Caspase Activator

Oxidopamine (6-OHDA) hydrobromide is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrobromide is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrobromide promotes COX-2 activation, leading to PGE₂ synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrobromide can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome.

Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.

Oxidopamine (6-OHDA) hydrochloride is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrochloride is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrochloride promotes COX-2 activation, leading to PGE₂ synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrochloride can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome.

Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G₂/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer.

Kanamycin sulfate (Kanamycin A sulfate) is an antibacterial agent. Kanamycin sulfate blocks Kir4.1 channels. Kanamycin sulfate inhibits bacterial mRNA translation and exerts bactericidal effects against Gram-positive, Gram-negative, and acid-resistant microorganisms. Kanamycin sulfate produces ROS and superoxide and induces caspase-3-mediated apoptosis. Kanamycin sulfate inhibits biofilms and reduces persister bacteria, and reduces Mycobacterium tuberculosis within macrophages. Kanamycin sulfate can be used in research on bacterial infections, urinary tract infections, tuberculosis, and Staphylococcus aureus-induced peritonitis.

Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

Raptinal, a agent that directly activates caspase-3, initiates intrinsic pathway caspase-dependent apoptosis. Raptinal is able to rapidly induce cancer cell death by directly activating the effector caspase-3, bypassing the activation of initiator caspase-8 and caspase-9.

Kanamycin (Kanamycin A) is an antibacterial agent. Kanamycin blocks Kir4.1 channels. Kanamycin inhibits bacterial mRNA translation and exerts bactericidal effects against Gram-positive, Gram-negative, and acid-resistant microorganisms. Kanamycin produces ROS and superoxide and induces caspase-3-mediated apoptosis. Kanamycin inhibits biofilms and reduces persister bacteria, and reduces Mycobacterium tuberculosis within macrophages. Kanamycin can be used in research on bacterial infections, urinary tract infections, tuberculosis, and Staphylococcus aureus-induced peritonitis.

Dacomitinib (PF-00299804; PF-299804) is an orally active irreversible pan-ERBB receptor tyrosine kinase inhibitor with inhibitory activity against HER1/EGFR, HER2, and HER4. Dacomitinib exerts antitumor effects in various tumor cells, inhibiting tumor cell proliferation, migration, and invasion, inducing cell cycle arrest and apoptosis, regulating the expression of molecules related to the cell cycle, apoptosis, and epithelial-mesenchymal transition, and it can also reverse partial drug resistance, producing synergistic effects when combined with chemotherapy. Dacomitinib inhibits key signaling pathways such as PI3K‑AKT‑mTOR and PLK1‑FOXM1. Dacomitinib ameliorates pathological changes associated with pulmonary arterial hypertension in rats. Dacomitinib can be used in research on breast cancer, bladder cancer, epithelial ovarian cancer, and pulmonary arterial hypertension.

Milrinone (Win 47203) is a selective PDE3 inhibitor with positive inotropic and vasodilatory effects. Milrinone inhibits cAMP hydrolysis and increases intracellular cAMP and PKA signaling. Milrinone reduces NF-κB, TLR4/MyD88, and NLRP3 inflammasome signaling and pro-inflammatory cytokine production, and has antioxidant and anti-apoptotic effects. Milrinone can be used in research on ischemia/reperfusion injury, sepsis, noise-induced hearing loss, acute lung injury, and Alzheimer's disease.

2-Methoxyestradiol (2-ME2; NSC-659853) is an endogenous steroid metabolite generated from 17β-estradiol, possessing various activities such as antitumor and antiangiogenic effects. 2-Methoxyestradiol competitively binds to the colchicine-binding site of tubulin (tubulin), interfering with microtubule assembly dynamics. 2-Methoxyestradiol inhibits CYP1A1/CYP1B1, HIF-1α/2α, and superoxide dismutase, activates the JNK signaling pathway, elevates ROS levels, and induces cell cycle arrest and apoptosis (apoptosis). 2-Methoxyestradiol is used in cancer-related research, such as breast cancer, prostate cancer, and multiple myeloma.

RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation.

Probucol (DH-581) is an anti-hyperlipidemic agent. Probucol activates glutathione peroxidase. Probucol promotes low density lipoprotein (LDL) catabolism, inhibits ABCA1-dependent cholesterol efflux, and decreases HDL-C levels. Probucol also has anti-inflammatory, antioxidant and neuroprotective properties. Probucol can be used for researches on bone, cardiovascular, cancer, neurological, and metabolism-related diseases.

Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC₅₀s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.

Zenidolol (ICI-118551) is a selective β2-adrenergic receptor antagonist with K_i values of Zenidolol for β2, β1 and β3 adrenergic receptors of 0.7, 49.5 and 611 nM, respectively. Zenidolol exerts antitumor effects via inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway by blocking β2-AR on tumor cells. Zenidolol exhibits a unique pulmonary vessel-specific vasodilatory effect in mouse models. Zenidolol can be used as an intraocular pressure-lowering agent in ophthalmic disease research.

Quinidine (15% dihydroquinidine) is an orally active antiarrhythmic agent. Quinidine (15% dihydroquinidine) reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine (15% dihydroquinidine) exerts sustained block and open-channel block effects on I_K(f). Quinidine (15% dihydroquinidine) alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine (15% dihydroquinidine) can be used in studies related to uterine sarcoma and seizures.

Ginsenoside Rh2 (20(S)-Ginsenoside Rh2) induces the activation of caspase-8 and caspase-9. Ginsenoside Rh2 induces cancer cell apoptosis in a multi-path manner.

Phlorizin (Floridzin) is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC₅₀ of 0.04 μM and a K_i of 39 nM against hSGLT2, and an IC₅₀ of 0.17 μM and a K_i of 0.31 μM against hSGLT1. Phlorizin promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin also exhibits antibacterial, anti-inflammatory and neuroprotective activities.

N1, N11-Diethylnorspermine tetrahydrochloride (DENSPM tetrahydrochloride) is a potent anticancer agent. N1,N11-Diethylnorspermine tetrahydrochloride activates polyamine catabolism and downregulates mTOR protein. N1,N11-Diethylnorspermine tetrahydrochloride induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine tetrahydrochloride kills glioblastoma multiforme (GBM) through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H₂O₂ production.

N-3-oxo-dodecanoyl-L-Homoserine lactone (3-oxo-C12-HSL) is a bacterial quorum-sensing signaling molecule produced by P. aeruginosa and strains of the B. cepacia complex.Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.N-3-oxo-dodecanoyl-L-Homoserine lactone induces the production of IL-8 in 16HBE human bronchial epithelial cells.