Interleukin Related Modulator

GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC₅₀ of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma.

RO8323 is an orally active, selective CDK8/CDK19 inhibitor, with an IC₅₀ of 2 nM against CDK8 and 3 nM against CDK19. RO8323 promotes regulatory T cell differentiation, inhibits effector T cell generation, reverses the Teff/Treg ratio, upregulates IL-10 production in myeloid cells, and suppresses the production of TNF-α, IL-6 and IL-12. RO8323 enhances immune reconstitution and prolongs cardiac allograft survival in a dose-dependent manner. RO8323 can be used in the research of chronic graft-versus-host disease, cardiac allograft rejection, acute graft-versus-host disease and experimental autoimmune encephalomyelitis.

IL-17 modulator 5 (compound 26) is a IL-17 inhibitor, with an IC₅₀ of 1 nM.

IIIM1 is an orally active anti-inflammatory peptide. IIIM1 ameliorates the symptoms of experimental autoimmune encephalomyelitis (EAE) by stimulating the proliferation of regulatory T cells and inducing them to produce RA1, and regulating the cytokine balance. IIIM1 can be used in the research of multiple sclerosis (MS).

α-MSH (11-13) (ACTH-(11-13)) is a C-terminal tripeptide of α-MSH that can cross the blood-brain barrier. α-MSH (11-13) exhibits antipyretic, anti-inflammatory, and antibacterial activities. α-MSH (11-13) also exerts neuroprotective effects after traumatic brain injury by inhibiting excessive activation of microglia and reducing neuronal apoptosis. α-MSH (11-13) can be used in research related to traumatic brain injury, fever, and bacterial infections.

APH003 is an orally active IRAK4 PROTAC degrader with a DC₅₀ of 0.74 nM in human peripheral blood mononuclear cells (hPBMCs). APH003 recruits IRAK4 to CRBN to form a ternary complex, mediates the ubiquitination and degradation of IRAK4 via the ubiquitin-proteasome pathway, and inhibits the kinase activity of IRAK4. APH003 inhibits LPS- or IL-1β/LPS-induced phosphorylation of ERK, JNK and NF-κB. APH003 inhibits the secretion of TNF-α, IL-6, IL-8 and IL-13 by stimulated hPBMCs. APH003 exhibits anti-inflammatory activity in rat TNBS-induced intestinal inflammation models and mouse IL-33-induced skin inflammation models. APH003 can be used in research related to inflammatory bowel disease and skin inflammation.

Antiflammin-1 is an anti-inflammatory peptide 1 (MQMKKVLDS). Antiflammin-1 is a derivative of uteroglobin. Antiflammin-1 has anti-inflammatory and antifibrotic actions in bleomycin (HY-108345)-induced lung injury.

2-ARA-LysoPtdEtn (1-Lyso-2-arachidonoyl-sn-glycero-3-phosphoethanolamine) is an orally active polyunsaturated acyl lysophosphatidylethanolamine. 2-ARA-LysoPtdEtn diminishes formation of LTC₄, LTB₄, and 12-HETE. 2-ARA-LysoPtdEtn lowers levels of IL-1β, IL-6, TNF-α, and NO. 2-ARA-LysoPtdEtn augments IL-10 levels and upgrades formation of 15-HETE and LXA₄. 2-ARA-LysoPtdEtn can be used for the research of peritonitis.

Lemairamin (Wgx-50) is a hydroxylamine compound. Lemairamin can be isolated from the pericarps of the Zanthoxylum plants. Lemairamin activates α7nAChR, stimulates the expression of IL-10 and POMC. Lemairamin shows a decrease in Akt. Lemairamin attenuates DSS-induced intestinal inflammation. Lemairamin alleviates pain hypersensitivity.

ADP-β-S (Adenosine 5'-(β-thiodiphosphate)) trilithium is a non-hydrolyzable ADP analog and a P2Y12 receptor agonist. ADP-β-S trilithium activates the P2Y12 receptor in microglia, thereby triggering downstream inflammatory signaling pathways. ADP-β-S trilithium activates P2Y purinergic receptors in rat pancreatic β cells and enhances glucose-induced insulin secretion. ADP-β-S trilithium can be used in the research of diseases such as inflammation and diabetes.

IKZF2-degrader 5 is a highly efficient, highly selective, rapidly acting, and orally active IKZF2 molecular glue degrader. IKZF2-degrader 5 induces IKZF2 degradation via the Cullin-CRBN-dependent pathway. IKZF2-degrader 5 promotes the production of pro-inflammatory IL-2. IKZF2-degrader 5 attenuates the immunosuppressive function of regulatory T cells (Tregs). IKZF2-degrader 5 triggers rapid, significant, and sustained IKZF2 degradation in the spleen and thymus of mice. IKZF2-degrader 5 inhibits tumor growth. IKZF2-degrader 5 can be used for the research of B16F melanoma.

PNA5 is a novel, blood-brain barrier permeable glycosylated angiotensin-(1-7) peptide and MasR agonist. PNA5 inhibits IL-7, increases IL-10. PNA5 inhibits ROS generation, decreases Iba-1 expression. PNA5 exhibits sustained cognitive protective effects. PNA5 rescues blunted cerebral functional hyperemia. PNA5 can be used in the research of inflammation-related brain diseases.

IL-17 modulator 1 is an orally active, highly efficacious small molecule IL-17 modulators extracted from patent WO 2020127685. IL-17 modulator 1 can be used for the research of preventing, researching or ameliorating a variety of diseases including psoriasis, ankylosing spondylitis and psoriatic arthritis.

HPK1-IN-69 is an orally active HPK1 inhibitor with an IC₅₀ of 1.7 nM. HPK1-IN-69 inhibits the HPK1-mediated TCR signaling pathway, reduces the phosphorylation level of SLP76, and promotes the release of IL-2. HPK1-IN-69 exhibits in vivo anti-tumor activity in mouse models. HPK1-IN-69 can be used for the research of colorectal cancer and MC38 syngeneic tumors.

IL-17 modulator 8 (compound 286) is an orally active modulator of IL-17. IL-17 modulator 8 significantly reduces IL-6, IFN-γ, and edema. IL-17 modulator 8 can used in study arthritis.

IL-17 modulator 9 (compound 453) is an orally active modulator of IL-17. IL-17 modulator 9 significantly reduces IL-6, IFN-γ, and edema. IL-17 modulator 9 can used in study inflammation.

LMP-420 is a selective tumor necrosis factor-α (TNF-α) inhibitor. LMP-420 reduces the release of pro-inflammatory cytokines (e.g., IL-1β, IL-2), inducing the expression of anti-inflammatory cytokine IL-10 and anti-apoptotic molecules SOCS-1 and Mn-SOD. LMP-420 also downregulates chemokines (e.g., IP-10, MCP-1) to reduce immune cell infiltration. LMP-420 is promising for research of type 1 diabetes mellitus, inflammatory diseases (e.g., colitis), and HIV-Mycobacterium tuberculosis coinfection.

cyclo-Cannabigerol (cyclo-CBG) is the major metabolite of Cannabigerol generated by cytochrome P450. Cyclo-Cannabigerol has weak anti-inflammatory activity.

IL-17 modulator 2 (compound 159) is an orally active modulator of IL-17. IL-17 modulator 2 significantly reduces IL-6, IFN-γ, and edema. IL-17 modulator 2 can used in study arthritis.

13 (S)-HOTrE is an oxylipin metabolite of α-Linolenic acid (HY-N0728). 13 (S)-HOTrE mediates the inactivation of the NLRP3 inflammasome through the PPAR-γ pathway to exert anti-inflammatory effects. 13 (S)-HOTrE inhibits NF-κB nuclear translocation, ROS production, autophagy and IL-1β levels, induces apoptosis, and increases IL-10 levels. 13 (S)-HOTrE alleviates LPS-induced inflammatory responses in macrophages, prolongs the survival time of septic mice, and regulates the immunometabolic phenotype in parenteral nutrition mouse models. 13 (S)-HOTrE can be used in the research of immune and inflammation-related diseases.