Inflammation/Immunology

Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.

ZXH-3-26 is a CRBN-recruiting BRD4 PROTAC degrader with a DC_50/5h of approximately 5 nM. ZXH-3-26 drives the ubiquitination and degradation of BRD4 by recruiting BRD4_BD1 to the CRL4^CRBN E3 ubiquitin ligase complex, thereby inhibiting the dynamic distribution of super-enhancers. ZXH-3-26 reverses TNF-α-induced impairment of the immunosuppressive function of mesenchymal stem cells, and affects RNA synthesis and the transcriptional elongation process of Pol II. ZXH-3-26 can be used in studies related to inflammatory arthritis, malignant tumors, and HIV latency.

Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC₅₀ of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC₅₀ of 6.81 μM.

Acitretin (Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. Acitretin also can be used for the research of Alzheimer’s disease.

Mepolizumab (SB 240563) is a humanized monoclonal antibody that binds to and neutralizes interleukin-5 (IL-5), the major cytokine involved in eosinophil proliferation, activation, and survival. Mepolizumab can be used for the research of eosinophilic granulomatosis with polyangiitis (EGPA) and severe eosinophilic asthma.

Kaempferide is an orally active flavonol isolated from Hippophae rhamnoides L. Kaempferide has anticancer, anti-inflammatory, antioxidant, antidiabetic, antiobesity, antihypertensive, and neuroprotective activities. Kaempferide induces apoptosis. Kaempferide promotes osteogenesis through antioxidants and can be used in osteoporosis research.

Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC₅₀s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.

Methazolamide (L584601) is a BBB-penetrable and orally active carbonic anhydrase inhibitor, with a K_i of 14 nM for human carbonic anhydrase II. Methazolamide can reduce intraocular pressure and has a neuroprotective effect, being able to inhibit neuronal apoptosis. Methazolamide can be used in the research of ophthalmic diseases such as glaucoma and cerebrovascular diseases such as subarachnoid hemorrhage.

Zabedosertib (BAY 1834845) is a selective, orally active IRAK4 inhibitor with immunomodulatory potential, IC₅₀ is 3.55 nM. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors. Zabedosertib exhibits anti-inflammatory property against IL-β, LPS (HY-D1056) and Imiquimod (HY-B1080) induced inflammation.

A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC₅₀ of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.

Anti-Mouse osteopontin/SPP1 Antibody (103D6) is a mouse-derived anti-mouse osteopontin/SPP1 IgG2c κ type antibody inhibitor. Anti-Mouse osteopontin/SPP1 Antibody (103D6) increases cytotoxic T lymphocyte lytic activity and suppresses colon tumor growth. Anti-Mouse osteopontin/SPP1 Antibody (103D6) ameliorates liver injury in common bile duct ligation (CBDL)-induced primary sclerosing cholangitis mice models.

Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.

N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC₅₀ = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC₅₀ = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration.

Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC₅₀s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.

Saikosaponin A is the main active ingredient in Bupleurum chinense, which can regulate lipid metabolism and promote cholesterol efflux in early atherosclerosis. In addition, Saikosaponin A may also serve as a potential peroxisome proliferator-activated receptor γ (PPAR-γ) agonist, significantly promoting the expression of PPAR-γ. Saikosaponin A can be used in the study of hyperlipidemic pancreatitis.

L-Glutathione reduced (Standard) is the analytical standard of L-Glutathione reduced. This product is intended for research and analytical applications. L-Glutathione reduced (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.

Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is an orally active, effective and selectively methanogenic bacteria inhibitor with bactericidal effects. Chlortetracycline hydrochloride is also a antibiotic that acts by inhibiting bacterial protein synthesis. Additionally, Chlortetracycline hydrochloride is a specific and potent calcium ionophore antibiotic, inhibiting binding of aminoacyl-tRNA to ribosomes.

Oxoadipic acid is a key intermediate metabolite in the lysine degradation pathway. The level of Oxoadipic acid is significantly negatively correlated with the abundance of Staphylococcus. That is, the higher the abundance of Staphylococcus-a potential pathogenic bacterium that usually increases in ulcerative colitis-the lower the level of Oxoadipic acid. Oxoadipic acid can be used in the research of ulcerative colitis.

PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC₅₀ value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC₅₀  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis.

α-Amyrin is a pentacyclic triterpenoid compound with oral activity. α-Amyrin activates the ERK and GSK-3β signaling pathways. α-Amyrin can inhibit cancer cells proliferation and induce apoptosis. α-Amyrin shows anti-bacterial and anti-inflammation activity. α-Amyrin can reduce blood glucose level. α-Amyrin can be used for the researches of cancer, infection, inflammation, metabolic disease and neurological disease, such as breast cancer, Streptococcus oralis infection, skin inflammation and diabetes.