immunomodulatory agent

Sulindac (Sulindac sulfoxide) is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death.

Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.

Leflunomide (HWA486) is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

Isotretinoin (13-cis-Retinoic acid) binds to and activates nuclear retinoic acid receptors (RARs), which act as transcription factors that promote cell differentiation and apoptosis. This naturally occurring retinoic acid has potential antineoplastic activity, exhibits immunomodulatory and anti-inflammatory responses, and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.

Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN) and is commonly used in the synthesis of PROTAC products.

Synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. Thymopentin (TP5) is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies.

1. Telocinobufagin (Telobufotoxin) is the major endogenous digitalis-like factor. 2. Telocinobufagin significantly decreases the bacterial burdens in the spleen and prolongs the survival time of FIST-immunized mice challenged with live S. typhimurium. 3. Telocinobufagin has immunomodulatory activity, can enhance a Th1 immune response to control intracellular infections, could be developed as a novel immunotherapeutic agent to treat cancer and other immune-mediated diseases.

(R)-AAL is an immunomodulatory agent with an ID50 of 0.009 mg kg for reducing circulating T lymphocytes in rats. It also acts as a substrate for sphingosine kinase (SphK), which catalyzes the phosphorylation of (R)-AAL.

RM 06 is an immunomodulatory agent containing a peptidyl-hypoxanthine structure.

GABAA receptor agent 4 (compound 1e) is a potent antagonist of γ-GABAAR, exhibiting a Ki of 0.18 µM, and demonstrates immunomodulatory potential by effectively rescuing the inhibition of T cell proliferation [1].

Sulindac (sodium) (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac (sodium) is used to reduce pain, swelling, and joint stiffness from arthritis. Sulindac is also used for the research of arthritis of the spine, gouty arthritis. Sulindac (sodium), as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac (sodium) also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1 [1] [2].

Vidofludimus hemicalcium (4sc-101; SC12267) is an orally active compound that acts as a dihydroorotate dehydrogenase (DHODH) inhibitor and serves as a novel modulator of the farnesoid X receptor (FXR). This immunomodulatory agent is utilized in the research of autoimmune disorders, including inflammatory bowel disease (IBD), and is explored for its potential in fatty liver disease research through FXR targeting.

Thymopentin acetate, primarily secreted by the epithelial cells of the thymic cortex and medulla, serves as an effective immunomodulatory agent. It possesses a short plasma half-life of 30 seconds and significantly enhances the generation of T-cell lineage from human embryonic stem cells (hESCs) [1] [2].

IP2, an immunomodulatory agent, enhances PTP (Pioneer Translation Product)-derived antigen presentation in cancer cells without exhibiting cytotoxicity. Additionally, IP2 has been shown to induce tumor growth defects in mouse models [1].

Leflunomide-d4 is a deuterated compound of Leflunomide. Leflunomide has a CAS number of 75706-12-6. Leflunomide is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.

Dimethyl Fumarate-2,3-d2 is a deuterated compound of Dimethyl Fumarate. Dimethyl Fumarate has a CAS number of 624-49-7. Dimethyl fumarate, a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.

Thiotaurine is a metabolite of Cystine. It serves as a sulfur donor and may participate in the activation of neutrophils and leukocyte energy metabolism by regulating the activity of GAPDH. Additionally, Thiotaurine is a potential anti-inflammatory and immunomodulatory agent.

Conalbumin (ovotransferrin) is an egg white protein and glycoprotein with antimicrobial, antioxidant, and immunomodulatory properties as a member of the transferrin and metalloprotease families. Conalbumin has a binding logarithm of 15 for Fe3+ at pH 7 or higher.