Apoptosis

PG-11047 2HCl treats genitourinary, immune, genetic, ocular, blood/lymphatic disorders, and aids lymphoma/prostate cancer research.

hMcl-1-IN-1 (Compound 9) is an hMcl-1 inhibitor based on a His224 arylsulfonyl fluoride, displaying an IC50 value of 5.8 nM.

β-Apopicropodophyllin, a natural product isolated from Hyptis wticillata, promotes apoptosis through mechanisms including microtubule disruption, DNA damage,

CPD-10 is a potent bifunctional PROTAC degrader targeting CCND1 and CDK4 and exhibits antiproliferative effects. It induces apoptosis and reduces the protein expression of Cyclin D1, Cyclin D3, CDK4, and P-Rb(5807/811) in a dose-dependent manner.

TPP-resveratrol is a conjugate of Resveratrol and triphenylphosphine (TPP), noted for its anticancer activity. This compound enhances the efficacy of Resveratrol by facilitating its targeted delivery to mitochondria, thus inducing mitochondrial-mediated cell apoptosis (apoptosis).

Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM.

AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity.

HNPMI is an epidermal growth factor receptor inhibitor that promotes apoptosis and is used in the study of colorectal cancer.

Daporinad hydrochloride (FK 866 hydrochloride) is a NAMPT inhibitor with antitumor and antiangiogenic activity that induces apoptosis in tumor cells.

Chol-CTPP targets the BBB and glioma cells; when combined with Chol-TPP, forms Lip-CTPP, enhancing anti-glioma drug efficacy.

HEMTAC CDK4/6 degrader 1, a PROTAC targeting HSP90/CDK4/6, Kd of 35.7 μM, disrupts B16F10 melanoma cell cycle, and induces apoptosis.

BMH-7 HCl is a p53 activator, showing anti-cancer activity by activating the p53 pathway.

Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) is a proton pump inhibitor drug, used for short-term treatment of erosion and ulceration of the esophagus

Delmitide, a TNF-alpha production inhibitor, is used potentially for the treatment of Crohn's disease and ulcerative colitis.

AZT triphosphate TFA, a Zidovudine metabolite, inhibits HIV & HBV replication and triggers mitochondrial apoptosis.

Mofarotene (Ro-40-8757) is a small molecule compound that shows considerable antitumor activity in many cancer cell lines and can be used for the treatment of

Mcl-1 Inhibitor 12 (Example 10), with a K i of 0.22 nM, functions as an MCL-1 inhibitor. It is utilized in cancer research [1].

Amino-PEG6-Thalidomide is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules.

Thalidomide-NH-PEG8-Ts: a synthesized Thalidomide-PEG8 E3 ligase linker for PROTAC-mediated IDO1 degradation.

Ganoderic acid Mf: antitumor triterpenoid, arrests G1 cell cycle, selective for cancer cells, triggers apoptosis via mitochondria.

Malformin A, from A. niger, is a plant growth regulator and has anti-TMV and cancer cell cytotoxic properties. Intraperitoneal LD50 in mice is 3.1 mg/kg.

Aviculin, a lignan glycoside, exhibits anticancer properties by inducing apoptosis in breast cancer cells with an IC50 of 75.47 μM.

Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC that links Pomalidomide and Dovitinib via a CRBN connector, exhibiting potent antiproliferative activity in

Calcimycin hemimagnesium is an antibiotic, ionophore, and ATPase inhibitor that boosts intracellular Ca2+, causing cell death and apoptosis.

Thalidomide-NH-PEG4-COOH is a E3 ligase ligand-linker for synthesizing the selective degrader dCBP-1 targeting p300/CBP.

HJC0416 hydrochloride: potent oral STAT3 inhibitor, better anticancer effects than Stattic, promising for breast cancer research.

Thalidomide-Piperazine-PEG2-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand with a PEG2 linker.

Bcl-2-IN-2 is a highly potent and selective inhibitor targeting Bcl-2 and Bcl-xL.

Anticancer Agent 153 (Compound 3) promotes apoptosis through the generation of Reactive Oxygen Species (ROS) and elevates the loss of Mitochondrial Membrane

PROTAC Bcl-xL degrader-1 targets Bcl-xL & IAP E3 ligases, degrades Bcl-xL, toxic to human platelets & MyLa 1929 (IC50: 62 nM, 8.5 μM).

VB-85247 is a STING agonist that, by activating the STING pathway, induces the upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as the maturation and activation of dendritic cells. It can lead to the regression of tumors within the bladder and is applicable in bladder cancer research.

L-threo-PPMP blocks GlcT, curbs glycosphingolipid creation, and triggers cell death, showing anti-cancer effects.

CIB-1476, a caspase-1 inhibitor, effectively reduces joint swelling in mouse models of arthritis and demonstrates lasting anti-inflammatory effects. This compound achieves its benefits by blocking IL-1β production, NF-κB activation, and GSDMD-mediated pyroptosis, all of which are triggered by the NLRP3 inflammasome.

PD-1/PD-L1 inhibitory peptide C8 disrupts the PD-1/PD-L1 interaction, leading to the activation of CD8+ and CD4+ T cells and an increase in IFN-γ secretion. In mouse models, PD-1/PD-L1 inhibitory peptide C8 has demonstrated antitumor activity.

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].

TOFA-Plasmalogen (compound 1), a derivative of glyceraldehyde, exhibits ferroptosis-inducing properties. This compound promotes lipid peroxidation in cell membranes, leading to cytotoxic effects with an inhibition concentration (IC 50 = 32.87 μM).

TAT-NEP1-40 TFA, a blood-brain barrier-permeable peptide, safeguards PC12 cells against oxygen and glucose deprivation (OGD) and fosters neurite outgrowth.

anti-TNBC agent-1 targets TNBC effectively, with IC50 of 0.20-0.27 μM, inducing apoptosis and G1 arrest in SUM-159 cells.

NOD1/2-IN-1 (Compound 18) is a potent RIPK2 inhibitor, demonstrating an IC50 value of 1.4 nM in the ADP-Glo assay. It blocks the production of pro-inflammatory cytokines by inhibiting the NOD1/NOD2 pathway (IC50 values are 18 nM and 170 nM for NOD1 and NOD2, respectively), thereby reducing inflammatory responses. This compound is utilized in research related to colitis.

ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.

4-Nitrothalidomide is a modified form of thalidomide that inhibits the growth and proliferation of HUVEC cells and is commonly used in the synthesis of pomalidomide, which has anticancer potential.

Calphostin C is a protein kinase C inhibitor.

PD-L1 ligand 1 is classified as a PROTAC-targeted protein ligand, primarily utilized as a degradation agent for PD-L1.

Ac-LEHD-AMC, a fluorogenic caspase-9 substrate, releases fluorescent AMC upon cleavage, aiding caspase-9 activity measurement.

H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC/D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.