Apoptosis

Ara-SH, a derivative of Cytarabine with a mercaptopropionic acid substitution, serves as the initiator for the self-assembly of a smart, co-loaded Cytarabine

6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study

Trametinib (GSK1120212), an ATP-noncompetitive MEK 1/2 inhibitor (IC50: 0.7/0.9 nM), weakly inhibits >180 kinases.

Dubermatinib (TP0903) is a potent and selective Axl kinase inhibitor.

The test principle applied in this kit is Sandwich enzyme immunoassay. The microtiter plate provided in this kit has been pre-coated with an antibody specific to Rat Smad2. Standards or samples are added to the appropriate microtiter plate wells then with a biotin-conjugated antibody specific to Rat Smad2. Next, Avidin conjugated to Horseradish Peroxidase (HRP) is added to each microplate well and incubated. After TMB substrate solution is added, only those wells that contain Rat Smad2, biotin-conjugated antibody and enzyme-conjugated Avidin will exhibit a change in color. The enzyme-substrate reaction is terminated by the addition of sulphuric acid solution and the color change is measured spectrophotometrically at a wavelength of 450nm ± 10nm. The concentration of Rat Smad2 in the samples is then determined by comparing the OD of the samples to the standard curve.

LQB-118, an orally active compound sourced from sandalwood, demonstrates multiple therapeutic capabilities. It has shown proficiency in inhibiting glioblastoma cell migration and inducing apoptosis. Additionally, LQB-118 can curtail both migration and invasion of prostate cancer cells by modulating the AKT/GSK3β pathway and regulating MMP-9/reck gene expression. The compound is also effective against yeast polysaccharide-induced inflammation in both in vivo and in vitro settings. Notably, LQB-118 specifically triggers ROS-mediated and mitochondrial-dependent apoptosis in Leishmania amazonensis, highlighting its potential in studies focusing on inflammation, infections, and various cancers.

Phytosphingosine: anticancer phospholipid; triggers apoptosis in cancer cells via caspase 8 activation and Bax translocation.

SJ-172550 is a small molecule inhibitor of MDMX (EC50: 5 μM).

PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor, isoform-specific mutants at Ser773, and potently inhibits DNA-PK with IC50 of 2 nM in cell-free assay.

Macitentan (ACT-064992) is an endothelin receptor antagonist that is used in the therapy of pulmonary arterial hypertension (PAH).

Poziotinib (NOV120101)(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM).

Floxuridine (FUDR) is an antimetabolite, floxuridine inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity.

Hederacoside D is a bioactive saponins from Hedera helix.

TW-37 is an nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 (Ki: 0.29/1.11/0.26 μM).

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM.

Apoptosisinducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, demonstrating antitumor activity by causing significant morphological changes, such as membrane blebbing, nuclear fragmentation, and apoptotic body formation, in MDA-MB-231 cells. The IC50 values for Apoptosisinducer 32 are 4.77 μM in MCF-7 cells, 6.56 μM in MDA-MB-231 cells, and 337.8 μM in HEK cells.

HA14-1, a Bcl-2/Bcl-XL antagonist, is a non-peptidic ligand of a Bcl-2 surface pocket (IC50: ~9 μM).

EA, a natural triterpene, is found in herbs; it has anti-inflammatory and antioxidant properties.

YUM70 inhibits GRP78 (IC50: 1.5μM), inducing ER stress and apoptosis in pancreatic cancer.