Brazikumab (AMG 139) is a human IgG2 monoclonal antibody, selectively binds the p19 subunit of IL-23, with a KD of 0.138 nM for human IL-23. Brazikumab can be used for the research of Crohn's disease[1].
(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].
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders[1][2][3].
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca2+ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer[1][2][3]
Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a high affinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells[1][2].
Apilimod(STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-γ/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.
Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate[1].
SC144 hydrochloride is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.IC50 value: < 1 uM (Cell assay) [1]Target: gp130 inhibitorSC144 shows greater potency in human ovarian cancer cell lines than in normal epithelial cells. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. In addition, SC144 shows potent inhibition of gp130 ligand-triggered signaling. Oral administration of SC144 delays tumor growth in a mouse xenograft model of human ovarian cancer without significant toxicity to normal tissues.
Nidanilimab (CAN04) is a fully humanized monoclonal anti-IL1RAP antibody with a Kd value of 1.10 pM. Nidanilimab blocks IL1α and IL1β signaling and stimulates the immune system to destroy tumour cells. Nidanilimab can be used in research of non-small lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC) [1][2].
Linderaspirone A is a natural compound that can be isolated from the roots of Lindera aggregate. Linderaspirone A shows significant inhibitory effects on the production of prostaglandin E2 (PGE2),TNF-α, and IL-6 [1][2].
Nosantine racemate is the racemate of Nosantine. Nosantine is an inducer of IL-2 or enhancer of IL-2 induction by phytohemagglutinin (PHA).
CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a high affinity for binding to CD47 with a subnanomolar Kd value. CC-90002 can be used for the research of hematologic malignancies and solid tumors[1][2].
Efineptakin alfa (NT-17) is a long-acting recombinant human IL-7. Efineptakin alfa supports the proliferation and survival CD4+ and CD8+ cells in both human and mice. Efineptakin alfa can be used for glioblastoma research[1].
Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo[1].
Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression[1].
Vadimezan (ASA-404; DMXAA), the vascular disrupting agent, is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines.
Rolinsatamab is a potent dual IL-4 and IL-13 inhibitor as a fully humanized bispecific monoclonal antibody. Rolinsatamab chimeric antigen receptor sequence T cell. Rolinsatamab can be used in research of immune disease[1].
Ordesekimab (AMG 714; PRV-015) is a fully human IgG1κ anti-IL-15 (Interleukin Related) monoclonal antibody. The binding of Ordesekimab to IL-15 inhibits the interaction of IL-15 with the IL-2Rβ and common γ chain of the IL-15 receptor complex, but not with the IL-15Rα chain. Ordesekimab has the potential for study of nonresponsive celiac disease (NRCD)[1].
Gamma-glutamylcysteine (TFA) ((γ-glutamylcysteine (TFA)), an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine (TFA) also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β) and attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes[1].
Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
Tyrphostin A1(AG9) inhibits CD40L-stimulated IL-12 production in macrophage cultures and antigen-induced generation of Th1 cells.IC50 value: Target: IL-12 production inhibitorAddition of increasing concentration of A1 resulted in a dose dependent decrease of IL-12 p40, with maximal inhibition (62.5%) occurring at a dose of 10 μM. tyrphostin A1 blocks CD40L-induced translocation of NF-κB to the nucleus, and reduces the activation of IL-12 p40 gene. In vivo therapy with A1 leads to decrease in generation of myelin basic protein (MBP) specific encephalitogenic T cells. In addition, treatment of SJL/J mice with A1 results in attenuation of experimental allergic encephalomyelitis (EAE) [1]. Tyrphostin A1 is a much weaker inhibitor of TK than other tyrphostins (IC50>1250 μM for epidermal growth factor receptor (EGFR) kinase), and therefore often used to differentiate TK-mediated effects of tyrphostins from other non-specific effects [2].
Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling[1][2][3].
Di-O-methyldemethoxycurcumin, a curcuminoid analog isolated from the medicinal plant Curcuma longa L., inhibits IL-6 production with an EC50 of 16.20 μg/mL. Anti-inflammatory and antioxidant properties[1].
Hydrocortisone hemisuccinate (Hydrocortisone 21-hemisuccinate), a physiological glucocorticoid, and is an orally active steroidal anti-inflammatory drug (SAID). Hydrocortisone hemisuccinate inhibits proinflammatory cytokine activity, with IC50s of 6.7 and 21.4 μM for IL-6 and IL-3, respectively. Hydrocortisone hemisuccinate can be used for the research of ulcerative colitis (UC)[1][2][3].
Vamikibart is a chimeric humanized IgG2κ antibody targeting IL6[1].
Nogapendekin alfa is a superagonist of IL-15. Nogapendekin alfa promotes the proliferation and viability of immune cells. Nogapendekin alfa combines with Inbakicept (HY-P99661) at a ratio of 2:1, to form ALT-803, an IL-15 cytokine antibody fusion protein. ALT-803 reduces tumor burden by activation of NK cells and CD8+ T cells[1].
Oxazolone is a haptenizing agent that induces acute or chronic inflammation of the large intestine and is used to construct models of colitis. Oxazolone can cause Th1/Th2-dependent colitis with weight loss and diarrhea. Oxazolone-induced inflammation can be mitigated by neutralizing anti-IL-4 or anti-TNF-α antibodies or decoy IL-13R2-α-FC proteins[1].
Dovanvetmab (ZTS-00521505) is an IgG1-κ antibody targeting Felcat IL31. Mainly expressed by CHO (Chinese Hamster Ovary) cells[1].
Imsidolimab (ANB 019) is a high-affinity, humanized monoclonal antibody of anti-IL-36R. Imsidolimab antagonizes IL-36 cytokine signal transduction. Imsidolimab has potential application in generalized pustular psoriasis (GPP) and other inflammatory skin diseases[1][2].