Apoptosis Inducer

Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via?p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.

Condurango glycoside A is an activator of p53. Condurango glycoside A initiates ROS generation and up-regulates p53 expression. Condurango glycoside A induces apoptosis and pre-mature senescence associated with DNA damage in HeLa cells.

Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC₅₀=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells.

Diclofenac-¹³C₆ is the ¹³C₆ labeled Diclofenac. Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.

Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft) is a monopegylated IFN-α that can be used for the research of myeloproliferative neoplasms.

MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with K_is of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity.

Conophylline is a vinca alkaloid extracted from leaves of a tropical plant Ervatamia microphylla. Conophylline is a differentiation inducer of for pancreatic cells. Conophylline suppresses HSC and induces apoptosis.

Nitrovin hydrochloride is an antibacterial growth promoter. Nitrovin hydrochloride induces ROS-mediated non-apoptotic and apoptotic-like cell death by targeting TrxR1. Nitrovin hydrochloride has anticancer activity, with IC₅₀ values of 1.31-6.60 μM for tumor and normal cells.

4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis.

(E)-2-Hydroxycinnamaldehyde is an aldehyde that can be separated from the stem bark of cinnamon. (E)-2-Hydroxycinnamaldehyde inhibits cell proliferation and induces apoptosis by inhibiting signal transduction of STAT3 and reactive oxygen species production. (E)-2-Hydroxycinnamaldehyde has antitumor activity.

RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRAS^G12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRAS^G12C mutant, with an IC₅₀ value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRAS^G12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for non-small cell lung cancer (NSCLC) research.

PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC₅₀ of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC₅₀ = 2.74 nM) and PARP2 (IC₅₀ = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer.

Arachidonoyl ethanolamide phosphate, an endocannabinoid, is an endogenous ligand for cannabinoid receptors in the central nervous system (CB1 subtype) and peripheral immune cells (CB2 subtype).

Psalmotoxin 1 (PcTx1) TFA is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 TFA is a potent and slective ASIC1a inhibitor (IC₅₀: 0.9 nM) by increasing the apparent affinity for H⁺ of ASIC1a. Psalmotoxin 1 TFA can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 TFA can be used in the research of cancers, or neurological disease.

FD274 is a highly potent PI3K/mTOR dual inhibitor with IC₅₀s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research.

Bizaxofusp (MDNA55) is a fusion protein formed by the linkage of IL-4 and a truncated Pseudomonas exotoxin. Bizaxofusp can bind to IL-4 receptors on the surface of tumor cells and be internalized, and its exotoxin moiety can inhibit protein synthesis and induce tumor cell apoptosis. Bizaxofusp can be used in the study of cancer.

Thalidomide-piperazine hydrochloride is a synthetic E3 ligase ligand-linker conjugate, comprising a cereblon ligand based on Thalidomide (HY-14658) and one linker. Thalidomide-piperazine hydrochloride can be used in studies related to PROTAC synthesis.

MI-217 is a potent SIRT3 inhibitor. MI-217 induces MDA-MB-231 apoptosis. MI-217 can be used in the study of breast cancer.

Floxuridine (Standard) is the analytical standard of Floxuridine. This product is intended for research and analytical applications. Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.

Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).