il-2 production

PKC-theta inhibitor 1 is an inhibitor of PKCθ (Ki of 6 nM)

AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation (IC50 = 1 μM), without blocking basal transcription driven by the β-actin promoter. It has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].

Inosine pranobex (Delimmun) has a number of immunomodulatory effects, including inducing T-lymphocyte differentiation, augmenting macrophage and NK cell functions, and stimulating IL-2 production. Through these effects and others, isoprinosine shows antiviral activity and has applications against subacute sclerosing panencephalitis. It also restores depressed immune responses in Y patients after irradiation and reduces the incidence of infection in leukemia patients undergoing chemotherapy. It is most commonly used to treat the rare measles complication subacute sclerosing panencephalitis in conjunction with intrathecal interferon therapy.

Methylthiouracil is a thiourea-class antithyroid agent that inhibits the synthesis of thyroid hormones and is commonly used to treat hyperthyroidism. Studies have shown that Methylthiouracil can also suppress the production of TNF-α and IL-6, as well as inhibit the activation of NF-κB and ERK1/2. It can be used to induce hyperlipidemia and neurological disorder models.

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

A-770041 is an orally active and selective Lck inhibitor that inhibits concanavalin A-stimulated IL-2 production in whole blood and prevents cardiac allograft rejection. A-770041 reduces pulmonary fibrosis by inhibiting TGF-β production in regulatory T cells.

NKH477 (Colforsin dapropate hydrochloride) is a derivative of forskolin with antidepressant activity. It inhibits ACh-induced Ca2+ mobilization by acting on ionomycin-sensitive storage sites. NKH477 is an adenylyl cyclase activator with bronchodilatory effects, inhibiting the production of CTL, T-cell proliferation in mixed lymphocyte reactions (MLR), as well as IL-2 production and mitogen responses.

Ppc-1 is a chemical compound known for its inhibitory effects on the Gram-negative periodontopathogen Porphyromonas gingivalis. It acts as a mitochondrial uncoupler, enhancing mitochondrial oxygen consumption without affecting ATP production. Additionally, Ppc-1 serves as a cell-permeate inhibitor of interleukin-2 (IL-2). This compound exhibits various beneficial activities, including anti-obesity, antibacterial, and anti-inflammatory properties.

PKCTheta-IN-2 (compound 14) is a potent and selective PKCθ inhibitor (IC50 = 0.25 nM) that suppresses IL-2 production in mice (IC50 = 682 nM).

PQA-18, an inhibitor of p21-activated kinase 2 (PAK2; IC50 = 10 nM), is derived from Ppc-1 (product number 42352) and exhibits immunosuppressive properties. It inhibits IL-2 production in Jurkat T cells induced by Concanavalin A (product number 14951) with an IC50 of 400 nM. Topically applied at 0.1%, PQA-18 reduces the severity of atopic dermatitis, serum IgE levels, and skin thickness in the NC/Nga mouse model. A lower concentration of 0.05% also decreases skin nerve fiber density in NC/Nga mice. Additionally, PQA-18 administered at 4 mg/kg improves graft survival in a rat small intestine transplantation model.

Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.

Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective anticancer compound targeting microtubule proteins. It disrupts microtubule stability, inhibiting microtubule polymerization. This agent causes human tumor cells to arrest in the G0/G1 phase and induces apoptosis (Apoptosis) through activation of the Caspase cascade pathway. Additionally, it exhibits anti-inflammatory properties, inhibiting the production of TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 also suppresses tumor growth in xenograft mice.

KRN7000 analog 8 (compound 8) is a variant of KRN7000 that demonstrates a strong stimulatory effect on IL-2 production. Compared to KRN7000, it induces lower levels of IFN-γ but results in higher IL-4 production.

HPK1-IN-56 (Compound A29) is an HPK1 inhibitor with an IC50 of 2.70 nM. It inhibits downstream p-SLP76 in Jurkat T cells with an IC50 of 8.1 nM. Additionally, HPK1-IN-56 induces IL-2 production in human PBMCs. This compound exhibits anticancer properties, enhancing T cell cytotoxicity and the antitumor efficacy of anti-PD-1 antibodies.

NLRP3-IN-69 (Compound 23) inhibits the activation of NF-κBp65 and the formation of the NLRP3 inflammasome. It suppresses the overexpression of IL-1β, iNOS, and COX-2 induced by LPS, and inhibits the production of NO (IC50=5.66 μM), thereby demonstrating anti-inflammatory activity.

JAK3-IN-17 is an orally active JAK3 inhibitor with an IC50 of 14.56 nM. It demonstrates anti-inflammatory activity by inhibiting the production of IL-2 and IL-6 in a DNCB-induced mouse model of atopic dermatitis.

Cbl-b-IN-16 (compound 31) is an orally active inhibitor of the RING E3 ligase Cbl-b, with an IC50 of 30 nM. It enhances IL-2 production in human T cells with an EC50 of 230 nM and exhibits antitumor activity.

SP-alkyne (compound 8) inhibits the production of IL-2 and the expression of AP-1 and NFAT genes.

Adenosine receptor antagonist 6 is an orally active, selective (S)-enantiomer compound that acts as an A2A adenosine receptor (A2AAR) antagonist. It binds to the A2A adenosine receptor with a Ki value of 19.18 nM. This antagonist inhibits cAMP production mediated by 5’-N-ethylcarboxamide adenosine (NECA) with an IC50 value of 0.089 μM and reduces immunosuppression, while enhancing the secretion of IL-2 and IFN-γ. It counteracts adenosine-induced immunosuppression in T cell activation and cytokine release and inhibits tumor growth in CT26/MC38 xenograft models, making it applicable for colorectal cancer research.

CD28-IN-1 (Compound 19MS-5) is a CD28 inhibitor with a dissociation constant (KD) of 12.48 μM. It demonstrates excellent binding affinity to CD28, effectively hindering the CD28-B7 interaction. CD28-IN-1 suppresses CD28-driven immune activation and reduces cytokine production (IFN-γ, IL-2, and TNF-α) in primary human T cells co-cultured with tumor spheroids and human epithelial tissues. This compound is suitable for use in tumor immunology research.

FPR2 agonist 5 is a selective agonist of formyl peptide receptor 2 (FPR2). It induces Ca2+ mobilization in HL60 cells transfected with FPR2, demonstrating an EC50 value of 1.2 μM, and causes FPR2 desensitization with an IC50 of 0.32 μM. Additionally, FPR2 agonist 5 exhibits neuroprotective effects by reducing LDH release, NO production, and the levels of IL-1β, IL-6, IL-33, and IL-10 in LPS-induced primary microglial cells from mice. It is utilized in research related to neuroinflammatory and inflammatory diseases.

HPK1-IN-65 is a selective, orally active HPK1 inhibitor with an IC50 value of less than 5 nM, demonstrating 1257-fold selectivity over the MAP4K kinase family member GLK. It inhibits pSLP76 phosphorylation with an IC50 of 92.3 nM and stimulates IL-2 production with an EC50 of 398 nM. Additionally, HPK1-IN-65 suppresses the phosphorylation of the TCR-induced SLP76Ser376 site in a dose-dependent manner. This compound is also applicable in colon cancer research.

N-3-oxo-dodecanoyl-L-Homoserine lactone (3-oxo-C12-HSL), a quorum-sensing signaling molecule synthesized by P. aeruginosa and specific B. cepacia complex strains [1][2], facilitates bacterial gene expression modulation in response to cell density escalation and triggers IL-8 production in 16HBE human bronchial epithelial cells [3].

BIRT-377 is a negative allosteric and orally bioavailable inhibitor of ICAM-1 and LFA-1(Ki = 25.8 nM). BIRT-377 inhibits the production of IL-2 and can be used in studies about inflammatory and immune disorders.