Apoptose

Ac-Trp-Glu-His-Asp-Aldehyde is a powerful and selective inhibitor of caspase-1, demonstrating a K_i value of 56 pM [1] [2].

PROTACPI3Kδ degrader-1 is a covalent PI3Kδ-targeting PROTAC degrader that targets lysine, with a DC50 of 3.98 nM. It exhibits potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). Additionally, PROTACPI3Kδ degrader-1 effectively degrades p-AKT, induces cell cycle arrest in the G1 phase, and promotes apoptosis and autophagy. It also significantly suppresses tumor growth in the SU-DHL-6 xenograft mouse model.

Thujopsene, a sesquiterpene found in T. dolabrata, exhibits a wide range of biological activities. It inhibits Na+/K+-ATPase and cytochrome P450 (CYP) isoform CYP2B6 with IC50 values of 25.9 µg/ml and Ki of 0.8 µM, respectively. Additionally, thujopsene demonstrates antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, such as S. aureus, M. luteus, and S. typhimurium, with MICs ranging from 25-50 µg/ml. It also suppresses antigen-induced β-hexosaminidase release in IgE-sensitized RBL-2H3 mast cells (IC50= 25.1 µM) and shows cytotoxicity against A549 non-small cell lung cancer cells with an LC50 of 35.27 µg/ml. Furthermore, thujopsene causes mortality in mites D. farinae and T. putrescentiae, with LC50s of 9.82 and 10.92 µg/cm2, respectively.

IBI-325 is a humanized monoclonal antibody inhibitor targeting CD73. It completely inhibits CD73 enzymatic activity without causing a hook effect. IBI-325 can reverse adenosine monophosphate-mediated immunosuppression and significantly inhibits T cell proliferation and the release of cytokines (IL-2, IFN-γ, and TNF-α). In both hPBMC-reconstituted mouse models and hCD73 knock-in mouse models, IBI-325 demonstrates potent antitumor activity. This compound is applicable for cancer immunotherapy research.

SB-T-1214 (SBT) is a taxane-based drug known for its ability to effectively suppress the expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induce apoptosis in drug-resistant tumorigenic CD133+/CD44+ colon cancer spheroids. In Pgp+ DLD-1 human colon tumor xenograft mouse models, SB-T-1214 successfully inhibits tumor growth. This compound is relevant for anti-tumor research, particularly against drug-resistant tumors such as colon, pancreatic, and renal cancers.

dASK1-VHL is an orally active PROTAC degrader targeting ASK1. It effectively binds to VHL, promoting the selective degradation of ASK1. By reducing ASK1 protein levels, dASK1-VHL inhibits the activation of p38 MAPK and decreases liver lipid content, offering new insights for MASH research.

1R,3R-RSL3 is a negative control for1S, 3R-RSL3.

M7GpppAmpG is a trinucleotide 5′ cap analog, exhibiting capping efficiencies of 90% for the produced RNAs [1].

PD-1/PD-L1-IN-40 (Compound EP16) is a PD-1/PD-L1 inhibitor. It effectively suppresses the production of exosomal PD-L1 with an IC50 of 0.108 μM. PD-1/PD-L1-IN-40 serves as a lead compound for the elimination of exosomal PD-L1 and is applicable in cancer research.

Apo A-I mimetic 5A peptide is a synthetic peptide molecule designed based on the structure and function of naturally occurring apolipoprotein A-I (Apo A-I). It facilitates the efflux of cholesterol from inside cells, helping to reduce intracellular cholesterol accumulation. Additionally, Apo A-I mimetic 5A peptide exhibits anti-inflammatory properties, lowering inflammatory markers in blood and tissues. This peptide is used in cardiovascular disease research.

PZ671 is a potent PROTAC degrader targeting Bcl-xL, exhibiting an IC50 of 1.3 nM in MOLT-4 cells and a DC50 of 0.9 nM for Bcl-xL. It induces apoptosis in MOLT-4 cells and effectively inhibits tumor growth in MOLT-4 xenograft mice, while quickly restoring transiently reduced platelet counts. PZ671 is applicable in cancer research, including studies on small cell lung cancer.

BAT-1306 is a human monoclonal antibody (mAb) targeting PDCD1/PD-1/CD279. It is applicable for research in colorectal cancer and solid tumors.

TTQ-SA is a near-infrared spiraling aggregation-induced emitter capable of converting near-infrared light (NIR) into thermal energy, resulting in thermal damage and death of tumor cells. In cancer cells MF-7, TTQ-SA shows cell uptake and targeting capabilities. TTQ-SA binds with DNAzyme to inhibit the expression of the survivin gene, enhancing the sensitivity of tumor cells to photothermal therapy.

CGP-74514,CDK1 inhibitor (IC50=25 nM). Induces G2/M arrest, apoptosis. Used in bladder cancer research.

DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]

VEGFR-2-IN-61 (Compound 7b) is an inhibitor of VEGFR-2 with an IC50 of 2.83 µM. It effectively inhibits the proliferation of various cancer cells, including MCF-7 cells, with an IC50 of 2.12 µM. Additionally, VEGFR-2-IN-61 suppresses cell migration and induces oxidative stress and apoptosis in MCF-7 cells.

VTX-0811 is a human IgG4 monoclonal antibody (mAb) that targets PSGL1/CD162. It modulates immune signaling pathways by enhancing TNF-α/NF-κB and chemokine-mediated signaling while reducing oxidative phosphorylation, fatty acid metabolism, and Myc signaling. VTX-0811 increases the proportion of CD8+ T cells among infiltrating T cells and exhibits antitumor activity in humanized mouse PDX models of melanoma.

Obestatin (human) is an endogenous ligand for G-protein eurythmic entity 39 formed by shearing of preproghrelin and can be used to study obesity.

GLPG4970 is a potent, selective, orally active dual inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3), with IC50 values of 0.3 nM and 0.7 nM, respectively. It exhibits weak inhibition of the hERG channel, with an IC50 value of 29 μM. GLPG4970 reduces the release of tumor necrosis factor α (TNFα) and increases the release of interleukin 10 (IL-10). This compound is applicable for research in inflammation and immunology, such as studies on colitis.

(GalNAc)3-CPT is a glycan-conjugated prodrug that targets the asialoglycoprotein receptor (ASGR) overexpressed on liver cells. It demonstrates significant antitumor activity by activating the cGAS-STING pathway and promoting CD8+ T cell infiltration into tumor sites, leading to apoptosis of tumor cells. In HepG2 cells, it shows an IC50 value of 3.07 μM.