pd-l1

PD-1 PD-L1-IN-10 is an orally active PD-1 PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.

PD-1 PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1 PD-L1 interaction. It enhances the immune cells' ability to kill tumor cells and demonstrates significant antitumor activity in vivo in a CT26 mouse model.

PD-1/PD-L1-IN-32 (compound A56) is a potent inhibitor of PD-1/PD-L1, displaying pronounced anticancer activity with an IC50 value of 2.4 nM. It effectively suppresses tumor growth in the hPD-L1 MC38 humanized mouse model and exhibits negligible toxicity to the mice's normal functions [1].

PD-L1-IN-1, a powerful PD-L1 inhibitor, demonstrated an IC50 of 115 nM. By forming a robust bond with the PD-L1 protein, PD-L1-IN-1 effectively suppressed tumor growth by enhancing the antitumor immune activity of peripheral blood mononuclear cells in co-cultures with PD-L1 expressing cancer cells (PC9 and HCC827 cells). It significantly elevated the release of interferon γ and induced apoptosis in cancer cells, while exhibiting minimal cytotoxicity in healthy cells [1].

PD-1/PD-L1-IN-27 is a potent inhibitor of PD-1/PD-L1, exhibiting an IC50 of 134 nM and demonstrating antitumor effects with minimal T cell cytotoxicity. It activates CD8+ T cells and mitigates T cell exhaustion [1].

PD-1/PD-L1-IN-28, an inhibitor of the PD-1/PD-L1 signaling pathway (IC 50 = 0.744 µM), demonstrates promising research potential in tumor immunity. This immune checkpoint inhibitor effectively blocks the interaction within the pathway, offering insights into cancer treatment strategies.

PD-1/PD-L1-IN 3 TFA inhibits the binding of human PD-1 to PD-Ll with an IC50 of 9 nM.

PD-1/PD-L1-IN-33 (Compound N11), a PD-1/PD-L1 inhibitor, effectively impedes the interaction between PD-1 and PD-L1 with an IC50 of 6.3 nM. By doing so, it enhances T-cell proliferation, activation, and infiltration within tumor environments, exhibiting immunomodulatory and anticancer properties [1].

PD-1/PD-L1-IN-31 is a potent inhibitor of PD-1/PD-L1 (IC50=2.2 nM) that enhances IFN-γ secretion and activates the immune response of peripheral blood mononuclear cells (PBMCs), resulting in the inhibition of tumor cells [1].

PD-1/PD-L1-IN-14 (compound 17) is an inhibitor of PD-1/PD-L1 interaction (IC50=27.8 nM). By inhibiting the interaction of PD-1/PD-L1, PD-1/PD-L1-IN-14 promotes dimerization, endocytosis and degradation of PD-L1.

PD-1/PD-L1-IN-17 (Compound P20) is a potent PD-1/PD-L1 inhibitor (IC50: 26.8 nM). PD-1/PD-L1-IN-17 is a promising lead compound for the development of inhibitors of PD-1/PD-L1 interactions. -17 has potential for cancer disease research.

PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, serves as a potent and selective inhibitor of PD-1/PD-L1 interaction. This compound disrupts PD-L1's binding with PD-1 and CD80 by directly binding to PD-L1, exhibiting IC50 values of 5.60 nM and 7.04 nM, respectively. It is utilized in the research of numerous illnesses, such as cancer and infectious diseases [1].

PD-1/PD-L1-IN-26 (Compound II-14) is a potent PD-1/PD-L1 inhibitor, demonstrating an IC50 of 0.0380 μM. It enhances the immune microenvironment by facilitating CD4+ T cell infiltration into tumor tissues, indicating potential use in cancer research [1].

PD-1/PD-L1-IN 5 is a potent PD-1/PD-L1 protein/protein interaction inhibitor (IC50 ≤ 100 nM).

PD-1/PD-L1-IN-22 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interactions that blocks PD-1/PD-L1 interactions (IC50: 0.732 μM). PD-1/PD-L1-IN-22 can be used to study cancer, infectious diseases and autoimmune diseases.

PD-1/PD-L1-IN-20 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-20 blocks the PD-1/PD-L1 interaction (IC50: 5.29 nM). PD-1/PD-L1-IN-20 can be used to study cancer, infectious diseases and autoimmune diseases.

CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, simultaneously inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM). This compound prompts early apoptosis in the fungal cell cycle, markedly diminishes intracellular IL-2, NLRP3, and NF-κBp65 protein concentrations, causes mitochondrial damage and ROS accumulation, and culminates in fungal lysis and cell death [1].

PD-1/PD-L1-IN-23 is a potent, orally active ester prodrug of L7, a benzooxadiazole derivative, and functions as an inhibitor of PD-1/PD-L1. It has been biologically evaluated for its inhibitory effects on PD-L1, demonstrating significant antitumor effects in both syngeneic tumor models and PD-L1 humanized mice.

PD-1/PD-L1-IN-25 is an inhibitor of PD-1/PD-L1 interaction (IC50: 16.17 nM) that effectively activates anti-tumor immunity of T cells in PBMCs. PD-1/PD-L1-IN-25 can be used to study cancer.

PD-1/PD-L1-IN-15 is a potent inhibitor of PD-1/PD-L1 (IC50: 60.1 nM) and has shown investigational potential for tumor immunotherapy.

PD-1/PD-L1-IN-34 (Compound (1S,2S)-A25) effectively inhibits the PD-1/PD-L1 interaction (IC 50 = 0.029 μM) and demonstrates selective binding affinity to PD-L1 (K D = 0.1554 μM), resulting in the activation of the immune microenvironment and suppression of tumor growth [1].

PROTAC PD-1/PD-L1 degrader-1 is a PD-L1 degrading PROTAC that inhibits PD-1/PD-L1 interaction (IC50: 39.2 nM). PROTAC PD-1/PD-L1 degrader-1 restores immunity in Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model of suppressed immunity, which reduces the protein content of PD-L1 in a lysosomal-dependent manner.

PD-1/PD-L1-IN-29 (S4-1) is a potent inhibitor of the PD-1/PD-L1 interaction, with an IC50 value of 6.1 nM. It effectively binds to PD-L1, inhibiting the PD-1/PD-L1 interaction, promotes PD-L1 dimerization and its internalization, enhances localization to the endoplasmic reticulum, and facilitates PD-L1's entry into the endoplasmic reticulum, demonstrating anticancer activity.

PD-1/PD-L1-IN-13 is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM for PD-1/PD- L1 interaction.PD-1/PD-L1-IN-13 promotes CD8+ T-cell activation and delays tumour growth in a Hepa1-6 homozygous mouse model.

PD-1/PD-L1-IN-16 is a potent inhibitor of PD-1/PD-L1 (IC50: 53.2 nM) and has shown research potential for tumour immunotherapy.

PD-1/PD-L1-IN 5 is an inhibitor of PD-1/PD-L1 protein/protein interaction (IC50 of ≤100 nM).

PD-1/PD-L1-IN-30 is a PD-1/PD-L1 binding inhibitor, with an IC 50 value of 0.018 μM. PD-1/PD-L1-IN-30 can be used for research of cancers and other related diseases .

PD-1/PD-L1-IN-NP19, a PD-1/PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1/PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].

PD-1/PD-L1-IN 6 (compound A13) is a potent inhibitor of PD-1/PD-L1 interaction (IC 50 = 132.8 nM). PD-1/PD-L1-IN 6 shows outstanding immunoregulatory activity. In a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion without significant toxic effect. In a T cell-tumor co-culture model, PD-1/PD-L1-IN 6 restores the immune response.

L-Threonine derivative-1 is acetylsalicylic acid-L-threonine ester with potential analgesic activity.

PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor(IC50 of 92.3 nM).

BMS202 hydrochloride (1675203-84-5(free base)) (PD-1/PD-L1 inhibitor 2 hydrochloride) is a small-molecule PD-1/PD-L1 interaction inhibitor (IC50: 18 nM). Biophysical studies demonstrate that BMS202 binds directly to PD-L1. Binding of BMS202 promotes PD-L1 dimerisation and blocks the PD-L1/ PD1 interaction.

(1R,5S,6r)-N-(2-methyl-1-((3-methylpyridin-2-yl)oxy)propan-2-yl)-3-azabicyclo[3.1.0]hexane-6-carboxamide L(+)-Tartaric acid is a potential SSTR4 agonist.

(25R)-3β,17α-dihydroxy-5α- spirostan-6-one3-O-α-L- rhamnopyranosyl-(1→2)-β- D-glucopyranoside is a natural product isolated from the bulbs of Lilium brownii var. viridulum.

PD-1-IN-17 is an inhibitor of programmed cell death-1 (PD-1). PD-1-IN-17 inhibits 92% splenocyte proliferation at 100 nM.

BMS-1 (PD-1/PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) PD-Ll (Programmed death-ligand 1) protein protein interaction.

L-97-1 is an antagonist of the adenosine A1 receptor.

RMP1-14 is an IgG1-like immunoglobulin and anti-Mouse PD-1 antibody that blocks PD-1/PD-L1 signaling.

Anti-Mouse PD-L1 Antibody is a rat-derived IgG2b monoclonal antibody that inhibits mouse PD-L1.

Human PD-L1 inhibitor I is a peptide ligand that specifically inhibits the interaction between human PD-L1 and human PD-1. It exhibits a KD value of 3.39 μM, indicating its binding affinity. The presence of Human PD-L1 inhibitor I disrupts the binding between human PD-L1 and human PD-1, thereby attenuating their respective functions.

PD-L1-IN-3 is a selective and potent PD-1/PD-L1 inhibitor with antitumor activity that blocks PD-1 signaling by preventing PD-1 from binding to PD-L1.PD-L1-IN-3 is used in the study of neoplasms and immune diseases.

Hederagenin 28-O-{β-D-xylopyranosyl-(1→6)-β-D-glucopyranosyl ester}3-O-{α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl} is a saponin known for its antitumor and anti-inflammatory properties [1].

Ophiogenin 3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside (Ophiogenin-3-O-alpha-L-rhaMnopyranosyl-(1->2)-beta-D-glucopyranoside) is a natural product, and has good pharmacological effects on the cardiovascular system.

Borneol 7-O-[beta-D-apiofuranosyl-(1->6)]-beta-D-glucopyranoside is a natural product from Radix ophiopogonis.

Acacetin 7-O-β-D-glucuronopyranosyl-(1→2)[α-L-rhamnopyranosyl-(1→6)]-β-D-glucopyranoside, also known as compound 8, is a flavonoid glycoside isolated from the leaf extract of the black locust (Leguminosae)[1].

Cannogenol 3-O-β-gentiobiosyl-(1→4)-α-L-thevetoside (Compound 12), a cardiac glycoside extracted from Thevetia peruviana seeds, exhibits cytotoxic effects on SW1990 and MGC-803 cells with IC50 values of 9.52 and 7.70 μM, respectively [1].

7-[α-L-Arabinopyranosyl-(1→6)-β-D-glucopyranosyloxy]cuminol, a cuminol glycoside, can be isolated from Rhodiola rosea^[1].

Luteolin-7-O-α-L-arabinopyranosyl-(1→6)-β-D-glucopyranoside, a flavonoid, exhibits antiradical activity [1].

Compound 1, (25R)-Ruscogenin-3-yl α-L-rhamnopyranosyl-(1→2)-[β-D-xylopyranosyl-(1→4)]-β-D-glucopyranoside, is a steroidal saponin that can be isolated from the roots of Ophiopogon japonicus [1].