Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2).
SIKs-IN-1 (compound 8h), a pyrimidine-5-carboxamide derivative, is a Salt-inducible kinases (SIKs) inhibitor. SIKs regulates the transformation of M1/M2 macrophages, involving in inflammation process. SIKs-IN-1 inhibits SIK activity, up-regulates anti-inflammatory cytokine IL-10, but down-regulates pro-inflammatory cytokine IL-12. SIKs-IN-1 shows excellent anti-inflammatory effects in a DSS-induced colitis model[1].
Girinimbine (Girinimbin) is a carbazole alkaloid with a variety of biological effects. Girinimbine can induce apoptosis, and has antitrypanosomal, antiplatelet activity, antibacterial activity, anti-inflammatory, antioxidant and antitumor activities[1][2][3].
Hedycoronen A has inhibitory activity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium[1].
ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM.
Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively (patent WO2018064119A1, compound 405)[1].
Orismilast (LEO-32731) is a PDE4 inhibitor used for the research of inflammatory diseases[1].
Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake[1][2][3].
Cannflavin B is a prenylated flavone, which can be isolated from Cannabis sativa L. Cannflavin B has anti-inflammatory activity[1].
c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor with an IC50 value of 17 nM. c-Fms-IN-13 can be used as an anti-inflammatory agent[1].
13-cis Acitretin D3 （Isoacitretin D3） is a deuterium labeled 13-cis Acitretin. 13-cis Acitretin is the metabolite of Acitretin after chronic administration. Acitretin(Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis[1][2].
Harringtonolide is a potent RACK1 inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities[1].
Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a Ki of <20 nM.
Antituberculosis agent-7, an oxetanyl-quinoline derivative, has shown good antibacterial activity against P. mirabilis with a MIC of 31.25 μM. Antituberculosis agent-7 shows good antifungal activity against A. niger with a MIC of 62.5 μM. Antituberculosis agent-7 shows excellent antimycobacterial activity with MIC 3.41 μM for M. tuberculosis H37Rv[1].
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity[1].
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough[1].
Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV.
Ganoderic acid J is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid J possesses anti-inflammatory anti-inflammatory activity[1][2].
Imiloxan is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan has the potential for acute kidney injury research[1][2].
JAK-IN-30 (compound 31) is a water-soluble JAK inhibitor with IC50 values of 2, 15, 18 and 2 nM for JAK2, JAK1, JAK3 and TYK2, respectively. JAK-IN-30 has research potential for dry eye disease (DED)[1].
Ciwujianoside C3, an orally active and brain penetrated compound, is isolated the leaves of Acanthopanax henryi Harms. Ciwujianoside C3 has anti-inflammatory effect and can reinforces object recognition memory[1][2].
ODN 2088 is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6[1][2][3].
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain)[1]. Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation[2].
HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research[1].
FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease[1][2].
Lys-Pro-Pro-Thr-Pro-Pro-Pro-Glu-Pro-Glu-Thr is a undecapeptide, corresponding to the carboxy terminus of simian virus 40 large T antigen. Lys-Pro-Pro-Thr-Pro-Pro-Pro-Glu-Pro-Glu-Thr can be targeted by antibodies secreted from three mouse hybridomas, designated KT1, KT3, and KT4, produced antibodies that immunoprecipitated large T antigen[1][2].
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively[1].
Serum thymic factor (Thymulin) is a zinc-dependent immunomodulatory peptide. Serum thymic factor induces hyperalgesia. Serum thymic factor protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor has anti-diabetic, analgesic and anti-inflammatory effects[1][2][3].
Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission[1].
Risuteganib is an anti-integrin that downregulates oxidative stress and restores homeostasis, and targets three integrin receptors that are implicated in dry age-related macular degeneration (AMD) in order to restore homeostasis in the retina [1].