Apoptosi

<p>HG-7-85-01 is a novel ATP-competitive and type II tyrosine kinase inhibitor targeting both wild-type and watchman mutant BCR-ABL, PDGFRα, Kit, and Src kinases.</p>

<p>GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting.</p>

<p>Sodium valproate is an anti-epileptic, boosting brain GABA levels and possibly affecting potassium channels for membrane stability.</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>DB0614 degrades 26 kinases including AAK1 and CDK6, targeting aberrant activity in disease research.</p>

<p>MEK/PI3K-IN-2 is a potent dual inhibitor (MEK1 IC50: 352 nM, PI3Kα: 107 nM, PI3Kδ: 137 nM) that reduces pAKT, pERK1/2, and hinders tumor cell growth.</p>

<p>Necroptosis-IN-3 (Cyclohexanecarboxamide, N-(2-thienylmethyl)-) (Compound 69) is a Necroptosis inhibitor that inhibits TNF-α induced necroptosis.</p>

<p>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</p>

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

<p>F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM.</p>

<p>Calcimycin hemimagnesium is an antibiotic, ionophore, and ATPase inhibitor that boosts intracellular Ca2+, causing cell death and apoptosis.</p>

<p>Asunercept (APG101/CAN008) is a CD95-Fc protein targeting CD95L, used in GBM, MDS, and GvHD research.</p>

<p>Apoptosisinducer 26 (compound [AgCl(dap2SH)(PPh3)2]) is a mononuclear Ag(I) ligand-based autophagy inducer that exhibits antibacterial and anticancer activities against various bacterial strains and cancer cell lines. This compound facilitates the accumulation of Ag(I) ions in the periphery of bacteria, effectively inhibiting the growth of both Gram-positive (+) and Gram-negative (-) bacteria. Additionally, Apoptosisinducer 26 can intercalate between the base pairs of CT DNA, inducing apoptosis in A549 cells. It also possesses radical scavenging properties, which helps prevent oxidative stress.</p>

<p>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.</p>

<p>EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.</p>

<p>p53 and MDM2 proteins-interaction-inhibitor (racemic) is an inhibitor of the interaction between p53 and MDM2 proteins.</p>

<p>LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S, with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del/T790M/C797S, and results in significant tumor reduction in a C797S mutant xenograft model.</p>

<p>PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.</p>

<p>HTH-01-091 TFA: Potent, selective MELK inhibitor (IC50=10.5 nM); also targets PIM1/2/3, RIPK2, DYRK3, smMLCK, CLK2; used in breast cancer research.</p>

<p>c-Met/HDAC-IN-4, a dual inhibitor of c-Met/HDAC, exhibits an IC 50 value of 28.92 nM for c-Met. This compound effectively induces G 0 /G 1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells. Additionally, c-Met/HDAC-IN-4 suppresses both the proliferation and invasion of breast cancer cell lines.</p>

<p>Chaetoglobosin A, the active compound extracted of Penicillium aquamarinium, is a member of the cytochalasan family. It preferentially induces apoptosis.</p>

<p>ZX782 acts as a GPX4 protein degrader and an inducer of ferroptosis (Ferroptosis), targeting GPX4 for destruction via both the ubiquitin-proteasome system and the autophagy-lysosome pathway. Following the degradation of GPX4 induced by ZX782, there is a significant increase in the accumulation of lipid reactive oxygen species (ROS) in HT1080 cells.</p>

<p>AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.</p>

<p>TNF-α-IN-9 is an NDM-1 inhibitor-3 analog and is a TNF-α inhibitor.TNF-α-IN-9 shows low inhibitory activity.</p>

<p>Bfl-1-IN-6 (Compound 20) is an orally active inhibitor of Bcl-2-related protein A1 (BFL1) with an IC50 of 19 nM. This compound can stabilize BFL1 protein, activate cleaved caspase 3, and demonstrates antitumor activity in mouse models.</p>

<p>Holothurin A is a triterpene glycoside.</p>

<p>Peginterferon beta-1a: first pegylated interferon for cancer, RMS research; induces tumor cell apoptosis.</p>

<p>Thalidomide-O-C7-NH2 is a cereblon ligand-linked E3 ligase for PROTAC use.</p>

<p>P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. It downregulates Pin1 substrate proteins, including Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. Additionally, P1D-34 exhibits antiproliferative activity across various acute myeloid leukemia (AML) cell lines and induces DNA damage and apoptosis by generating reactive oxygen species (ROS).</p>

<p>Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.</p>

<p>K-252c is a staurosporine analog isolated from Nocardiopsis sp.</p>

<p>Thalidomide-5,6-Cl is a cereblon ligand derivative that recruits CRBN protein and forms PROTACs with a linker.</p>

<p>A unique collection of 420 compounds targeting PI3K/Akt/mTOR signaling for research in PI3K/Akt/mTOR signaling, and drug discovery in diseases involved with</p>

<p>BT44, a potent second-gen GDNF mimetic, is a lead for treating neurodegeneration.</p>

<p>RIPK1-IN-30 (compound 24) is a potent RIPK1 inhibitor with an IC50 of 2.01 μM. It demonstrates a protective effect in the HT-29 cell model of TSZ-induced necroptosis, with an EC50 of 6.77 μM.</p>

<p>GA-Mk is a triterpenoid from Ganoderma lucidum mycelia, inhibits HeLa cell growth, and induces apoptosis via mitochondria; used in cervical cancer studies.</p>

<p>Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding &amp; osteoclastogenesis, induces PC12 cell apoptosis.</p>

<p>DCZ3301 is a novel aryl-guanidino inhibitor.</p>

<p>intestinal epithelium-specific growth factor</p>

<p>KTX-582: potent IRAK4/Ikaros degrader (DC50=4/5nM), induces MYD88 MT DLBCL apoptosis &amp; tumor regression in lymphoma.</p>

<p>Indinavir is an HIV protease inhibitor,HAART. inhibits the activation of MMP-2 in endothelial cells and exhibits affinity for α7-nAchR and SARS-CoV-2 Mpro.</p>

<p>Hexapeptide-11 is a novel proteostasis network modulator in human diploid fibroblasts.</p>

<p>SL-01, an oral gemcitabine derivative, potently induces apoptosis to hinder breast cancer more effectively than gemcitabine.</p>

<p>Monensin, from Streptomyces cinnamonensis, inhibits Wnt/β-catenin. Potential anticancer agent.</p>

<p>GPX4-IN-5 is a GPX4 inhibitor with antitumor activity.GPX4-IN-5 induces iron death and may be used for the treatment of triple negative breast cancer.</p>

<p>LIB3S0280 is a potent inhibitor of TBK1, with an IC50 of 493.9 nM. It suppresses TBK1 downstream signaling by reducing the phosphorylation of IκBα and AKT. LIB3S0280 causes G2/M phase arrest and induces apoptosis in pancreatic cancer cells. Notably, it exhibits significant inhibitory effects on pancreatic cancer cell lines with high TBK1 expression, with a 96-hour IC50 value ranging from 6.64-10.98 μM. LIB3S0280 shows potential for research in pancreatic ductal adenocarcinoma (PDAC).</p>

<p>BGC4 is a gold(III) complex based on biphenyl. It inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity with an IC50 of 5.4 μM in MDA-MB-231 cells, and induces apoptosis. Additionally, BGC4 demonstrates antitumor activity in mouse models.</p>

<p>PPA-904 FA is a cationic photosensitizer with antimicrobial activity that can be used to study chronic leg ulcers and diabetic foot ulcers.</p>

<p>HYS-072 is an orally active derivative of chrysin with antitumor properties. It induces apoptosis (Apoptosis) and autophagy (Autophagy) by inhibiting the PI3K/AKT/mTOR signaling pathway, and suppresses tumor growth in xenograft models in vivo by modulating autophagy-related pathways. HYS-072 is applicable for research in treating triple-negative breast cancer.</p>

<p>dTAG-7 selectively degrades BRD4 and FKBP12F36V by linking BET bromodomains to E3 ligase CRBN; it's a heterobifunctional degrader.</p>