pd1in24

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

Dynorphin A (1-10) acetate is an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.

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).

Cholesterol 24-hydroxylase-IN-1 is an orally active, selective, and potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) that crosses the blood-brain barrier.Cholesterol 24-hydroxylase-IN-1 may be useful in the study of epilepsy-like neurological disorders. Cholesterol 24-hydroxylase-IN-1 is used to study epilepsy-like neurological diseases.

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.

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.

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

C24 dihydro 1-Deoxyceramide (m18:0/24:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C24 dihydro 1-Deoxyceramide (m18:0/24:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found in mouse brain, spinal cord, and sciatic nerve at one, three, and six months of age.4 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemical structure of native 1-deoxysphingosine. J. Lipid Res. 57(7), 1194-1203 (2016).|2. Alecu, I., Othman, A., Penno, A., et al. Cytotoxic 1-deoxysphingolipids are metabolized by a cytochrome P450-dependent pathway. J. Lipid Res. 58(1), 60-71 (2017).|3. Alecu, I., Tedeschi, A., Behler, N., et al. Localization of 1-deoxysphingolipids to mitochondria induces mitochondrial dysfunction. J. Lipid. Res. 58(1), 42-59 (2017).|4. Schwartz, N.U., Mileva, I., Gurevich, M., et al. Quantifying 1-deoxydihydroceramides and 1-deoxyceramides in mouse nervous system tissue. Prostaglandins Other Lipid Mediat. 141, 40-48 (2019).

Ponatinib, also known as PonatiLink-1-24, is a selective inhibitor of the Abelson murine leukemia (ABL) enzyme [1].

Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds in the transmembrane domain of the κ-receptor.

PD-1-IN-24 (compound 1) is an orally active PD-1 inhibitor.

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-IN-17 TFA is a potent inhibitor of programmed cell death-1 (PD-1), inhibiting 92% of splenocyte proliferation at a concentration of 100 nM.

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.

Josiphos SL-J009-1 Pd G3 has a wide range of applications in life science related research.

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

C24:1 3'-sulfo Galactosylceramide (d18:1 24:1(15Z)) is the predominant sulfate analog in the mature myelin sheath. C24:1 3'-sulfo Galactosylceramide (d18:1 24:1(15Z)) interacted with C-type lectin and immunoglobulin-like receptors to give the highest affinity for LMIR5. Galactosylceramide (d18:1 24:1(15Z)) induces MCP-1 production by basophils, which activates NFAT by increasing LMIR5, but not mast cells .C24:1 3'-sulfo Galactosylceramide (d18:1 24:1(15Z)) binds in vitro to CD1d binding and increased the proliferation of free mouse splenocytes.

PD-1-IN-20 is the less active enantiomer of PD-1-IN-1.

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.

Sintilimab (IBI308) is a humanized IgG4 monoclonal antibody with significant anti-tumor activity that restores endogenous anti-tumor T-cell responses by binding to PD-1 and thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2).Sintilimab is used in combination with other compounds for the treatment of classical Hodgkin's lymphoma, non-cellular lung cancer and esophageal cancer. Sintilimab is used in combination with other compounds to treat classical Hodgkin's lymphoma, non-small cell lung cancer and esophageal cancer.

Gonadotropin-Releasing Hormone-Associated Peptide (GAP) (1-24), human, also known as hGAP-1-24, is the 1-24 fragment of the human GAP, which is connected to the luteinizing hormone-releasing hormone (LH-RH) through a 3 amino acid processing site [1].

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.

(Des-His^6)-ACTH (1-24) (human, bovine, rat) is an adrenocorticotropic hormone (ACTH) analog. Produced by the anterior pituitary gland, ACTH is a polypeptide tropic hormone that regulates the production of cortisol and androgens [1].

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-IN-18 is a PD1 inhibitor of signaling pathway, and acts as an immunomodulator.

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-IN-17 TFA is a inhibitor of programmed cell death-1 (PD-1) .

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 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.

HIV-1 inhibitor-24 (compound S-12a) is a potent inhibitor of HIV-1 reverse transcription (HIV-1 RT) (IC50: 9.5 nM). HIV-1 inhibitor-24 exhibits a high antiviral effect on wild-type HIV-1 with an EC50 value of 1.6 nM and low cytotoxicity (CC50 on MT-4 cells). HIV-1 inhibitor-24 was well tolerated in mice at a dose of 2 g/kg and had a significant cardiovascular safety profile.

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 .

Brain Derived Basic Fibroblast Growth Factor (1-24) (FGF basic 1-24), a synthetic peptide, exhibits anti-bacterial and anti-HBV properties, finding application in infectious and immune disease research [1].