Apoptosi

HFY-4A is a novel HDAC inhibitor.HFY-4A has antitumour activity and has shown antiproliferative activity in breast cancer cells.

<p>CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.</p>

<p>Compound 6b is a synthetic Thalidomide-VHL E3 ligase-linker for PROTACs.</p>

<p>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.</p>

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

<p>Tilogotamab (GEN-1029) is an agonistic hexameric complex targeting two independent epitopes on DR5, used for studying multiple myeloma (MM).</p>

<p>POV-PC is an oxidized phospholipid that inhibits VSMC growth under high serum conditions and induces cell apoptosis under low serum conditions.</p>

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

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

<p>KHKI-01215 is a NUAK2 inhibitor with anticancer activity, inhibiting the proliferation of SW480 cancer cells and inducing apoptosis.</p>

<p>H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC/D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.</p>

<p>SDU-071 is a BRD4-p53 inhibitor, suppressing MDA-MB-231 cell proliferation, inducing cell cycle arrest and apoptosis.</p>

<p>Z-VDVA-(DL-Asp)-FMK is a derivative compound of Z-VDVAD-FMK specifically designed as an inhibitor targeting caspase-2.</p>

<p>Thalidomide-O-amido-C6-NH2 is a synthetic E3 ligase used for PROTAC creation, containing cereblon ligand and linker.</p>

<p>NS3694 is an inhibitor of apoptosis and inhibits apoptosome formation and caspase activation.</p>

<p>LH1307 blocks PD-1/PD-L1 interaction, IC50 = 3 nM (HTRF assay), activates Jurkat cells, EC50s: 79 nM (U2OS), 763 nM (CHO).</p>

<p>FF2039 (compound 1j) is a PROTAC degrader specifically targeting HDAC1, HDAC6, and various subtypes of class I, IIa, and IIb HDACs. It induces cell cycle arrest and apoptosis, showing significant antiproliferative activity against both hematological and solid tumor cell lines. The IC50 values for FF2039 against HDAC1, HDAC2, HDAC4, and HDAC6 are 1.03, 2.15, 12.4, and 0.053 μM, respectively. FF2039 exhibits antiproliferative effects on solid tumors such as MM.1S, MDA-MB-231, and U-87MG, with EC50 values of 2.8, 28, and 30 μM, respectively.</p>

<p>UBX1325, a potent Bcl-xL inhibitor, induces cell death in aging cells, useful for age-related eye disease research.</p>

<p>Flu-BakBH3 peptide, derived from Bak's BH3 domain, binds tightly to a crucial pocket of Bcl-XL, essential for its anti-death role.</p>

<p>Thalidomide-NH-C8-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand and a specific linker.</p>