IL-2 Modulator

FPFT-2216 is an orally active Molecular glue degrader targeting IKZF1, IKZF3, CK-1α, and PDE6D, with a DC₅₀ of 8 nM against PDE6D. FPFT-2216 mediates ubiquitin-proteasome degradation via the CRL4^CRBN E3 ubiquitin ligase complex and interacts with the non-isoprenoid-binding region of PDE6D. FPFT-2216 activates the p53 signaling pathway, inhibits the CBM complex/NF-κB pathway, upregulates IL-2, suppresses IL-1β and IL-6, and induces tumor cell Apoptosis. FPFT-2216 exhibits anticancer activity against multiple myeloma and lymphoma. FPFT-2216 can be used in research related to multiple myeloma, lymphoma, acute lymphoblastic leukemia, acute myeloid leukemia, pancreatic ductal adenocarcinoma, non-small cell lung cancer, and gastric adenocarcinoma.

Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α.

Ginsenoside F3 is a saponin extracted from the leaves of Panax ginseng with immunoenhancing and antitumor immunostimulatory activities. Ginsenoside F3 upregulates RIPOR2 with a K_d value of 3.77 μM. Ginsenoside F3 enhances NF‑κB activation, upregulates T‑bet and downregulates GATA‑3, increases the production of IL‑2 and IFN‑γ, decreases the production of IL‑4 and IL‑10, reverses CD8⁺ T‑cell exhaustion, restores cytokine secretion, and enhances antitumor immunity in a mouse non‑small cell lung cancer model. Ginsenoside F3 can be used for the research of non-small cell lung cancer.

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).

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.

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.