Apoptosis Activator

Tolinapant (ASTX660) is an orally active cIAP1/2 and XIAP antagonist, with an IC₅₀ of < 40 nM against XIAP and an IC₅₀ of <12 nM against cIAP1. Tolinapant triggers TNFα-dependent Apoptosis in cancer cells. Tolinapant inhibits tumor growth in mouse xenograft models. Tolinapant can be used in research related to breast cancer, melanoma, lymphoma, multiple myeloma, acute lymphoblastic leukemia and advanced solid tumors.

Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects.

Licochalcone B is an extract from the root of Glycyrrhiza uralensis. Licochalcone B inhibits amyloid β (₄₂) self-aggregation (IC₅₀=2.16 μM) and disaggregate pre-formed Aβ₄₂ fibrils, reduce metal-induced Aβ₄₂ aggregation through chelating metal ionsLicochalcone B inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone B inhibits growth and induces apoptosis of NSCLC cells. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction.

Levonorgestrel is an orally active inhibitor of progesterone (HY-N0437). Levonorgestrel has anticancer activity and can induce Apoptosis. Levonorgestrel can be used as a contraceptive and in combination with other medications. Levonorgestrel can be used in the study of osteoporosis and uterine leiomyoma.

Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19.

BV02 is a 14-3-3 inhibitor and an antibacterial agent. BV02 enhances the cleavage of PARP and caspase-3. BV02 induces Apoptosis, Autophagy, and enhances Akt activation. BV02 has anti-B. melitensis infection and epilepsy-promoting effects. BV02 can also be used in colitis research.

Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models.

Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC₅₀s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

1,2-DLPC (1,2-Dilauroyl-sn-glycero-3-phosphocholine) is a ligand for LRH-1 agonists. 1,2-DLPC is a phospholipid used in the synthesis of liposomes. 1,2-DLPC enhances fat breakdown and apoptosis in fat cells through a TNFα-dependent pathway, while also inhibiting palmitate-induced insulin resistance through PPARα-mediated inflammation in muscle cells.

Neladalkib (NVL-655) is an oral ALK inhibitor, the IC₅₀ for Neladalkib in inhibiting ALK is 2.8 nM. Neladalkib promotes cell apoptosis and has anti-tumor activity.

Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis.

Geraniol is an olefin terpene with oral activity. Geraniol inhibits cell proliferation and promotes apoptosis. Geraniol has antibacterial, antifungal, antioxidant, anti-inflammatory and antitumor activities. Geraniol can be used to study diabetes.

TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats.

Ethyl methanesulfonate is an orally active biochemical agent. Ethyl methanesulfonate induces Apoptosis. Ethyl methanesulfonate acts on DNA, alkylating it and causing changes in DNA structure, which in turn triggers a series of biological effects such as mutation and cell death. Ethyl methanesulfonate induces kidney and nervous system tumors. Ethyl methanesulfonate is widely used in the field of genetic toxicology research and is often used to induce gene mutations in organisms to study gene function, the mechanism of genetic diseases, and the effects of environmental mutagenic factors, etc.

N6-Cyclopentyladenosine (CPA) is a selective Adenosine A₁ receptor agonist, with K_i values of 2.3 nM, 790 nM and 43 nM for human A₁, A_2A and A₃ receptors, respectively. N6-cyclopentyladenosine increases Apoptosis. N6-Cyclopentyladenosine has antitumor activity against leukemia. N6-cyclopentyladenosine improves 5-fluorouracil (HY-90006)-induced hematopoietic damage, regulates sleep, and delays Aminophylline-induced clonic epileptic seizures.

Oxcarbazepine is a sodium channel blocker. Oxcarbazepine significantly inhibits glioblastoma cell growth and induces apoptosis or G2/M arrest in glioblastoma cell lines. Anti-cancer and anticonvulsant effects.

Subtilisin (EC 3.4.21.14) is a bacterial serine protease. Subtilisin induces Apoptosis. Subtilisin stimulates the expression of pro-allergic cytokines (IL-1α, IL-33). Subtilisin induces prototypic allergic lung inflammation. Subtilisin exhibits anticancer activity against breast and colon cancer. Subtilisin shows antifouling activity. Subtilisin can be used as a detergent additive.

STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.

Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium (18:1 Lyso-PS) is a modified PS product generated following NADPH oxidase activation and Lyso-PS signal transduction. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium signals through macrophage G2A to enhance the phagocytic uptake of PS-dependent apoptotic (apoptosis) neutrophils and PS-exposed activated neutrophils. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium enhances macrophage phagocytic uptake of apoptotic cells, carboxylate-modified microspheres, and PS-exposed non-apoptotic activated neutrophils. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium serves as an acyl acceptor substrate for the lysophosphatidyltransferase At1g78690p to generate diacylphosphatidylserine. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium reduces the secretion of IL-8 and decreases the proportion of viable colon cancer cells. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium is applicable to studies on peritonitis and inflammatory bowel disease.