Apoptosi

PDE4B-IN-4 is an inhibitor of PDE4B (IC50: 2.82 nM) and TNF-α (IC50: 7.20 nM). It demonstrates anti-inflammatory properties by reducing neutrophilia in a mouse model of lipopolysaccharide (LPS)-induced sepsis.

Compound Ir5 (Antitumor agent-145) serves as a tumor inhibitor characterized by significant fluorescence and mitochondrial targeting. It promotes anti-cancer activity by inducing necroptosis and stimulating the necroptosis-related immune response [1].

RLX HCl is anticancer, inhibits tumour proliferation by suppressing the PI3K/Akt/FoxO3a in experimental colon cancer, antiproliferative.

PD-L1inhibitory peptide is an inhibitor peptide that targets the programmed cell death ligand 1 (PD-L1). By binding to PD-L1, it lifts immune suppression and restores the anti-tumor activity of T cells. PD-L1inhibitory peptide holds promise for use in tumor research.

Cot inhibitor-1 hydrochloride blocks TPL-2 kinase (IC50=28nM) and TNF-α synthesis (IC50=5.7nM) in human blood.

PBE-AMF is a prodrug that activates H2O2 and exhibits anticancer activity. It impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing cell death (apoptosis), and blocking the cell cycle. PBE-AMF effectively and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells.

Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].

Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.

d-(KLAKLAK)2 is an antimicrobial and antitumor peptide, notable within the group of antimicrobial peptides, and exhibits strong anticancer properties. It kills bacteria by disrupting their cell membranes, causing leakage of cell contents. Additionally, d-(KLAKLAK)2 inhibits tumor cell proliferation by inducing apoptosis through mitochondrial swelling and membrane damage.

C-Peptide 1 (rat) is a polypeptide isolated from proinsulin. C-Peptide acts as a β-catenin/GSK-3β activator, influences Na/K-ATPase, regulates apoptosis.

PD-L1-IN-5 (X22) is an orally active PD-L1 inhibitor with an IC50 of 785.6 nM, demonstrating antitumor activity in vivo.

RIPK1-IN-13 (compound 28) is a selective inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), showing a pKi of 7.66 as measured by the ADP-Glo kinase assay. It exhibits inhibitory effects in human leukemia U937 cells with a pIC50 of 7.2.

TopoisomeraseII inhibitor 17 (compound 4c) is a thiazolopyrimidine-based inhibitor of Topoisomerase II with an IC50 of 0.23 μM. This compound significantly disrupts the cell cycle and induces apoptosis.

LZFPN-90 (LZ90) is a dual-target compound aimed at NAMPT and PD-L1. It inhibits the interaction between PD-1/PD-L1 and NAMPT activity. LZFPN-90 suppresses cell growth in a NAMPT-dependent manner, blocking the cell cycle and subsequently inducing apoptosis. Additionally, LZFPN-90 exhibits target-dependent antitumor activity, impacting metabolic processes and the immune system.

Anticanceragent 204 (Compound 6) is a fluorinated derivative of cinnamamides with anticancer activity. It can arrest the cell cycle of HepG2 cells in the G1 phase and induces apoptosis by reducing mitochondrial membrane polarization (MMP) levels.

Antitumor agent-170 (Compound C6) inhibits PD-1/PD-L1 interaction and PARP7 with IC50 values of 0.342 μM and 7.05 nM, respectively. It shows high affinity for human PD-L1, with a Ki of 9.31 nM, and can restore T cell function while increasing IFN-γ secretion. In mouse models, Antitumor agent-170 exhibits antitumor effects against melanoma and demonstrates favorable pharmacokinetic properties.

Thalidomide-N-C3-O-C4-O-C3-OH is a conjugate of an E3 ligase ligand and a linker, used in the synthesis of the Aster-APROTAC degrader.

EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. It exhibits antiproliferative activity, effectively inhibiting the proliferation of H1975 cells and inducing apoptosis (apoptosis). EGFR-IN-107 is applicable in cancer research.

Cu(I) chelator 1 (Compound LH2) is a chelating agent specifically targeting the Cu(I) redox state. It inhibits the production of ROS.

P-gp inhibitor 16 (compound 14) is an inhibitor of p-glycoprotein. It significantly enhances apoptosis induced by doxorubicin and displays anticancer properties.

Pacmilimab (CX-072) is a Probody immune checkpoint inhibitor targeting programmed death ligand 1 (PD-L1) with anti-tumor activity for the study of solid tumors.

C188, a naphthol-based STAT3 inhibitor, blocks IL-6-induced STAT3 activity in HepG2 cells, sparing STAT1.

Trimebutine (Mebutin) is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid

(E/Z)-LAQ824 is an inhibitor of histone deacetylase.

Isorhamnetin 3-glucuronide is a useful organic compound for research related to life sciences and the catalog number is T124938.

Phosphocreatine dipotassium, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives.

YJ1206 is a highly potent and selective CDK12/13 PROTAC degrader oral, DNA damage and cell-cycle arrest,and inhibits the proliferation of prostate cancer cells.

SC-2001 inhibits MCL-1 and STAT3, enhances SHP-1, induces apoptosis in breast cancer, and counters STAT3-driven sorafenib resistance in liver cancer.

Albicanol is a biochemical.

Ceftiofur hydrochloride (U-67279A) is a stable, broad-spectrum 3rd-gen cephalosporin with antibacterial properties.

RET-IN-28 (Compound 16) is an inhibitor of RET (a transmembrane receptor tyrosine kinase). It specifically inhibits the activity of a mutant RET enzyme (RET-V804M) and is utilized in cancer research.

TopoisomeraseI/II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.

Taltirelin acetate (TA-0910 acetate) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R)(IC50 of 910 nM and EC50 of 36 nM for stimulating an

Ferroptosis-IN-14 (compund 36) exhibits the most potent anti-ferroptotic activity with an EC50 value of 0.58 ± 0.02 μM, demonstrating excellent anti-ferroptotic efficacy, as well as stability in microsomes and plasma.

Ac-IEPD-AFC (IEPD) is a fluorescent substrate for granzyme B and can be used to measure granzyme B activity.

KC01 selectively inhibits ABHD16A (IC50: 0.2-0.5 μM), much more potent than KC02 (>10 μM); human ABHD16A IC50: 90±20 nM.

Tralokinumab: human IgG4 monoclonal antibody, blocks IL-13, may treat atopic dermatitis.

5α-dihydro Levonorgestrel is a metabolite of the synthetic progestin levonorgestrel .

Tyroserleutide HCl, a tripeptide from pig spleen, inhibits tumor growth in vivo/vitro.

Cytotoxic and antiproliferative effects of Hellebrin on breast and lung cancer cells.

Boc-D-FMK is an irreversible, cell-permeable, and broad-spectrum caspase inhibitor and inhibits apoptosis stimulated by TNF-α (IC50: 39 μM).

ATWLPPRAANLLMAAS is a chimeric peptide with anti-angiogenic and potent antitumor capabilities. It effectively inhibits the proliferation, viability, migration, and invasion of human hepatocellular carcinoma cells, and induces apoptosis (apoptosis).

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and

Human TNF alpha (46-65) peptide.

IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug that suppresses IDO expression. It induces apoptosis, reduces mitochondrial membrane potential, and inhibits tumor cell migration and invasion. Additionally, IDOi-Pt(IV) prodrug-1 triggers reactive oxygen species-mediated endoplasmic reticulum stress and the secretion of damage-associated molecular patterns (DAMPs), leading to immunogenic cell death (ICD). Compared to cisplatin, IDOi-Pt(IV) prodrug-1 exhibits relatively high efficiency and low toxicity in its antitumor activity.

ERK1/2 inhibitor 13 (Compound 21y) is an orally bioavailable ERK inhibitor that targets ERK1 and ERK2, with IC50 values of 91.71 nM and 97.87 nM, respectively. It effectively suppresses the proliferation of cancer cell lines MCF-7, 4T1, MDA-MB-468, and HCC1970 with IC50 values of 0.67 μM, 2.76 μM, 2.15 μM, and 1.68 μM, respectively. Additionally, it inhibits cancer cell migration, induces apoptosis and autophagy in MCF-7 cells, and demonstrates anti-tumor and anti-metastatic effects in a 4T1 xenograft mouse model.

β-ESA, a polyunsaturated fatty acid in seed oils, inhibits Caco-2 cell growth dose- and time-dependently.