PD-1/PD-L1 Inhibitor

BMS-8 inhibits the PD-1/PD-L1 interaction with IC₅₀ of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1.

PD-L1 inhibitory peptide TFA is an inhibitor targeting the PD-1/PD-L1 interaction. PD-L1 inhibitory peptide TFA inhibits the PD-1-mediated apoptosis signaling pathway, maintains the survival and activity of T cells, activates the anti-tumor effect of cytotoxic T lymphocytes, and significantly improves the survival rate of mice in fungal sepsis models. PD-L1 inhibitory peptide TFA can be used for research on sepsis, breast cancer and other related diseases, as well as immunotherapy.

TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (K_D=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function.

Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) is a recombinant chimeric version of the original 10F.9G2 antibody (HY-P99145). The variable domain sequences are identical to the original 10F.9G2 but the constant region sequences have been switched from rat IgG2b to mouse IgG2a. Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) contains a LALA-PG mutation in the Fc fragment rendering it unable to bind to endogenous Fcγ receptors. Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) blocks PD-1 signaling. Anti-Mouse PD-L1/B7-H1 (LALA-PG) Antibody (10F.9G2) can be used for the research of cancer.

PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC₅₀ of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.

Sugemalimab is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb). Sugemalimab shows anticancer activities and can be used for non-small cell lung cancer research.

PD-1/PD-L1-IN-14 (compound 17) is a bifunctional inhibitor of PD-1/PD-L1 interactions, with an IC₅₀ of 27.8 nM. PD-1/PD-L1-IN-14 (compound 17) inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1.

Palverafusp alfa (IMM-2510; SYN-2510) is a PD-L1/VEGF-targeting IgG1κ type humanized antibody. Palverafusp alfa blocks PD-1/PD-L1 binding, relieves immune suppression, mediates PD-L1-directed antibody-dependent cellular cytotoxicity (ADCC). Palverafusp alfa blocks VEGF/VEGFR binding, inhibits angiogenic signaling, relieves VEGF-induced immune suppression. Palverafusp alfa reduces endothelial cell proliferation, enhances ADCC and antibody-dependent cellular phagocytosis (ADCP), inhibits tumor growth, reverses T cell immune suppression. Palverafusp alfa exhibits immune stimulatory, antiangiogenic, and anti-tumor activity in the tumor microenvironment. Palverafusp alfa can be used for the research of cancer, such as solid tumors, non-small cell lung cancer.

BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC₅₀ value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM.

1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with K_i of 0.007 μM. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid is the Inhibitor for PD-1/PD-L1.

(R)-JQ-1 carboxylic acid, is an isomer of JQ-1 carboxylic acid (HY-78695). JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.

Anti-Canine PD-L1/B7-H1 Antibody (JC071) is an anti-canine PD-L1/B7-H1 IgG1 monoclonal antibody. Anti-Canine PD-L1/B7-H1 Antibody (JC071) can specifically bind to CHO-PDL1 cells and K562-cCD20-cPD-L1 cells. Anti-Canine PD-L1/B7-H1 Antibody (JC071) can enhance the level of IFN-γ. Anti-Canine PD-L1/B7-H1 Antibody (JC071) is often used in western blot experiments.

Anti-Mouse/Human phosphorylated PD-1/CD279 Antibody (407.6G12) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to mouse/human phosphorylated PD-1/CD279. Anti-Mouse/Human phosphorylated PD-1/CD279 Antibody (407.6G12) can detect the phosphorylated form of the PD-1 ITSM by both western blot and flow cytometry.

[D-Leu-4]-OB3 inhibits expressions of pro-inflammatory, proliferative and metastatic genes and PD-L1 expression. [D-Leu-4]-OB3 stimulates expression of pro-apoptotic genes.

PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC₅₀ of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer.

LY3415244 is a bispecific antibody that targets and inhibits TIM-3 and PD-L1. LY3415244 blocks the interaction between TIM-3 on immune cells and PD-L1 on the surface of tumor cells, establishes intercellular connections between TIM-3-positive immune cells and PD-L1-positive tumor cells, and blocks dual immunosuppressive signals. LY3415244 alleviates T cell exhaustion and restores T cell proliferation. LY3415244 induces broad-spectrum anti-drug antibodies, which impairs the binding capacity to soluble TIM-3 targets. LY3415244 can be used in research related to various advanced solid tumors.

MDX-1105 is a human antibody expressed in CHO that targets B7-H1/PD-L1/CD274. MDX-1105 has a huIgG4SP type heavy chain, and its predicted molecular weight (MW) is 150 kDa. The isotype control for MDX-1105 can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).

NSC622608 is a V-domain Ig suppressor of T-cell activation (VISTA) ligand with an IC₅₀ value of 4.8 μM.

BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC₅₀ of 7.68 nM. BMSpep-57 binds to PD-L1 with K_ds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs.

ASC-69 (APY69)is a potent and promising?PD-1/PD-L1 small-molecule inhibitor.