Interleukin Related Activator

PROTAC HPK1 Degrader-8 is a HPK1 PROTAC degrader with a DC₅₀ of 1-10 nM. PROTAC HPK1 Degrader-8 promotes HPK1 ubiquitination and degradation. PROTAC HPK1 Degrader-8 induces IL-2 production, with an EC₅₀ of 3 nM. PROTAC HPK1 Degrader-8 can be used in research related to hematologic malignancies and solid tumors.

PTPN22-IN-3 is a potent, selective, and orally active inhibitor of PTPN22 with an IC₅₀ of 0.49 μM and a K_i of 0.28 μM. PTPN22-IN-3 exhibits over 14-fold selectivity against a broad panel of PTPs and shows no significant inhibition against SRC/CSK kinases or IDO1/Arginase metalloenzymes. PTPN22-IN-3 enhances TCR signaling, increases IL-2 expression and secretion, and promotes mouse splenic T cell proliferation. In immune-competent C57BL/6J mice, PTPN22-IN-3 suppresses MC38 syngeneic tumor growth and synergizes with Pembrolizumab (anti-PD-1) (HY-P9902A) therapy. PTPN22-IN-3 can be used for the study of colorectal cancer and other solid tumors responsive to T cell-mediated anti-tumor immunity.

RS-0481 is an orally active lymphocyte population function restorer. RS-0481 enhances IL-2 production activity. RS-0481 can re-establish the function of certain lymphoid cell populations impaired by the presence of a growing tumor in an animal. RS-0481 markedly augments the tumor-specific cytotoxic T lymphocytes, T_DTH, and the nonspecific lymphokine-activated-killer-cell-like cell responses.

PROTAC HPK1 Degrader-4 is an orally active HPK1 PROTAC degrader and immune activator, with DC₅₀ values of 3.16 nM and 72.59 nM in Jurkat cells and PBMCs, respectively. PROTAC HPK1 Degrader-4 induces degradation via the ubiquitin-proteasome system, downregulates the HPK1-SLP76 signaling pathway, reduces the phosphorylation level of SLP76 (S376), and promotes immune activation. PROTAC HPK1 Degrader-4 can be used in the research of colorectal cancer and B-cell lymphoma.

Stigmastanol (Standard) is the analytical standard of Stigmastanol. This product is intended for research and analytical applications. Stigmastanol is a 6-amino derivative. Stigmastanol can be isolated from Hypericum riparium. Stigmastanol increases the secretion of IL-2 and IL-10. Stigmastanol reduces the maximum mitochondrial respiration of cells. Stigmastanol has beneficial effects on the weakened immune function of asthma.

Adenosine receptor antagonist 6 is an orally active and selective A_2A adenosine receptor (A_2AAR) antagonist, with a K_i of 19.18 nM. Adenosine receptor antagonist 6 inhibits 5’-N-ethylcarboxamide adenosine (NECA) (HY-103173)-mediated cAMP production (IC₅₀ = 0.089 μM) and immunosuppression, while promoting IL-2 and IFN-γ secretion. Adenosine receptor antagonist 6 abolishes the immunosuppressive effects of adenosine on T-cell activation and cytokine release. Adenosine receptor antagonist 6 inhibits tumor growth in a CT26/MC38 xenograft model. Adenosine receptor antagonist 6 can be used for the study of colon cancer.

5-Androstenetriol is a systemic radiation protector that can boost the host's immunity, leading to increased resistance to infections. 5-Androstenetriol can raise levels of IL-2, IL-3, and IFN, while countering the immunosuppressive effects of Hydrocortisone (HY-N0583).

23ME-00610 is a humanized effector-function-null IgG1 antibody targeting CD200R1, with a K_d of <0.1 nM for hCD200R1. 23ME-00610 blocks the binding of CD200 to CD200R1 and inhibits the recruitment of the downstream adaptor protein DOK2 to CD200R1. 23ME-00610 restores IL-2 production suppressed by CD200. 23ME-00610 induces cytokine production in cells. 23ME-00610 enhances cell-mediated tumor cell killing in vitro. 23ME-00610 can be used for melanoma research.

M802 is an anti-HER2/CD3 bispecific antibody, with a K_d of 0.578 nM for human HER2 and a K_d of 71.2 nM for human CD3. M802 inhibits the PI3K/AKT and MAPK signaling pathways, suppresses tumor cell proliferation, activates caspase-3, and promotes tumor cell apoptosis (apoptosis). M802 recruits and activates CD3-positive immune cells, mediates cytotoxicity against HER2-positive tumor cells, and induces immune cells to secrete IFN-γ, TNF-α, IL-2 and IL-6. M802 exhibits anti-tumor efficacy in mice with gastric cancer xenografts. M802 can be used in research related to HER2-positive breast cancer, HER2-positive gastric cancer and other cancers. The recommended isotype control is human IgG1 kappa (HY-P99001).

DC-PGKI is an orally active ATP-competitive PGK1 inhibitor(IC₅₀ = 0.16 Μm, K_d = 99.08 nM). DC-PGKI stabilizes PGK1 in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. DC-PGKI-mediated inhibition of PGK1 leads to the accumulation of NRF2 (nuclear factor-erythroid factor 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1β and IL-6 genes, and suppresses the LPS-induced expression of these genes. DC-PGKI can be used for the study of colitis.

KRN7000 analog 2 is a iNKT agonist, which is promising for research of antitumor agents and vaccine adjuvants.

LG190155 is a nonsteroidal vitamin D receptor (VDR) agonist. LG190155 activates VDR in mesenchymal stem cells, thereby upregulating the BMP6-IL6 autocrine axis. Pretreatment of mesenchymal stem cells with LG190155 significantly enhances their ability to induce differentiation of acute myeloid leukemia cells, without inducing hypercalcemia. LG190155 is applicable to research related to acute myeloid leukemia (AML).

Cbl-b-IN-28 (Compound B2) is an orally active Cbl-b inhibitor. Cbl-b-IN-28 promotes the secretion of cytokines such as IL-2 and enhances the function of immune cells by regulating the phosphorylation levels of key proteins in the T-cell receptor signaling pathway. Cbl-b-IN-28 can be used in research in the field of cancer immunology.

HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC₅₀ value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC₅₀ of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC₅₀ of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research.

MSP-1 P2 is a synthetic peptide of merozoite surface protein-1 (MSP-1). MSP-1 P2 stimulates umbilical cord blood lymphocytes to produce IFN-γ and IL-13, and this immune response is primarily mediated by CD4+ T cells. MSP-1 P2 can be used as a specific antigen stimulus to detect T cell responses and cytokine levels.

GAP214 is a monosaccharide lipid A analogue and TLR4/MD-2 complex modulator.GAP214 binds to the TLR4/MD-2 complex via hydrophobic interactions, salt bridges, and hydrogen bonds, induces dimerization of the complex to initiate intracellular signaling cascades.GAP214 functions as an immunostimulant and vaccine adjuvant, enhances antigen-specific IgG antibody production in a mouse model.

C6 D-Threo Ceramide (d18:1/6:0) is a bioactive sphingolipid and cell-permeable analog of ceramides. C6 D-Threo Ceramide (d18:1/6:0) enhances IL-4 production induced by Phorbol 12-myristate 13-acetate (HY-18739) in EL4 T cells.

PROTAC HPK1 Degrader-7 (compound D02) is a potent and selective PROTAC HPK1 degrader with an DC₅₀ of 3.07 nM. PROTAC HPK1 Degrader-7 exhibits selectivity over GLK. PROTAC HPK1 Degrader-7 induces HPK1 degradation in a CRBN- and proteasome-dependent manner. PROTAC HPK1 Degrader-7 inhibits SLP-76 phosphorylation, induces IL-2 and IFN-γ secretion in human primary T cells. PROTAC HPK1 Degrader-7 can be used for immunology research.

SMU-L11-R is a selective TLR7 agonist with an EC₅₀ of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8⁺T cells. SMU-L11-R shows potential in colorectal cancer studies.

RR-171 is an amino acid polypeptide and an inhibitor of the Wnt signaling pathway. RR-171 reduces the expression levels of Wnt-1, GSK3β and β-catenin. RR-171 induces apoptosis (Apoptosis) in pancreatic cancer cells, which is characterized by an increased Bax/Bcl-2 ratio, activation of Caspase-3/7/9, and increased Cleaved-PARP; this pro-apoptotic effect can be partially reversed by Z-VAD-FMK (HY-16658B). RR-171 also induces pyroptosis (Pyroptosis) in pancreatic cancer cells, which is manifested by activation of the NLRP-3 inflammasome, activation of Caspase-1, cleavage of GSDMD, upregulation of IL-1β and IL-18, and increased LDH release; this pro-pyroptotic effect can be partially reversed by VX-765 (HY-13205). RR-171 inhibits the viability, proliferation and colony formation of pancreatic cancer cells, with low cytotoxicity against normal cells. RR-171 downregulates the expression of Ki-67 and PCNA in tumor tissues in vivo, with favorable biosafety. RR-171 can be used in studies related to pancreatic cancer.