Dexchlorpheniramine is an potent and blood-brain barrier (BBB) penetrant histamine 1 (H1) receptor antagonist with anticholinergic properties. Dexchlorpheniramine can be used for researching allergies[1].
Tylvalosin (Acetylisovaleryltylo?sin) is a broad-spectrum macrolide antibiotic that has antibacterial activity. Tylvalosin is an antiviral agent and can be used for PRRSV infection. . Tylvalosin induces apoptosis. Tylvalosin also has anti-inflammatory activity, relieves oxidative stress, and relieves acute lung injury by suppression of NF-κB activation[1][2].
Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively.
ACAT-IN-2 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 187. ACAT-IN-2 inhibits NF-κB mediated transcription[1].
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ALR-38 is a 5-lipoxygenase (5-LOX) inhibitor (IC50: 1.1 μM) with anti-inflammatory activity. ALR-38 effectively reduces ROS levels in neutrophils[1].
TNF-α-IN-10 (compound 8a) is a IL-6 and TNF-α inhibitor. TNF-α-IN-10 shows anti-inflammatory activity[1].
THR-β agonist 6 is an orally active, selective thyroid hormone receptor β (THR-β) agonist with EC50s of 0.03 μM and 0.22 μM for THR-β and THR-α, respectively. THR-β agonist 6 exhibits an xcellent liver-to-serum ratio of 93:1 in mice. THR-β agonist 6 has the potential for nonalcoholic steatohepatitis (NASH) research[1].
NLRP3-IN-9 is a potent NLRP3 inhibitor. NLRP3-IN-9 inhibits IL-1β release. NLRP3-IN-9 reduces inflammation and mechanical hyperalgesia. NLRP3-IN-9 has the potential for the research of gout[1].
16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes[1][2].
PDE4-IN-14 (Compound 1) is a PDE4 inhibitor that can be used in the study of PDE4-related diseases (such as inflammatory and immune diseases, cancer, and metabolic diseases, etc.)[1].
ABC1183 is a potent, selective, orally active GSK3α/β and CDK9 inhibitor with IC50 of 327/657 nM and 321 nM (CDK9/cyclin T1), shows growth inhibitory activity against a broad panel of cancer cell lines; decreases cell survival through G2/M arrest and modulates oncogenic signaling through changes in GSK3, GS and β-catenin phosphorylation and MCL1 expression; suppresses tumor growth and inflammation-driven gastrointestinal disease symptoms without organ or hematological toxicity in vivo.
PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and with great potential for use in the treatment of inflammatory disorders and cancer metastasis[1].
Picroside III is an iridoid glycoside isolated from Picrorhiza scrophulariiflora (PS), a traditional Chinese medicine[1].
BnO-PEG6-OH is a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Aloperine is an alkaloid in sophora plants such as Sophora alopecuroides L, which has shown anti-cancer, anti-inflammatory and anti-virus properties[1]. Aloperine is widely used to treat patients with allergic contact dermatitis eczema and other skin inflammation in China[2]. Aloperine induces apoptosis and autophagy in HL-60 cells[1].
ISIS 104838 is an antisense oligonucleotide drug that reduces the production of tumor necrosis factor (TNF-alpha), a substance that contributes to joint pain and swelling in rheumatoid arthritis.
Nasunin, an antioxidant anthocyanin, possesses antiangiogenic activity[1].
Clobetasone butyrate is a synthetic glucocorticoid and has topical anti-inflammatory activity especially in skin. Clobetasone butyrate can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis and psoriasis[1].
IL-2-IN-1 is a potent IL-2 inhibitor with an IC50 value of 1978 nM. IL-2-IN-1 shows antiproliferative activities[1].
C11 BODIPY 581/591 is a lipid-soluble ratiometric fluorescent indicator of lipid oxidation. Upon oxidation, its excitation maximum shifts from 581 to 500 nm and the emission maximum shifts from 591 to 510 nm. C11 BODIPY 581/591 has been used in the quantitation of ferroptosis.
FeTPPS, a 5,10,15,20-tetrakis (4-sulfonatophenyl) porphyrin iron III chloride peroxynitrite decomposition catalyst, possessed evident neuroprotective effects in a experimental model of spinal cord damage[1]. FeTPPS acts as a peroxynitrite scavenger and anti-nitrating agent in vivo. FeTPPS reduces nitric oxide (NO) production and apoptosis process[2].
Paridiprubart (NI-0101) is a humanised anti-TLR4 monoclonal antibody. Paridiprubart has the potential for the research of rheumatoid arthritis[1].
MJN110 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor[1]. MJN110 reduces hepatic macrophage number, inflammatory gene expression and slowes down fibrosis progression[2].
Hetrombopag is a potent, selective, orally-active Thrombopoietin (TPO) receptor agonist; specifically stimulates proliferation and/or differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells, with low nanomolar EC50 values through stimulation of STAT, PI3K and ERK signalling pathways; specifically enhances the viability and promoted the growth of 32D-MPL cells in hollow fibres implanted in nude mice, exhibiting much higher potency than eltrombopag in vivo. Other Indication Phase 2 Clinical
trans-Stilbene-NHCO-(CH2)3-acid, a trans-stilbene hapten, can be used to elicit a panel of monoclonal antibodies that display a range of fluorescent spectral behavior[1].
P2X7 receptor antagonist-2 is a potent P2X7 receptor antagonist with a pIC50 value of 6.5-7.5. P2X7 receptor antagonist-2 has efficacy of combating neuroinflammation[1].
Vapendavir diphosphate (BTA798 diphosphate) is a potent enteroviral capsid binder (CB). Vapendavir diphosphate (BTA798 diphosphate) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains[1][2].
HIF-2α agonist 2 (compound 10) is a HIF-2α agonist with an EC50 value of 1.68 μM at the dose of 20 μM. HIF-2α agonist 2 is non-cytotoxic against 786-O-HRE-Luc cells. HIF-2α agonist 2 can be used for oxygen metabolism research[1].
Atractylone (Atractylon) is a sesquiterpenoid extracted from Atractylodis Rhizoma. Atractylone (Atractylon) alleviates influenza A virus (IAV)-induced lung injury via regulating the TLR7 signaling pathway, and acts as a promising agent for IAV treatment. Atractylone (Atractylon) inhibits the degranulation of mast cell and exhibits potential for the treatment of mast cell-mediated allergic reactions[1][2].