Keap1–Nrf2 IN-1 (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1–Nrf2 IN-1 (compound35) activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models[1].
GSK345931A is an EP1 receptor antagonist. GSK345931A shows measurable CNS penetration in the mouse and rat and potent analgesic efficacy in acute and sub-chronic models of inflammatory pain[1].
PG 116800 (PG 530742) is an orally avtive MMP inhibitor. PG 116800 has high affinity for MMP-2, -3, -8, -9, -13, and -14, while having substantially lower affinity for MMP-1 and -7. PG 116800 can be used for knee osteoarthritis research[1].
BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor.
Methylthiomcresol-C1-benzoic acid is a fenthion hapten that can be used for immunoreagent production (protein conjugates and polyclonal antibodies)[1].
DZ2002 is a potent and reversible S-Adenosyl-L-homocysteine Hydrolase(SAHH; AdoHcy Hydrolase) inhibitor with Ki of 17.9 nM.IC50 value: 17.9 nM(Ki) [1]Target: AdoHcy Hydrolase inhibitorin vitro: The cytotoxicity of DZ2002 is significantly less than DHCaA with an IC50 of 100 to 600 μM compared with 6 to 14 μM and shows very little cytotoxicity up to 100 μM. DZ2002 had little effects on lymphocyte proliferation (0.1 μM = 150,604 ± 13,862, 1 μM = 159,894 ± 11,152, and 10 μM = 136,157 ± 21,943 cpm) versus untreated Con A-stimulated cells (168,725 ± 8025 cpm). Similarly, little effect was seen in regards to IL-2 production from DZ2002-treated cells (0.1 μM = 1,838 ± 88, 1 μM = 1,793 ± 58, and 10 μM = 1,731 ± 36 pg/ml) versus untreated Con A-stimulated cells (1,806 ± 43 pg/ml). Although DZ2002 had little effect when T cells were stimulated with Con A, DZ2002 suppressed the MLR by 24.5, 42.3, and 46.0% at dosages of 0.1, 1, and 10 μM, respectively [1]. DZ2002 (500 μmol/L) significantly suppressed TLR agonists-stimulated up-regulation in IL-6, IL-12p40, TNF-α, and IgG and IgM secretion as well as in HLA-DR and CD40 expression of dendritic cells among human PBMCs in vitro. DZ2002 (100 μmol/L) also significantly suppressed TLR agonists-stimulated up-regulation in IL-6 and IL-23p19 production in murine BMDCs, and prevented Th17 differentiation and suppressed IL-17 secretion by the T cells in a BMDC-T cell co-culture system [3].in vivo: As compared with controls, consecutive 7-day i.p. injections of DZ2002 inhibited hemolysis by 24.5 and 18.4% at doses of 0.08 and 2 mg/kg, respectively, thus decreasing anti-SRBC antibody production in vivo [1]. Male C57BL/6 mice immunized with ovalbumin (OVA) were treated with DZ2002 (1, 5, and 25 mg/kg/day) after which lymphocyte proliferation, cytokine production, and IgG responses to OVA were monitored. Administration of DZ2002 dose dependently suppressed OVA-specific lymphocyte proliferation and anti-OVA IgG production compared with controls [2]. Treatment of the mice with DZ2002 significantly attenuated the progression of glomerulonephritis and improved the overall health. In ex vivo studies, treatment of the mice with DZ2002 suppressed the development of pathogenic Th17 cells, significantly decreased IL-17, TGF-β, IL-6, and IL-23p19 production and impeded activation of the STAT3 protein and JNK/NF-κB signaling in splenocytes [3].
Aeruginosin 865, isolated from terrestrial cyanobacterium Nostoc sp. Lukešová 30/93, is the first aeruginosin-type peptide containing both a fatty acid and a carbohydrate moiety. Aeruginosin 865 inhibits translocation of NF-kB to the nucleus. Aeruginosin 865 has anti-inflammatory effect[1]
TOK-8801 is a synthesized dihydroimidazothiazole carboxamide and is under development as an immunomodulator.
(R)-IL-17 modulator 4 is the R-configure of IL-17 modulator 4 (HY-141692). IL-17 modulator 4 is a prodrug of IL-17 modulator 1 (HY-141535). IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator[1].
Ketorolac D4 (RS37619 D4) is the deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2[1][2].
TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
Thunberginol C is a natural product that can be isolated from Hydrangea macrophyll. Thunberginol C attenuates stress-induced anxiety. Thunberginol C also has antimicrobial and antiallergic activity[1][2].
A potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.
Curculigoside is the main saponin in C. orchioide, exerts significant antioxidant, anti-osteoporosis, antidepressant and neuroprotection effects. Curculigoside possesses significant anti-arthritic effects in vivo and in vitro via regulation of the JAK/STAT/NF-κB signaling pathway[1].
AA 497 is a bronchodilator[1].
Porphyra 334 is an antioxidative and anti-photoaging agent. Porphyra 334 suppresses ROS production and the expression of MMPs following UVA irradiation[1][2].
TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose[1].
Voclosporin is a calcineurin (CN) inhibitor.
N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist.
Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a commonly used PKC activator.
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM[1]. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity[2].
PAT1inh-B01 is a selective SLC26A6 inhibitor. PAT1inh-B01 inhibits PAT1 (a Cl-/HCO3- exchanger)-mediated anion exchange (IC50: 350 nM). PAT1inh-B01 blocks fluid absorption in small intestine. PAT1inh-B01 can be used for research of small intestinal hyposecretory disorders[1].
Methylnissolin-3-O-glucoside (Methylnissolin-3-O-β-D-glucoside) is a flavonoid from the roots of Astragalus membranaceus with anti-inflammatory effects[1].
Enokizumab (MEDI-528) is a monoclonal antibody targeting to interleukin (IL)-9. IL-9 regulates the development of airway inflammation, mucus production, airway hyperresponsiveness, and airway fibrosis largely by increasing mast cell numbers and activity in the airways[1].
CP-24879 (hydrochloride) is a potent, selective and combined delta5D/delta6D inhibitor. CP-24879 (hydrochloride) can significantly reduce intracellular lipid accumulation and inflammatory injury in hepatocytes. CP-24879 (hydrochloride) exhibits superior antisteatotic and anti-inflammatory actions in fat-1 and ω-3-treated hepatocytes, and can be used for non-alcoholic steatohepatitis research[1][2].
Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78)[1].
Thymoctonan (THF-γ2) is the immunomodulatory octapeptide, thymic humoral factor γ2. Thymoctonan has the half-life less than 6 min at 37 °C in blood from human, rat and mouse[1].
Pefcalcitol is a new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures.
Viaminate is a derivative of Retinoic acid, which is used for the treatment of severe acne and other keratinization disorders.
Asapiprant is a potent and selective DP1 receptor antagonist with a Ki of 0.44 nM.