Interleukin Related Activator

Y 25510 is a 1H-pyrazolo[3,4-b]pyridine-1-acetic acid derivative. Y 25510 stimulates production of cytokines (IL-1α, IL-1β, IL-10 and IL-6).

STING agonist-50 is an orally active STING agonist with an IC₅₀ of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer.

PD-1/PD-L1-IN-54 (Compound 6) is a moderately affinic PD-1/PD-L1 inhibitor (K_D: PD-1, 55.8 μM; PD-L1, 46.4 μM; IC₅₀: 88.6 μM). PD-1/PD-L1-IN-54 inhibits PD-1/PD-L1 interactions and shows anticancer activity by activating CD8⁺ T cells, upregulating PD-1 expression, and increasing secretion of IFN-γ and IL-2. PD-1/PD-L1-IN-54 inhibits cancer cell proliferation and promotes apoptosis. PD-1/PD-L1-IN-54 also regulates T cell immunity through the PI3K/Akt pathway correlated with PD-1/PD-L1.

Cbl-b-IN-29 is an orally active CBL-B inhibitor. Cbl-b-IN-29 binds to the CBL-B active pocket. Cbl-b-IN-29 induces Jurkat cell release IL-2 with an EC₅₀ of 159 nM, effectively inhibiting the function of immune E3 ubiquitin ligase. Cbl-b-IN-29 demonstrates robust anti-tumor efficacy in vivo with good tolerability and no observed adverse reactions. Cbl-b-IN-29 can be used for cancer immunotherapy, colorectal cancer and immune-oncology combination research.

Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.

4-Hydroxybenzophenone-d₄ (4HBP-d₄) is the deuterated-labeled 4-Hydroxybenzophenone (HY-W014937). 4‑Hydroxybenzophenone (4HBP) is a major metabolite of Benzophenone (HY-Y0546) and is orally active. 4-Hydroxybenzophenone triggers endoplasmic reticulum stress and activates the PERK-eIF2α-ATF4-CHOP and IRE1α-XBP1s pathways, and inhibits IκB translation. 4-Hydroxybenzophenone induces endoplasmic reticulum stress, unfolded protein response activation, protein homeostasis imbalance, protein aggregation, oxidative stress, ROS accumulation, mitochondrial membrane potential decrease, ATP depletion, and cytotoxicity. 4-Hydroxybenzophenone induces neural stem cell apoptosis (apoptosis) and affects neuronal differentiation. 4-Hydroxybenzophenone promotes malignant proliferation of hepatocellular carcinoma cells and xenograft tumor growth in nude mice. 4-Hydroxybenzophenone can be used in research related to neurodevelopmental toxicity and hepatocellular carcinoma.

10 (11)-Cl-BBQ is a high-affinity aryl hydrocarbon receptor (AhR) agonist. 10 (11)-Cl-BBQ is a mixture of 10-Cl-BBQ and 11-Cl-BBQ, among which 11-Cl-BBQ exhibits higher AhR activation potency than 10-Cl-BBQ. Low-dose/short-term AhR activation by 10 (11)-Cl-BBQ promotes IL-17 production, while high-dose/sustained activation induces regulatory T cells and suppresses immune responses. 10 (11)-Cl-BBQ can be used in immunomodulation research.

PD-1/PD-L1-IN-65 is a PD-1/PD-L1 checkpoint inhibitor, with an EC₅₀ of 6.06 μM for blocking the PD-1/PD-L1 interaction and a K_d of 1.43 μM for PD-L1. PD-1/PD-L1-IN-65 upregulates pro-inflammatory cytokines IFN-γ, IL-1α, IL-1β and the cytolytic protein perforin, and reverses T cell exhaustion. PD-1/PD-L1-IN-65 enhances T cell-mediated cancer cell lysis. PD-1/PD-L1-IN-65 can be used in the research of breast cancer.

Murabutide is an immunomodulator and also a NOD2 receptor agonist. Murabutide enhances the signal transduction of ATR and NOD2, mediates the activation of the DDR pathway, and thereby repairs radiation-induced DNA double-strand breaks. Murabutide inhibits radiation-induced cell apoptosis and protects cells and mice from radiation-induced toxic damage. Murabutide induces the expression and DNA-binding activity of Oct-1 in macrophages, thereby inhibiting the transcription and replication of HIV-1. Murabutide reduces the expression levels of CD4 and CCR5 on the surface of macrophages, and induces the secretion of β-chemokines, TNF-α and IL-6. Murabutide enhances non-specific viral resistance and targets reticuloendothelial cells. Murabutide can be used in research related to radiation-induced damage and human immunodeficiency virus type 1 infection.

GCS-12 is a Th1/2-balanced sulfonamide glycolipid with improved interaction with CD1d. GCS-12 is an agonist for natural killer T (NKT) cell, that induces the secretion of cytokine IFN-γ and IL-4, and exhibits immunomodulatory and anti-tumor activities in mice.

HPK1-IN-58 (Compound 26) is an inhibitor of HPK1 (IC₅₀: 2.6 nM) and SLP76 (IC₅₀: 20 nM). HPK1-IN-58 enhances IL-2 secretion and reverses PGE2-induced immunosuppression. HPK1-IN-58 can be used in anti-tumor immunity research.

IDO1-IN-34 is a selective IDO1 inhibitor with an IC₅₀ of 0.093 μM. IDO1-IN-34 exhibits cytotoxicity against various cancer cell lines. IDO1-IN-34 inhibits the kynurenine (kynurenine) pathway and activates IL-2. IDO1-IN-34 induces cell apoptosis via the endogenous mitochondrial pathway, while increasing the levels of cytochrome c, caspase-3, caspase-9 and PARP-1. IDO1-IN-34 can be used for research on liver cancer, lung cancer, breast cancer, prostate cancer, colon cancer and leukemia.

TLR7/8 agonist 14 is a TLR7 and TLR8 agonist with EC₅₀ values of 0.53 μM and 4.3 μM, respectively. TLR7/8 agonist 14 increases the secretion of the proinflammatory cytokines TNF-α, IL-1β, IL-8 and IFN-γ. TLR7/8 agonist 14 increases cytokine secretion and expression of CD86. LR7/8 agonist 14 can be used for research colorectal carcinoma.

SAR444200 is a nanobody targeting GPC3 (glypican-3) and TCRαβ (T-cell receptor αβ). The K_D of SAR444200 for human GPC3 is 0.023 nM, and its K_D for human TCRαβ is 5.2 nM. SAR444200 mediates T cell-dependent cytotoxicity, and exhibits high selectivity and killing activity against GPC3-positive tumor cells. SAR444200 binds to GPC3 in a dual-epitope manner, and binds to TCRαβ via its N-terminal nanobody, forming an artificial immunological synapse between T cells and tumor cells. SAR444200 can be used in studies of GPC3⁺ solid tumors, including liver cancer, lung squamous cell carcinoma and melanoma.

LAS190792 is a bifunctional muscarinic acetylcholine receptor (mAChR) antagonist and β2-adrenergic receptor agonist. LAS190792 has a pIC₅₀ of 8.8 against human M3 muscarinic receptor and a pIC₅₀ of 9.1 against human β2-adrenergic receptor. LAS190792 exhibits vasodilatory and anti-inflammatory activities, and induces sustained bronchodilation in dogs. LAS190792 inhibits the release of IL-8, MMP9, IL-1β and GM-CSF from lipopolysaccharide-stimulated neutrophils. LAS190792 can be used in research related to respiratory system diseases.

1α-Hydroxyvitamin D5 (CARD-024) is a vitamin D analog with extremely low hypercalcemic effects. 1α-Hydroxyvitamin D5 effectively attenuates the pro-fibrotic response of colonic myofibroblasts to TGFβ and high-stiffness substrates by inhibiting the expression of αSMA, the phosphorylation of FAK, and the gene expression of MLCK and ET-1, while activating the anti-inflammatory pathway of IL-1β/COX-2. 1α-Hydroxyvitamin D5 can be used in research related to intestinal fibrosis associated with Crohn's disease.

IRBP (651-670) human, mouse TFA is an epitope and uveitis inducer naturally processed from the conserved region of native IRBP. IRBP (651-670) human, mouse TFA increases the levels of proinflammatory cytokines in ocular tissues (IL-1β, IL-6, TNFα, IL-17A and IL-17F). IRBP (651-670) human, mouse TFA is a IRBP fragment conserved among human, mouse and bovine species. IRBP (651-670) human, mouse TFA induces experimental autoimmune uveitis. IRBP (651-670) human, mouse TFA is applicable to research related to experimental autoimmune uveitis.

SMU-3k is a STING activator and PD-L1 inhibitor, with a PD-L1 IC₅₀ of 106 nM, a K_D of 386 nM for human PD-L1, and a K_D of 352 nM for murine PD-L1. SMU-3k activates the STING pathway, induces phosphorylation of TBK1 and IRF3, and promotes the expression of IFN-β, IL-6 and CXCL10. SMU-3k blocks the PD-1/PD-L1 interaction, reduces PD-L1 levels and induces PD-L1 internalization. Through dual immunomodulation, SMU-3k exerts synergistic tumor growth inhibitory effects in a mouse colon cancer model. SMU-3k can be used for the research of colon cancer.

Sodium chloride, United States Pharmacopeia (USP) Reference Standard is an orally active salt. Sodium chloride, United States Pharmacopeia (USP) Reference Standard induces the expression of ATP1A1. Sodium chloride, for cell culture induces the pro-inflammatory cytokines IL-2, TNFα, IL-9 and several chemokines. Sodium chloride, United States Pharmacopeia (USP) Reference Standard enhances the anti-tumor activities of Digoxin (HY-B1049) against small cell lung cancer. Sodium chloride, United States Pharmacopeia (USP) Reference Standard drives autoimmune disease by the induction of pathogenic Th17 cells.

VISTA-IN-1 is an orally active VISTA inhibitor. VISTA-IN-1 inhibits the function of VISTA and promotes the secretion of IL-2. VISTA-IN-1 exerts inhibitory effects on mouse melanoma in vivo. VISTA-IN-1 is applicable to melanoma-related research.