumarin. Auraptene is primarily isolated from plants in the Rutaceae family, such as citrus fruits. Auraptene decreases the secretion of matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8, and chemokine (C-C motif) ligand-5(CCL5)[1].
Fmoc-Thr[GalNAc(Ac)3-α-D]-OH i a building block in the development of cancer vaccine.
15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM[1][2].
Tacrolimus is a macrocyclic lactone with potent immunosuppressive properties. Tacrolimus binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase.
Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s of 2.2 μM and 36 μM for human platelet COX-1 and IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.
Ocrelizumab is an anti-CD20 antibody that depletes circulating immature and mature B cells but spares CD20-negative plasma cells. The effector mechanisms of Ocrelizumab are complement-dependent cytotoxicity and antibody-dependent cellular cytotoxicity. Ocrelizumab is the first monoclonal antibody for secondary primary progressive multiple sclerosis (PPMS)[1].
Leupeptin is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin potently inhibits serine, cysteine and threonine proteases. Leupeptin inhibits Mpro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity[1][2][3].
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist. IC50 value:Target: Histamine H1 receptorBepotastine Beslilate (Bepreve) also suppresses some allergic inflammatory processes such as allergic rhinitis, chronic urticaria or pruritus associated with skin conditions (eczema/dermatitis, prurigo or pruritus cutaneus).Bepotastine Beslilate (Bepreve) is useful for allergic conjunctivitis.
2,6-Dimethoxy-1,4-benzoquinone, a natural phytochemical, is a known haustorial inducing factor. 2,6-Dimethoxy-1,4-benzoquinone exerts anti-cancer, anti-inflammatory, anti-adipogenic, antibacterial, and antimalaria effects[1].子
LEESGGGLVQPGGSMK, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α[1].
Luteolin-7-rutinoside has both anti-arthritic and antifungal activities, can result in a combination therapy for the treatment of fungal arthritis due to C. albicans infection.
Wogonoside, a flavonoid glycoside isolated from Huangqin, possesses anti-inflammatory effects. Wogonoside induces autophagy in breast cancer cells by regulating MAPK-mTOR pathway[1][2].
Blisibimod (A 623) is a potent and selective tetravalent inhibitor of B-cell activating factor (BAFF). Blisibimod can be used for the research of systemic lupus erythematosus (SLE)[1][2].
C-Reactive Protein (CRP) 174-185 is the 174-185 fragment of C-Reactive Protein. C-Reactive Protein (CRP), the prototypic marker of inflammation, is a cardiovascular risk marker and may promote atherogenesis[1].
Saikosaponin E is a saikosaponin isolated from Bupleurum yinchowense[1].
ROCK-IN-1 is a potent inhibitor of ROCK, with an IC50 of 1.2 nM for ROCK2.
Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
Glycerophosphoinositol choline is an essential nutrient that activates alpha7 nicotinic receptors and has analgesic and anti-inflammatory activity. Glycerophosphoinositol choline can affect diseases such as liver disease, atherosclerosis and neurological disorders[1][2].
Plasma kallikrein-IN-4 (Example 153) is a plasma kallikrein inhibitor with an IC50 of 0.016 μM against human plasma kallikrein[1].
Fisetin is a natural flavonol found in many fruits and vegetables with various benefits, such as antioxidant, anticancer, neuroprotection effects.
MCC950 is a potent and selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
TC-F2 is a reversible non-covalent binding inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 28 nM. FAAH is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders[1].
Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
Toralizumab (IDEC-131) is a humanized monoclonal antibody (mAb) against CD40L (CD154) comprised of human gamma 1 heavy chains and human kappa light chains. Toralizumab binds specifically to human CD40L on T cells, thereby preventing CD40 signaling. Toralizumab, a immunosuppressive drug, has the potential for active systemic lupus erythematosus (SLE) research[1][2].
Fenspiride Hcl is an α adrenergic and H1 histamine receptor antagonist.IC50 value:Target: Adrenergic receptor; H1 receptorFenspiride hydrochloride is a bronchodilator with anti-inflammatory properties. Fenspiride hydrochloride inhibits mucus secretion and reduces the release of tachykinins at a prejunctional level. Fenspiride hydrochloride also may be an antagonist at α adrenergic and H1 histamine receptors.
14-Deoxy-11,12-didehydroandrographolide is an analogue of Andrographolide that can be isolated from A. paniculata. 14-Deoxy-11,12-didehydroandrographolide inhibits NF-κB activation.
Terfenadine-d3 ((±)-Terfenadine-d3) is the deuterium labeled Terfenadine. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].
Briakinumab (ABT-874) is a fully human anti-IL-12/23p40 monoclonal antibody. Briakinumab targets and neutralizes IL-12 and IL-23. Briakinumab can be used for the research of rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis[1].
A novel Glucocorticoid receptor modulator.