Apoptose

<p>Apoptosis inducer37 (Derivative 10) is an agent that induces apoptosis and exhibits anticancer properties by causing cell cycle arrest at the S-G2/M phase and promoting cell apoptosis. It significantly inhibits HCT116, SKOV3, and HepG2 cancer cells with IC50 values of 24.98 μM, 26.15 μM, and 23.09 μM, respectively. Apoptosis inducer37 demonstrates antitumor activity and can be utilized in ovarian cancer research.</p>

<p>ROCK/HDAC-IN-2 (Compound C-9) is a dual inhibitor of ROCK/HDAC, characterized by IC50 values of 0.185 µM for HDAC6, 0.8 µM for ROCK1, and 0.7 µM for ROCK2. It effectively induces apoptosis and mitochondrial membrane potential alterations in cancer cells and demonstrates notable antitumor activity, making it useful for research in pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).</p>

<p>PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.</p>

<p>2,5-Dimethylcyclohexa-2,5-diene-1,4-dione inhibits the viability of HL60 and K562 cells and exhibits antibacterial and anticancer properties.</p>

<p>TAS-117, a PKB/Akt inhibitor, is used potentially for the treatment of solid tumors.</p>

<p>DB2313 is a potent PU.1 inhibitor (IC50=14 nM) that disrupts gene binding, induces AML cell apoptosis, and has anticancer properties.</p>

<p>ElteN378: potently inhibits FKBP12 (Ki=0.5 nM), low weight, similar affinity to Rapamycin.</p>

<p>BRD4 Inhibitor-39 (compound 12m) is an orally active inhibitor of BRD4 with an IC50 of 0.02 μM. It can induce apoptosis and demonstrates antitumor activity.</p>

<p>MRIA9 inhibits SIK1/2/3 &amp; PAK2/3 with IC50: SIK1 (516 nM), SIK2 (180 nM), SIK3 (127 nM); ATP-competitive.</p>

<p>PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)</p>

<p>EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.</p>

<p>MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.</p>

<p>Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active inhibitor of tubulin polymerization. It acts at the colchicine binding site to inhibit tubulin polymerization with an IC50 value of 2.505 μM, effectively disrupting the intracellular microtubule network and interfering with mitosis. Tubulin polymerization-IN-76 shows significant inhibitory effects on MGC-803 and HGC-27 cells, with IC50 values of 1.61 and 1.82 nM, respectively. It effectively suppresses colony formation and cell migration activities in these cell lines, inducing G2/M phase cell cycle arrest and apoptosis (Apoptosis). Furthermore, Tubulin polymerization-IN-76 exhibits broad-spectrum antiproliferative activity.</p>

<p>RETligand-3 is the ligand for PROTAC QZ2135, which targets RET.</p>

<p>TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, showing significant antiproliferative activity. It can induce G1 phase cell cycle arrest and apoptosis (with notable increases in early and late apoptosis rates) and is useful for research in cancers such as colon, breast, and liver cancer.</p>

<p>10-SLF is a PROTAC FKBP12 degrader. It facilitates the formation of a ternary complex between FKBP12 and FBXW7-R465C, leading to the proteasomal degradation of FKBP12 in a FBXW7-R465C-dependent manner. 10-SLF selectively reduces FKBP12 levels in cells that express FBXW7-R465C.</p>

<p>cis-Clovamide is a naturally occurring phenolic compound with noteworthy antioxidant, anti-inflammatory, and antiapoptotic properties.</p>

<p>Src Inhibitor4 (Compound 18) is a derivative of KX-01 and functions as a Src inhibitor. It effectively disrupts tumor cells, damages microtubules, and induces cell cycle arrest, apoptosis, and immunogenic cell death. After introducing phenol or aniline functional groups, Src Inhibitor4 serves as a payload conjugation site for antibody-drug conjugates, showcasing antitumor activity.</p>

<p>GL392 is a senolytic agent that delivers the potent senescence-clearing compound Dasatinib specifically to senescent cells. By targeting the LBD domain, it binds lipofuscin in these cells and releases Dasatinib via an ester linkage, inducing apoptosis (Apoptosis) in senescent cells. Additionally, GL392 is encapsulated in PEO-b-PCL microcapsules to ensure efficient intracellular delivery while minimizing systemic toxicity. GL392 is applicable in cancer research.</p>

<p>Type-I/-II Photosensitizer-1 (compound 8b) is a photosensitizer with anticancer properties. It exhibits significant phototoxicity against A549 and 4T1 tumor cells. Under laser irradiation, Type-I/-II Photosensitizer-1 demonstrates strong oxygen-independent antitumor activity with an IC50 ranging from 1.50 to 1.76 μM.</p>

<p>MALT1-IN-13 (compound 10m) is an inhibitor of the mucosa-associated lymphoid tissue lymphoma translocation protein (MALT1), forming a covalent and irreversible bond with the MALT1 protease, thereby inhibiting its activity with an IC50 of 1.7 μM. It suppresses the proliferation of ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1 cells. Additionally, MALT1-IN-13 regulates the mTOR and PI3K-Akt pathways.</p>

<p>FMP is a platinum (IV) complex. It significantly upregulates the expression of γ-H2AX and p53, enhances ROS production, and markedly increases the expression of apoptosis (Apoptosis) related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP exhibits antiproliferative activity against breast cancer.</p>

<p>Compound A6, a potent PROTAC HDAC6 degrader, has a DC50 of 3.5 nM and induces apoptosis in myeloid leukemia cells.</p>

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

<p>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.</p>

<p>PROTACSMARCA2/4 degrader-38 is a SMARCA2/4 PROTAC degrader with DC50 values of 3.0 nM and 4.0 nM, respectively. It facilitates the ubiquitination and degradation of SMARCA2/4 and can block the G0/G1 phase of the cell cycle, leading to the induction of apoptosis. PROTACSMARCA2/4 degrader-38 is applicable in acute myeloid leukemia (AML) research.</p>

<p>MS78, an acetylation targeting chimera (AceTAC), specifically acetylates the p53Y220C mutant by recruiting the histone acetyltransferase p300/CBP.</p>

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

<p>Thalidomide-O-PEG2-propargyl is a cereblon-based E3 ligase ligand with a PEG linker for PROTAC-induced protein degradation.</p>

<p>Moracin N, a ferroptosis inhibitor derived from mulberry leaves, exhibits neuroprotective activity by mitigating oxidative stress [1].</p>

<p>Eldecalcitol, orally active vitamin D analog, boosts bone density and treats osteoporosis.</p>

<p>Curzerene, a sesquiterpene compound derived from the rhizome of Curculigo orchioides Gaertn, possesses potent anti-cancer properties.</p>

<p>RET-IN-4: Oral RET inhibitor, IC50 ~1 nM for variants. Selective over JAK2/FLT3. Potent anticancer use.</p>

<p>PROTACKDM4 degrader-1 (Compound 11) is a proteolysis-targeting chimera (PROTAC) degrader specifically designed for KDM4. It effectively degrades KDM4A-C while sparing KDM4D. In esophageal cancer cells, PROTACKDM4 degrader-1 demonstrates strong antiproliferative activity, inducing apoptosis and cell cycle arrest, and inhibits lysine demethylation of histone H3.</p>

<p>Anti-TNBC agent-9 (Compound 3as) is an anticancer agent used for treating triple-negative breast cancer (TNBC). It exhibits significant inhibitory activity against MDA-MB-453 cells, with an IC50 value of 8.5 μM. Anti-TNBC agent-9 impedes tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. Additionally, it inhibits tumor cell proliferation by inducing apoptosis, achieved through the increased expression of pro-apoptotic protein BAX and decreased expression of anti-apoptotic protein BCL-2.</p>

<p>1-Methyl-1H-pyrrolo[2,3-b]pyridine exhibits cytotoxicity against MCF-7 cells and can be used in related research in the field of life sciences.</p>

<p>NSC90616 is a mutant p53 rescue compound [1] .</p>

<p>BU 224 hydrochloride is a selective imidazoline I(2) binding site ligand and has antinociceptive and antidepressant-like activities.</p>

<p>sEH inhibitor-19 (Compound (R)-14i) is an orally active soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 1.2 nM. This compound suppresses the expression of TNF-α and IL-6 and exhibits anti-inflammatory effects in mouse models of acute pancreatitis and Carrageenan-induced edema.</p>

<p>Z-Asp-CH2-DCB is an irreversible inhibitor of broad spectrum caspase.</p>

<p>Volrustomig is a bi-engineered fragment crystallizable (Fc) domain, a monovalent bispecific IgG1 monoclonal antibody targeting the key immune checkpoint receptors PD-1 and CTLA-4. It boosts T-cell activation and antitumor immunity, making it a promising immunotherapy for various cancers. Molecular weight: 146.77 kDa.</p>

<p>Pomalidomide-PEG3-CO2H is a cereblon ligand-PEG3 linker for PROTACs.</p>

<p>Prodigiosin is a secondary metabolite of Symbiotic bacteria. It also has anti-fungal and anti-cancer activity.</p>

<p>Sodium 2,4-dichlorophenoxyacetate: selective herbicide, controls broadleaf weeds by disrupting growth and protein/DNA synthesis.</p>

<p>Apoptosisinducer 33 (compound H2) is a hydrazone derivative. It exhibits antioxidant and antimicrobial properties, capable of inhibiting the growth of Staphylococcus aureus, Escherichia coli, and Candida albicans. Additionally, Apoptosisinducer 33 can suppress tumor cell proliferation and induce apoptosis (apoptosis), making it useful for tumor research.</p>

<p>(E/Z)-Eltrombopag 13C4 is a mix of E/Z isotopologues, both 13C-labeled TPO receptor agonists for thrombocytopenia.</p>

<p>ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.</p>

<p>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.</p>

<p>YF135 is a reversible-covalent KRAS G12C PROTAC that degrades its target via the VHL-proteasome pathway.</p>

<p>DC 81: Streptomyces-derived antitumor antibiotic, potent nucleic acid synthesis inhibitor, binds DNA sequences, forms covalent adducts.</p>