Apoptosis Activator 2

MDK83190 (Apoptosis Activator 2) is a potent apoptosis activator, induceing caspase-3 activation, PARP cleavage, and DNA fragmentation .

N-Oleoyl-L-Serine (N-Oleoylserine) is an endogenous long-chain fatty acid amide that is a lipid modulator of bone remodeling and stimulates osteoclast apoptosis which can be used to study osteoporosis. N-Oleoyl-L-Serine showed high activity in an osteoblast proliferation assay.N-Oleoyl-L-Serine promotes osteoclast apoptosis by inhibiting Erk1 2 phosphorylation and expression of nuclear κB ligand (RANKL) receptor activator in bone marrow stromal cells and osteoblasts, which attenuates osteoclast populations.

p53 Activator 7 is a highly potent and cell-permeable activator of the p53 mutation Y220C (MDM-2 p53), which induces apoptosis.

1. Ganoderic acid A exhibits antitumor activity, mediated through its inhibitory effect on nuclear transcription factor-kappaB and activator protein-1. 2. Ganoderic acid A can induce proliferation inhibition, apoptosis and suppression of invasion in human

BSO-07 is a ROS JNK activator that exhibits potent anti-cancer properties, demonstrated by an IC50 of 24.81 μM in human breast cancer (BC) cells. The mechanism of action for BSO-07 involves JNK activation and the promotion of increased ROS levels, which lead to the induction of apoptosis (Apoptosis) and tumorigenic apoptosis. This includes enhanced expression of apoptosis-related proteins such as PARP, Bax, phosphorylated p53, ATF4, and CHOP, along with a reduction in the levels of anti-apoptotic proteins (e.g., Bcl-2, Bcl-xL, and Survivin). BSO-07 holds promise for research in the field of breast cancer.

MIRA-1 (WRN Helicase Inhibitor) is a restorer of wild-type p53 conformation cellular function and selectively inhibits Werner syndrome WRN helicase activity with an IC50 of 20 µM.

Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This compound increases fluorescence by 233% in a SIRT1 activity assay. [Activator activity was defined as the percentage of signal increase relative to signal window in the following formula: 100 x (Sample - Signallow)/(Signalhigh - Signallow)]. CAY10591 suppresses TNF-α in a dose-dependent manner. In THP-1 cells, TNF-α levels decreased from 325 pg/ml (control) to 104 and 53 pg/ml with 20 and 60 µM CAY10591, respectively. This activator also has a significant dose-dependent effect on fat mobilization in differentiated adipocytes, which would indicate the potential of SIRT1 activators for anti-obesity or anti-diabetic purposes.

Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms that effectively induces the translocation of nPKC-delta, -epsilon, and -theta, as well as PKC-mu, from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].

Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor that targets PDE3 to relax airway smooth muscle and is used in asthma and chronic obstructive pulmonary disease (COPD) research. It also functions as an adenosine receptor antagonist, histone deacetylase (HDAC) activator, and exhibits anti-inflammatory activity by increasing IL-10 levels and inhibiting NF-κB nuclear import, while inducing apoptosis [1] [2] [3] [4] [5].

p53 Activator 2 (compound 10ah) intercalates into DNA, causing significant double-strand breaks and upregulating the expression of p53, p-p53, CDK4, and p21, leading to cell cycle arrest at the G2 M phase. It induces apoptosis, reduces anti-apoptosis proteins Bcl-2, Bcl-xL, and cyclin B1 levels, and shows anti-proliferative activity against MGC-803 cells with an IC50 of 1.73 μM. Additionally, p53 Activator 2 exhibits potent anticancer effectiveness in MGC-803 xenograft tumor models [1].

rel-MDM2 4-p53-IN-2 (2q) is a potent dual MDM2 MDM4 inhibitor and p53 activator that acts on both the MDM2-p53 complex (IC50: 70.7 nM) and the MDM4-p53 complex (IC50: 81.4 nM). rel-MDM2 4-p53-IN-2 is capable of regulating cell cycle, induce apoptosis, and exhibit anti-cancer effects.

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

Caspase-3 7 Activator 2 is a potent compound that selectively activates Caspase-3 7, demonstrating tumor specificity, anti-proliferative properties, and a high capacity for inducing apoptosis.

MDM2 4-p53-IN-2 (2q) is a potent dual inhibitor of MDM2 MDM4 and activator of p53, demonstrating IC50 values of 70.7 nM for MDM2-p53 and 81.4 nM for MDM4-p53 complexes. It facilitates cell cycle regulation, promotes apoptosis, and exhibits anticancer properties [1].

Melittin free acid, a basic 26-amino-acid polypeptide, constitutes the primary active component of honeybee venom and serves as a phospholipase A2 (PLA2) activator. Exhibiting a broad-spectrum antifungal effect, it presents MIC values ranging from 0.4-60 μM. Its mechanism includes inducing cell apoptosis, inhibiting (1,3)-β-D-glucan synthase, and engaging in multiple pathways [1] [2].

Caspase-3 Activator 2 (Compound 2f) is a caspase 3 activator with cytotoxic effects on HL-60 and K562 cells, exhibiting IC 50 values of 33.52 μM and 76.90 μM, respectively [1]. It facilitates apoptosis, rendering it useful in cancer research.

TM5441, an orally bioavailable plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 values ranging from 13.9 to 51.1 μM, effectively induces intrinsic apoptosis across multiple human cancer cell lines. Additionally, it mitigates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence [1] [2].

PAWI-2 functions as both a p53 activator and a Wnt inhibitor. It suppresses β3-KRAS signaling independently of KRAS and selectively inhibits the phosphorylation of TBK1. Additionally, PAWI-2 triggers apoptosis (activation of caspase-3 7) and induces PARP cleavage. It facilitates the translocation of retinoblastoma protein into the nucleus, leading to G2 M cell cycle arrest. PAWI-2 reverses the cancer stem cell-like properties of KRAS-dependent human pancreatic cancer stem cells (hPCSC) and overcomes drug resistance. Moreover, it inhibits the growth of hPCSC tumors in an orthotopic xenograft mouse model.

Cucurbitacin D, a triterpenoid isolated from Ecballium elaterium (L.), exhibits anticancer and antitumor activity, inhibits glucose uptake and lactate production in metastatic PrC, and induces inflammasome activation independent of ERK1 2 activation. Cucurbitacin D, a novel inflammasome activator in macrophages, inhibits HepG2 cell proliferation and induces apoptosis by modulating the JAK STAT3, PI3K Akt mTOR and MAPK signaling pathways, and can be used in the study of cervical cancer, leukemia, and prostate cancer.

PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide that acts as a direct activator of Bak with a Kd of 26 nM. PUMA proteins bind Bcl-2, localize to the mitochondria, and induce cytochrome C release and apoptosis in response to p53, potentially mediating p53-induced apoptosis.