immunosuppression

Acyclovir (Aciclovir) is a guanine analog and orally active antiviral agent characterized by a narrow antiviral spectrum, high selectivity, and low toxicity. Acyclovir exhibits activity against HSV-1 (IC50 = 0.85 μM), HSV-2 (IC50 = 0.86 μM), and varicella-zoster virus. Acyclovir can be used for herpesvirus treatment research.

Genipin ((+)-Genipin), an active aglycone derived from an iridoid glycoside called geniposide, is found in the fruit of Gardenia jasminoides Ellis.

B7/CD28 interaction inhibitor 1 (CTLA-4 inhibitor) is a potent CTLA-4 inhibitor.

CD73-IN-3 (LY-3475070) is a potent and selective CD73 inhibitor with an IC50 of 28 nM, and its use alone or in combination with pembrolizumab is currently being tested in patients with advanced cancer.

cis-Urocanic acid ((E)-Urocanic acid) is a 5-HT2A receptor agonist (Kd: 4.6 nM). It is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a reversible inhibitor of arginase with anti-leukemic activity, effective in treating endothelial dysfunction, immunosuppression, and metabolism regulation.

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

Indoximod (NLG-8189) is a methylated tryptophan with immune checkpoint inhibitory activity. Indoximod inhibits the enzyme indoleamine 2, 3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy.

HPK1-IN-58 is an inhibitor of HPK1 (IC50: 2.6 nM) and SLP76 (IC50: 20 nM). It enhances IL-2 secretion, thereby reversing PGE2-induced immunosuppression. HPK1-IN-58 is applicable for research in antitumor immunity.

A2AR modulator-1 (Compound 45) is a selective negative allosteric modulator of the adenosine A2a receptor (A2aR), with an IC50 value of 9 nM. It reduces the affinity of endogenous adenosine for the receptor and inhibits the activation of the cAMP signaling pathway. A2AR modulator-1 effectively restores pCREB phosphorylation in CD4+ T cells, reverses immunosuppression in the tumor microenvironment, and shows potential in inhibiting tumor growth and metastasis in a triple-negative breast cancer model.

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.

1-(1-Naphthyl)piperazine is a modulator of 5-HT receptors, acting both as a 5-HT2A receptor antagonist and a 5-HT1A receptor agonist, with a human 5-HT6 receptor binding constant (Ki) of 120 nM. It partially inhibits forskolin-stimulated adenylate cyclase activity in bovine substantia nigra and can suppress UV radiation-induced immunosuppression. Additionally, 1-(1-Naphthyl)piperazine induces S-phase cell cycle delay, apoptosis, and increases reactive oxygen species (ROS) levels, leading to the inhibition of MNT-1 cell proliferation. This compound is utilized in melanoma research.

NP1192 is a potent and selective PROTAC NAT10 degrader that reduces NAT10 protein expression in cancer cells and inhibits ac4C modification. It disrupts the NAT10/HIF-1α/PD-L1 axis, leading to dual suppression of hypoxia-driven glycolysis and immunosuppression, demonstrating significant antitumor efficacy both in vitro and in vivo, and producing synergistic effects when combined with anti-PD-L1 treatment. NP1192 is applicable for research in ovarian cancer, cervical cancer, and glioblastoma.

SRX3207 is an inhibitor of Syk and PI3K and relieves tumor immunosuppression.

Scoparone (Aesculetin dimethyl ether) can be found in a number of food items such as sweet orange, wild celery, mandarin orange (clementine, tangerine), and lemon. It is found in the Chinese herb Artemisia scoparia and has been studied for its potential pharmacological properties including immunosuppression and vasorelaxation. Scoparone is found in anise. Scoparone is found in several citrus oils.

BMS-243117 is an effective selective LCK inhibitor with good cell activity (IC(50)=1.1 microM) and inhibition of T cell proliferation, which has great potential for therapeutic immunosuppression and the treatment of diseases such as rheumatoid arthritis a

eIF4E-IN-1 (WO2021003194A1, compound Y), is a highly effective inhibitor of eIF4E, a key protein involved in immunosuppression. By targeting immune checkpoint proteins such as PD-1, PD-L1, LAG3, TIM3, and IDO, eIF4E-IN-1 functions to disrupt immune suppression and promote immune release in specific diseases such as cancer and infectious diseases.

CD73-IN-10 can be used in preparing tumor-related diseases medicament. CD73-IN-10 is a potent CD73 inhibitor that can catalyze the adenosine production from extracellular 5'-phosphate adenosine (5'-AMP). Adenosine induces immunosuppression and can promote tumor proliferation and/or metastasis [1].

CD73-IN-11 is able to used for tumor-related diseases medicament preparing. CD73-IN-11 is an effective CD73 inhibitor. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP) which induce immunosuppression and promote tumor proliferation and/or metastasis [1].

BMS-566419 is an acridone-based inhibitor of inosine 5'-monophosphate dehydrogenase, a rate-limiting enzyme in de novo guanosine nucleotide biosynthesis, and through suppression of lymphocyte proliferation it has demonstrated clinical utility as a research compound for investigating immunosuppression mechanisms and therapeutic strategies in transplant rejection.

OP-5244 sodium is a potent, orally active inhibitor of CD73 (IC50: 0.25 nM). OP-5244 sodium has shown potential for cancer research by blocking adenosine production and thereby reversing immunosuppression.

Belatacept (BMS 224818) is a selective blocker of T-cell costimulation that binds to CD 80/86 ligands, inhibiting CD-28-mediated T-cell activation. It is useful for studying immunosuppression in organ transplantation.

Inupadenant, also known as EOS-850, is a highly selective small molecule antagonist of the adenosine A2a receptor, in the adenosine triphosphate adenosine pathway, a key driver of immunosuppression in the tumor microenvironment across a broad range of tumors.

MNF is a specific aryl hydrocarbon receptor (AhR) antagonist that effectively inhibits TCDD-induced AhR signaling pathway activation, attenuates TCDD-induced activation of downstream signaling molecules Akt and Erk1/2 and TGFα expression, and reverses the anti-apoptotic effect of TCDD. It is commonly used in research on AhR-related functions and signaling pathways.