cd4+ cells

Cyclic-di-GMP disodium (5GP-5GP disodium) is a bacterial second messenger and a STING agonist involved in a variety of prokaryotic processes including biofilm formation, motility, and cell cycle progression.Cyclic-di-GMP disodium displays antiproliferative activity against cancer cells, inducing elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research cancer.

ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50= 1.1 μM in a reporter assay).1It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50= 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated na?ve cord blood human CD4+T cells into Th17 T helper cells.

Anisperimus (LF 15-0195) is an immunosuppressant that enhances activation-induced T-cell death by promoting caspase-8 and caspase-10 activation at the DISC level, and prevents CNS autoimmunity by promoting the development of Foxp3-expressing regulatory CD4 T cells.

Benzoylmesaconine (Mesaconine 14-benzoate) is the most abundant component of Wutou decoction, which is widely used in China because of its therapeutic effect on rheumatoid arthritis. Benzoylmesconine has analgesic activity. Benzoylmesconine may improve the resistance of T6S-mice (or thermally injured mice) to the infection of HSV-1, through the induction of antagonistic CD4+ T cells against burn-associated type-2 T cells.

Ethyl Caffeate (ETHYL 3,4-DIHYDROXYCINNAMATE) suppressed the differentiation of naive CD4+ T cells into Th1 in vitro. Furthermore, Ethyl Caffeate intensely blocked the transcriptional expression in interferon-γ-related signaling, including IFN-γ, T-bet, STAT1, and STAT4.

Naringenin chalcone (Isosalipurpol) has antiallergic activity Naringenin chalcone suppresses asthmatic symptoms by inhibiting Th2 cytokine production from CD4 T cells. Naringenin chalcone is a potent tomato flavonoid that improves adipocyte metabolic functions and exerts insulin-sensitizing effects by activating an adiponectin-related pathway. Naringenin chalcone exhibits anti-inflammatory properties by inhibiting the production of proinflammatory cytokines in the interaction between adipocytes and macrophages, may be useful for ameliorating the inflammatory changes in obese adipose tissue.

Temsavir (BMS626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.

Quazomotide, a class II peptide epitope of WT1 with the sequence RSDELVRHHNMHQRNMTKL, elicits a peptide-specific CD4(+) response to target WT1(+) tumor cells. It serves both as an immunological agent for active immunization and as an antineoplastic agent [1] [2].

NY-ESO-1 (87-111) is a pan-MHC class II-restricted peptide interacting with various HLA-DR and HLA-DP4 molecules, inducing activation of CD4+ T cells with Th1-type and Th-2 Th0-type responses when presented with these molecules.

Defensin HNP-3 is a peptide secreted by human polymorphonuclear leukocytes (PMNs) that has antimicrobial properties. It induces lysis of mammalian cells when used at a concentration of 25 μg/mL. It also inhibits growth of E. faecalis (ED50 = 100 nM) and clinical isolates of P. aeruginosa (MIC90 = 4 μM). HNP-3 binds to recombinant HIV-1 envelope glycoprotein (gp120) and human CD4 (Kds = 52.8 and 34.9 nM, respectively). It also binds to recombinant, immobilized human surfactant protein D (SP-D; Kd = 55.7 nM) and inhibits focus formation in Madin-Darby canine kidney (MDCK) cells infected with influenza A virus (IAV).

S1PL-IN-31 is a dual-function chemical compound acting as an inhibitor of sphingosine-1-phosphate (S1P) lyase with an IC50 value of 210 nM and as an antagonist of the Smoothened (Smo) receptor with an IC50 of 440 nM. Demonstrating therapeutic potential, this compound, at a dosage of 2 mg/kg per day, effectively mitigates cervical and thoracic lymphocyte infiltration and neuromuscular weakness in rats suffering from experimental autoimmune encephalomyelitis (EAE), a condition triggered by the MOG29-152 peptide from myelin oligodendrocyte glycoprotein. Additionally, it significantly decreases the total lymphocyte count, including reductions in subsets of CD4+ T cells, CD8+ T cells, and B cells. At a higher dosage of 100 mg/kg, S1PL-IN-31 elevates S1P levels within the heart and lymph nodes, while doses of 3 and 10 mg/kg per day notably lower heart rates in female rats, showcasing its multifaceted biological impacts and potential for clinical application.

ARN-6039, an orally available inverse agonist of RORγ, targets Autoimmune Neuroinflammatory Demyelinating Disease. Its efficacy was demonstrated in a RORγ-activated IL-17A Prom LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 release from CD4+T cell assays (220 nM).

Flavipin, an aryl hydrocarbon receptor (Ahr) agonist, activates Ahr downstream gene expression in mouse CD4+ T cells and CD11b+ macrophages. This compound disrupts the stabilizing effect of Arid5a on the newly identified target mRNA, Il23a 3′UTR. Additionally, Flavipin demonstrates significant antioxidant properties, evidenced by its DPPH free radical scavenging capability with an IC50 value of 7.2 μM, and exhibits potent α-glucosidase inhibitory activity with an IC50 value of 33.8 μM.

Ferrichrome (iron-free) is a hydroxamate siderophore produced by various fungi (including U. sphaerogena) that facilitates iron chelation and uptake by these organisms and is also used by bacteria as a heterologous siderophore , including Pseudomonas aeruginosa and Vibrio parahaemolyticus. Ferrichrome (iron-free) (0.8 μM) inhibits concanavalin A-induced proliferation of mouse splenic monocytes and reduces the number of concanavalin A-stimulated CD4+ T cells. It also inhibits heme-catalyzed oxidation of LDL by hydrogen peroxide in a concentration-dependent manner.

Efineptakin alfa (NT-17), a long-acting recombinant human interleukin-7 (IL-7), promotes the proliferation and survival of CD4+ and CD8+ cells in both humans and mice. It has applications in glioblastoma research [1].

CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Kocik, J., et al.Di-bromo-based small-molecule inhibitors of the PD-1/PD-L1 immune checkpointJ. Med. Chem.63(19)11271-11285(2020)

Tregalizumab, a humanized IgG1-type monoclonal antibody targeting CD4, selectively activates regulatory T cells (Tregs) with suppressive functions in vitro and has potential applications in researching autoimmune diseases (due to inadequate Treg activity) and allergies [1] [2] [3].

Ibalizumab(TMB-355) is a humanized IgG4 monoclonal antibody that acts as a CD4 receptor inhibitor, blocking the entry of HIV-1 into cells by binding to the CD4 receptor.Ibalizumab has anti-HIV-1 infectious activity and may be used to maintain normal immune function.

Murabutide, a safe synthetic immunomodulator, diminishes the expression of CD4 and CCR5 receptors and promotes the secretion of high levels of beta-chemokines, thereby enhancing nonspecific resistance to viral infections. It does not impact virus entry, reverse transcriptase activity, or the formation of early proviral DNA in the cytoplasm of infected cells [1].

Retrocyclin-1, a Theta-defensin, selectively binds to carbohydrate-rich surface molecules such as fetuin, gp120 (K d =35.4 nM), CD4 (K d =31 nM), and galactosylceramide (K d =24.1 nM) [1], thereby shielding cells from HIV-1 infection.

CFP10 (71–85) is an immunologically active peptide that induces IFN-γ production and cytotoxic T lymphocyte (CTL) activity in CD4+ and CD8+ T cells from individuals with diverse MHC class II and I expression profiles.

Apelin-36(human) TFA, an endogenous agonist of the orphan G protein-coupled receptor APJ, exhibits a potent EC50 of 20 nM and high affinity (pIC5 50 = 8.61) for human APJ receptors in HEK 293 cells. It is involved in significant cardiovascular and metabolic activities. Furthermore, Apelin-36(human) TFA can inhibit the entry of certain HIV-1 and HIV-2 strains into NP2/CD4 cells expressing the APJ receptor. [1] [2] [3] [4]

Apelin-36(rat, mouse) TFA, an endogenous agonist for the orphan G protein-coupled receptor APJ, exhibits a strong affinity for APJ receptors with an IC 50 of 5.4 nM and effectively inhibits cAMP production with an EC 50 of 0.52 nM. Moreover, it obstructs the invasion of certain HIV-1 and HIV-2 strains into NP-2/CD4 cells that express the APJ receptor [1] [2].

Apelin-17(human, bovine) TFA is an endogenous agonist of the orphan G protein-coupled receptor APJ, demonstrating affinity for human APJ receptors on HEK 293 cells with a pIC50 value of 9.02. It also blocks the entry of certain HIV-1 and HIV-2 strains into NP2 CD4 cells that express the APJ receptor [1] [2] [3].

7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 µM. It increases IL-17A production in Th17-polarized isolated human na ve CD4+ T cells when used at a concentration of 300 nM. 7β,27-dihydroxy Cholesterol (60 mg/kg) increases IL-17A production in isolated mouse γδ T cells stimulated with 12-myristate 13-acetate and ionomycin .

Endogenous APJ receptor agonist (EC50 = 20 nM) that is secreted by adipocytes. Binds with high affinity to human APJ receptors expressed in HEK 293 cells (pIC50= 8.61). Involved in regulation of cardiovascular function, fluid homeostasis and feeding. Bloc

RDN2150 (Compound 25), a ZAP-70 inhibitor with an IC50 of 14.6 nM, covalently binds to the C346 residue of ZAP-70, suppressing the expression of CD25 and CD69 and inhibiting the activation of CD4+ T cells, making it suitable for psoriasis research [1].

Indinavir sulfate (L735524 sulfate) is a HIV protease inhibitor.It inhibits the HIV-1 protease with an IC50 value of 0.41 nM and Ki value of 0.24 nM.

BI8626 is a ubiquitin ligase HUWE1 inhibitor with protective effects against spontaneous desiccation syndrome in NOD/ShiLtj mice.BI8626 inhibits intracellular cholesterol and decreases the expression of phosphorylated ZAP-70, CD25, and other activation markers, and inhibits the proliferation of CD4 T-cells.

JNJ-61803534 is a potent, orally active RORγt inverse agonist, demonstrating anti-inflammatory activity through inhibition of IL-17A production in human CD4+ T cells under Th17 differentiation conditions, with an IC50 of 9.6 nM.

ODN 2216 is a TLR9 (toll-like receptor 9) ligand or agonist that induces the production of large amounts of IFN-α and IFN-β. ODN 2216 can induce IFN-α using pDC (plasma cell-like DC) and IL-12 (p40) using DC (dendritic cells). ODN 2216 is capable of indirectly stimulating IFN-γ production by peripheral blood mononuclear cells (PBMC), mediated by IFN-α/β. ODN 2216 activates NK cells and induces IFN-γ production by TCR-triggered CD4+ T cells.

Endogenous APJ receptor agonist that is secreted by adipocytes. Binds with high affinity to APJ receptors (IC50 = 5.4 nM) and potently inhibits cAMP production in vitro (EC50 = 0.52 nM). Involved in regulation of cardiovascular function, fluid homeostasis

Priliximab (CEN 000029), an anti-CD4 humanized monoclonal antibody, binds to CD4 receptors on T cells, leading to a significant and sustained decrease in circulating CD4+ T cells. This property renders it useful in the study of rheumatoid arthritis (RA) [1].

Rp-dGTPαS, an enantiomer of the dNTPαS nucleotide, serves as the substrate for SAMHD1, a critical regulator of cellular dNTP levels that curtails the replication of viruses (HIV-1, etc.) in CD4+ myeloid lineage and resting T cells. The SAMHD1 tetrameric complex facilitates the hydrolysis of Rp-dGQTPαS into 2'-deoxynucleosides and triphosphates [1].

Fostemsavir Tris (BMS-663068 Tris) is the prodrug of BMS-626529,is a oral, safe and effective inhibitor of HIV-1 attachment. It inhibits human immunodeficiency virus type 1 (HIV-1) infection by binding to gp120 and interfering with the attachment of virus to CD4+ T-cells.

Ivuxolimab, an OX40 (also known as CD134; TNFRSF4) agonist monoclonal antibody, targets a costimulatory receptor found on activated CD4+ and CD8+ T cells. It demonstrates antitumor properties and may exhibit immunostimulatory activity [1].

HOXB7 (8-25), a peptide fragment derived from homeobox B7 (HOXB7)—a key controller of cell growth and oncogene activator—facilitates antigen presentation when pulsed onto dendritic cells obtained from human peripheral blood mononuclear cells (PBMCs). This process promotes the activation and interferon-gamma (IFN-γ) production by CD4+ helper T cells, triggering targeted and broad-spectrum antitumor responses.

TPP-1, a peptide inhibitor, targets the interaction between programmed cell death protein 1 (PD-1) and its ligand (PD-L1), binding specifically to PD-L1 with a dissociation constant (Kd) of 94.67 nM. At a concentration of 20 µM, TPP-1 effectively counteracts the PD-L1-induced suppression of IFN-γ production in anti-CD3-stimulated isolated human CD4+ T cells. Furthermore, TPP-1 demonstrates significant efficacy in reducing tumor volume in a mouse xenograft model of HL-60 leukemia. This model involved HL-60 cells co-cultured with anti-CD3-activated isolated human CD4+ T cells, with TPP-1 administration at a dosage of 4 mg/kg showing notable antitumor activity.

Feglymycin is a 13-amino acid peptide originally isolated from Streptomyces that has antibacterial and antiviral activities. It is active against Gram-positive bacteria (MICs = 32-64 μg/ml) and inhibits HIV viral replication in H9 cells (IC50 = ~5 μM). Feglymycin is also active against clinical isolates of HIV-1 from clades A-D, A/E, and G (EC50s = 0.5-6.7 μM). It interacts with gp120 and inhibits HIV-1 NL4.3 binding to human soluble CD4 (EC50 = 4.4 μM) and to CD4+ SupT1 T cells by 74.5% when used at a concentration of 10.5 μM. Feglymycin inhibits the E. coli peptidoglycan biosynthesis enzymes MurA and MurC (Kis = 3.4 and 0.3 μM, respectively) in a noncompetitive manner.

AKP-11 is a sphingosine-1-phosphate receptor 1 (S1P1) agonist with an EC50 of 0.047 μM for [35S]GTPγS binding to CHO-K1 cell membranes expressing human S1P1. It reduces S1P1 surface expression and enhances Akt and ERK phosphorylation in CHO cells with S1P1-HA at a 100 nM concentration. At doses of 1.3 and 3 mg/kg, AKP-11 lowers IFN-γ and IL-17 protein levels in the spinal cord and mitigates disease severity in a rat experimental autoimmune encephalomyelitis (EAE) model. Additionally, it decreases peripheral total lymphocyte and specific T cell subsets (CD4+, CD8+, and CD26L+ T cells) counts in both EAE rats and healthy controls at a 1.3 mg/kg dosage.

Prostratin, a protein kinase C activator, has been shown to exhibit promising therapeutic potential against other diseases such as cancer and Alzheimer's disease. Prostratin has the potential to be useful in the treatment of HIV as it could flush viral re

BDC2.5 mimotope is a potent mimetic antigenic peptide that activates a population of CD4+ T cells sharing the same antigen recognition properties as BDC2.5 cells. This mimotope can be utilized in research for the prevention or treatment of Type 1 diabetes in specific T cell populations.

5J-4 is a potent a blocker of calcium release-activated calcium (CRAC) channel and store-operated calcium entry (SOCE). 5J-4 reduces the production of IL-17 and decreases the expression of RORα and RORγt.