Apoptosis Inducer

Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC₅₀ of 8 µM) and primary CML cells (IC₅₀ of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis^[3.

PI-103 is a potent PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.

4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a K_d of 25 μM against eIF4E binding.

Piceatannol is a well-known Syk inhibitor and reduces the expression of iNOS induced by TNF. Piceatannol is an effective agent for research of acute lung injury (ALI). Piceatannol is a naturally occurring polyphenolic stilbene found in various fruits and vegetables and exhibits anticancer and anti-inflammatory properties. Piceatannol induces apoptosis in DLBCL cell lines. Piceatannol induces autophagy and apoptosis in MOLT-4 human leukemia cells.

Dexrazoxane, as an intracellular iron chelating agent, reduces the formation of superoxide radicals and has cardioprotective, anti-inflammatory, antioxidant, anti-tumor and neuroprotective activities. Dexrazoxane inhibits ferroptosis of H9c2 cells by inhibiting HMGB1. Dexrazoxane induces DNA damage and apoptosis in human fibrosarcoma cells .

Hyperoside is a NF-κB inhibitor, found from Hypericum monogynum. Hyperoside shows anti-tumor, antifungal, anti-inflammatory, anti-viral, and anti-oxidative activities, and can induce apoptosis.

Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis.

Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52. Alemtuzumab does not cross-react with murine CD52. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes. Alemtuzumab is capable of complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity (ADCC), as well as induction of apoptosis. Alemtuzumab has the potential for B-cell chronic lymphocytic leukaemia research.

ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC₅₀s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis.

BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC₅₀ of 10 μM.

BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC₅₀ of 100 nM in a cell-free assay.

S-Adenosyl-L-methionine (S-Adenosyl methionine) tosylate is an orally active methyl group donor. S-Adenosyl-L-methionine tosylate is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine tosylate also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine tosylate has the potential for, cancer, liver disease and osteoarthritis research.

Cu(II)-Elesclomol is a complex formed by Elesclomol (HY-12040) and Cu²⁺ (copper ions). Cu(II)-Elesclomol is also a weak inhibitor of DNA topoisomerase I. Cu(II)-Elesclomol exerts anticancer effects by inducing oxidative stress and DNA damage through copper chelation. Cu(II)-Elesclomol can inhibit tumor cell proliferation and induce cell cycle arrest and apoptosis. Cu(II)-Elesclomol can be used in the study of cancer.

Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC₅₀=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC₉₀=37 nM). Zotatifin induces cell apoptosis.

Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).

Pyridinium bisretinoid A2E (A2E) TFA is a fluorophore that can be isolated from lipofuscin in the retinal pigment epithelium (RPE). Pyridinium bisretinoid A2E TFA is an initiator of blue-light-induced apoptosis. Photoactivation of Pyridinium bisretinoid A2E TFA mediates autophagy and the production of reactive oxygen species. Pyridinium bisretinoid A2E TFA can be used in the study of retinal degenerative diseases.

7,8-Dihydroxyflavone is a potent and selective TrkB agonist that mimics the physiological actions of Brain-derived neurotrophic factor (BDNF). Displays therapeutic efficacy toward various neurological diseases.

Cirtociclib (BLU-222) is an orally active and highly selective CDK2 inhibitor. Cirtociclib disrupts Rb signaling and causes G1 arrest and apoptosis in CCNE1-amplified endometrial cancer cells.

EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a K_d of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions. EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.