immunosuppression

ADH-503 (GB1275) is a potent agonist of the integrin CD11b to mitigate myeloid cell immunosuppression.

Indoximod (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.

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

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Acyclovir (Aciclovir) is a synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses of the herpesvirus family.

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

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.

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

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.

Dargistotug (M-6223) is a fully human IgG1 monoclonal antibody that targets TIGIT (T cell immune receptor with Ig domain and ITIM), an inhibitory immune checkpoint responsible for NK cell depletion and diminished cytokine secretion via interaction with CD155. It also modulates effector T cell activity and increases regulatory T cell (Tregs) function, contributing to immunosuppression [1].

Ziralimumab (ABX-RB2), an anti-human CD147/BSG monoclonal antibody, is employed for immunosuppression [1].

OATD-02 is an orally active, competitive, reversible, noncovalent inhibitor with slow offset kinetics that targets both Arginase1 and 2, exhibiting inhibitory concentrations (IC50) of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1). Notably, OATD-02 mitigates tumor immunosuppression provoked by these arginases and has potential application in melanoma research [1].

VISTA-IN-2 (Compound 1) is a V-domain Ig suppressor of T-cell activation (VISTA) inhibitor that promotes the degradation of VISTA in cells via autophagy, reverses VISTA-related immunosuppression, and fortifies the antitumor responses of immune cells. Additionally, this compound stimulates antitumor immunity and suppresses tumor growth in a CT26 mouse model [1].

Belatacept (BMS 224818) is a selective blocker of T-cell costimulation. Belatacept binds CD 80/86 ligands and thus exhibits an inhibitory effect on CD-28-mediated T-cell costimulation. Belatacept can be used to study organ transplantation immunosuppression.

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.

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.

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

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].

MNF, also known as 3,4-MNF, is an antagonist of the aryl hydrocarbon receptor (AhR). MNF reduces UVR-mediated immunosuppression and induces Tregs in murine contact hypersensitivity (CHS).

Protosappanin A (PTA) has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

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].

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.

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

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.

JTE-607 is a cytokine production inhibitor. JTE-607 induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells.