Apoptosi

MDMX/MDM2-IN-2 is a potent dual inhibitor of p53-MDM2/MDMX, demonstrating dissociation constants (Kis) of 0.23 μM for MDM2 and 2.45 μM for MDMX.

CGP 3466B (Omigapil) is an oral drug inhibiting GAPDH nitrosylation and apoptosis, potentially treating Alzheimer's and CMD.

BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2].

CAY10726, an arylurea fatty acid, cuts ATP by 28% and promotes apoptosis in breast cancer cells by depleting mitochondrial lipids.

Pipernonaline is a useful organic compound for research related to life sciences. The catalog number is T124000 and the CAS number is 88660-10-0.

eIF4E-IN-2 effectively inhibits eIF4e, crucial for research on diseases like cancer.

Photosensitizer-3, generates single-linear oxygen upon near-infrared light excitation in combination with FAP,potent and selective killing cancer cells.

UCM-1336 (3,3′-(Octylimino)bis[N-phenylpropanamide]) is a potent ICMT inhibitor with an IC50 of 2 μM which is selective against the other enzymes involved in

Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties.

RO7567132 is a bispecific antibody that binds and agonizes LTBR bivalently while binds and antagonizes FAP monovalently, inducing the formation of local TLS.

Baceridin, a cyclic hexapeptide and proteasome inhibitor, can be isolated from the culture medium of Epiphytic Bacillus.

TQB-2858 is a bifunctional fusion protein composed of an anti-PD-L1 monoclonal antibody fused with the extracellular domain of the TGF-β receptor. It exhibits high affinity for PD-L1, TGF-β1, and TGF-β3, and demonstrates a high target occupancy rate for PD-L1. TQB-2858 can be used in research on osteosarcoma and alveolar soft part sarcoma (ASPS).

Thalidomide-O-C7-acid: A cereblon ligand from Thalidomide linked via a PROTAC-used linker.

EGCG-4″-sulfate, a predominant polyphenol in green tea, demonstrates notable anticancer, antioxidant, and anti-inflammatory effects, particularly against

DAPK Substrate Peptide is a synthetic peptide substrate for death-associated protein kinase (DAPK) (Km = 9 μM).

PROTAC AR Degrader-8 (Compound NP18) functions as a PROTAC degrader targeting the androgen receptor (AR) and effectively degrades AR-FL in both 22Rv1 and LNCaP cells with DC50 values of 0.018 μM and 0.14 μM, respectively. It also degrades AR-V7 in 22Rv1 cells with a DC50 of 0.026 μM. Additionally, PROTAC AR Degrader-8 inhibits the proliferation of 22Rv1 and LNCaP cancer cells, exhibiting IC50 values of 0.038 μM and 1.11 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in 22Rv1 cells (apoptosis). Demonstrating anticancer efficacy, PROTAC AR Degrader-8 shows activity in both mouse and zebrafish models. [Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon]

VEGFR2/HDAC1-IN-1 (compound 13) is a potent dual inhibitor of VEGFR-2 and HDAC, with IC50 values of 57.83 nM for VEGFR-2 and 9.82 nM for HDAC.

HQY1428 is an orally active CDK12 inhibitor. It impedes DNA replication, causing cell cycle arrest at the G2/M phase in SKOV3 cells, and induces DNA double-strand breaks as well as apoptosis. In the SKOV3 xenograft mouse model, HQY1428 demonstrates antitumor activity. Additionally, when combined with the HER2 inhibitor Lapatinib in the NCI-N87 xenograft mouse model, HQY1428 produces a synergistic therapeutic effect.

Gemcitabine monophosphate disodium salt is a monophosphate derivative of Gemcitabine.

Isoharringtonine, an alkaloid from Cephalotaxus koreana, inhibits and induces apoptosis in cancer cells.

(+)-Mcl-1 inhibitor 22 (Example 37) is an MCL-1 inhibitor that impedes the anti-apoptotic function of MCL-1 by blocking its interaction with pro-apoptotic proteins. It demonstrates antiproliferative activity against various cancer cell lines and is applicable for cancer research.

Pamlectabart is a humanised antibody targeting TNFRSF17/BCMA, (ADC) Pamlectabart tismanitin multiple myeloma.

DB0614 degrades 26 kinases including AAK1 and CDK6, targeting aberrant activity in disease research.

Nrf2 activator 19 is a compound capable of crossing the blood-brain barrier and acts as an NRF2/HO-1 activator, offering potent antioxidant and neuroprotective effects. It effectively reduces brain damage and minimizes the accumulation of Reactive Oxygen Species (ROS). Additionally, Nrf2 activator 19 inhibits neuronal apoptosis, aiding in the recovery of neural function and motor skills. It has demonstrated significant potential in ischemic stroke research.

Waltonitone is a natural ursane-type pentacyclic triterpene isolated from Gentian waltonii Burkill.

Enniatin complex: fungal cyclohexadepsipeptides inhibit enzymes, induce cancer cell apoptosis, and have ionophoric, antibiotic, and hypolipidemic effects.

Ferroptosis-IN-13 (compound NY-26) is an inhibitor of ferroptosis. It effectively suppresses RSL3-induced ferroptosis in 786-O cells, with an EC50 value of 62 nM.

Compound 25b, an FPR1 antagonist, exhibits potent inhibition of the formyl peptide receptor 1 with an IC50 of 70 nM.

Ferroptosis-IN-16 (Compound 13l) acts as a specific inhibitor of ferroptosis, demonstrating EC50 values of 0.7 nM in ES-2 cells and 0.9 nM in LX-2 cells. It effectively alleviates acute liver injury induced by Acetaminophen in mouse models and shows excellent metabolic stability in mouse liver microsomes.

Eucalyptol, a natural monoterpenoid and cyclic ether found in eucalyptus species, effectively controls excessive airway mucus secretion and asthma by inhibiting pro-inflammatory cytokines. It serves as an efficacious treatment for non-purulent sinusitis, reducing inflammation and pain when applied topically, and demonstrating leukemic cell-killing capabilities in vitro.

BCL6-IN-6 is an inhibitor of Bcl-6 and can be used in studies about diffuse large B-cell lymphoma.

VK-28 is a brain permeable iron chelator with neuroprotection. VK-28 inhibits basal as well as iron-induced mitochondrial lipid peroxidation.

Cereblon ligand for PROTAC R&D; has E3 ligase, alkylC1-PEG3-alkylC3 linker, terminal amine. Part of Arvinas-licensed tool molecules.

CST626 is a PROTAC degrader that targets XIAP, cIAP1, and cIAP2.

CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.

The compound is a negative control peptide for the Bax inhibitor peptides V5 and P5.

Compound 6b is a synthetic Thalidomide-VHL E3 ligase-linker for PROTACs.

PPIA-IN-1 (Compound 20b) is an inhibitor of peptidyl-prolyl isomerase A (PPIA) with a KD of 0.52 μM. It demonstrates antiproliferative activity across various cancer cell lines, including an IC50 of 0.69 μM in HCT116 cells, induces cell cycle arrest at the G0/G1 phase, and exhibits antimetastatic effects in HCT116 cells. PPIA-IN-1 elevates ROS levels, causing DNA damage, ER stress, and mitochondrial dysfunction, and induces apoptosis in HCT116 cells via the MAPK pathway. Additionally, PPIA-IN-1 shows antitumor activity in a CT26 xenograft mouse model.

2,4,6-trichloroanisole inhibits the cell viability of CHO and C32 cell lines and apoptosis, antibacterial activity against Plasmodium falciparum.

Thalidomide-derived cereblon ligand linked to a PROTAC technology linker, Thalidomide-O-amido-C3-NH2, is a synthetic E3 ligase ligand-linker.

Thalidomide-O-amido-C4-N3 (Cereblon Ligand-Linker Conjugates 4) is an E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and

Mcl-1 Inhibitor 16 (Compound 9), a platinum-based mitochondrial-targeting agent, inhibits Mcl-1 and induces Bax/Bak-dependent apoptosis in cancer cells.

Zalypsis, a transcription factor inhibitor, is used potentially for the treatment of lymphoma, and cervical carcinoma.

Tubulin/MMP-IN-3 (Compound 15j) is a dual inhibitor of tubulin polymerization and MMP, effectively inhibiting MMP-2 and MMP-9 with IC50 values of 21.13 μM and 19.24 μM, respectively. It disrupts the NF-κB signaling pathway, leading to mitochondrial dysfunction and mitochondrial-dependent apoptosis. Tubulin/MMP-IN-3 shows antiproliferative activity in various cancer cells by causing cell cycle arrest at the G2/M phase and demonstrates antitumor effects in mouse models.

EGFR-IN-86 (compound 4i), an EGFR inhibitor (IC50: 1.5 nM), demonstrates potent activity against glioblastoma by inducing apoptosis and causing G2/M phase cell

Apoptolidin, from Nocardiopsis, induces apoptosis, targets mitochondrial ATPase (Ki 4-5 μM), kills glial cells, and has antibiotic and antifungal properties.

CIB-1476, a caspase-1 inhibitor, effectively reduces joint swelling in mouse models of arthritis and demonstrates lasting anti-inflammatory effects. This compound achieves its benefits by blocking IL-1β production, NF-κB activation, and GSDMD-mediated pyroptosis, all of which are triggered by the NLRP3 inflammasome.