Apoptose

<p>CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC50 of 0.21 μM. It exhibits cytotoxicity towards Vero cells with an IC50 of 28.52 μM.</p>

<p>PIM-1/CK2-IN-2 (compound 3aA) is an inhibitor of the PIM-1/CK2 enzymes. This compound can induce the mitochondrial apoptosis pathway in CCRF-CEM cells and is utilized in cancer research.</p>

<p>BCL-XL-IN-1 (Compound 11) is a selective inhibitor of BCL-XL, exhibiting a Ki of less than 0.01 nM against BCL-XLTR-FERT. It is primarily used in cancer research.</p>

<p>PROTAC EGFR degrader 5 effectively breaks down EGFR Del19 in HCC827 cells at 34.8 nM, inducing apoptosis and G1 arrest.</p>

<p>LSD1-IN-36, an effective LSD1 inhibitor with an IC50 value of 0.8 nM, induces cell apoptosis and arrests the cell cycle. This compound also exhibits antitumor activity.</p>

<p>Antiproliferative agent-59 (Compound 14u) acts as an inhibitor of tubulin polymerization. Demonstrating anticancer activity in Huh7, SGC-7901, and MCF-7 cell lines, this compound achieves IC50 values of 0.03, 0.18, and 0.13 μM, respectively. Additionally, it arrests the cell cycle at the G2/M phase and induces apoptosis in Huh7 cells. In a xenograft mouse model utilizing Huh7 cells, Antiproliferative agent-59 exhibits antitumor effects against hepatocellular carcinoma without significant toxicity.</p>

<p>BK50164: CD73 inhibitor, IC50=13.089µM; binds CD99, KD=1.5µM; anticancer, induces apoptosis, arrests sub-G1.</p>

<p>Vallesiachotamine, a recognized monoterpene indole alkaloid, exhibits anti-tumor activity [1].</p>

<p>Tomuzotuximab: fully human, glycoengineered IgG1 anti-EGFR monoclonal antibody with anticancer properties.</p>

<p>BM-1197, a highly potent and specific dual inhibitor of Bcl-2 and Bcl-xL, effectively targets these proteins with IC50 values of 3.5 nM and 5.2 nM for Bcl-2 and</p>

<p>ReACp53 inhibits amyloid formation, restores p53 in cancer cells and HGSOC-derived organoids.</p>

<p>STM3006 is an orally active, selective and and potent METTL3 inhibitor with antitumor activity for the study of acute myeloid leukemia (AML).</p>

<p>Didocosahexaenoin, omega-3 diglyceride, disrupts mitochondria, induces ROS, apoptosis, and is cytotoxic to prostate cancer cells.</p>

<p>Chalcones A-N-5, a non-cytotoxic trihydroxy chalcone, aids cell growth &amp; neuroprotection, inhibits ferroptosis, and targets AD research.</p>

<p>Thiocolchicine inhibits tubulin polymerization (IC50: 2.5 µM, Ki: 0.7 µM), induces apoptosis, and serves as an ADC cytotoxin.</p>

<p>Sanggenon G inhibits XIAP by binding its BIR3 domain; affinity is 34.26 μM, boosting caspase activation.</p>

<p>MDM2/4-p53-IN-3 inhibits MDM2/4-p53 PPIs (IC50: 18.5nM MDM2, 14.8nM MDM4), used in cancer research.</p>

<p>MEK/PI3K-IN-1 (6r) is a dual MEK/PI3K inhibitor; IC50: 124 nM (MEK1), 130 nM (PI3Kα), 236 nM (PI3Kδ). It reduces pAKT, pERK1/2, and hinders tumor growth.</p>

<p>FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.</p>

<p>Dimeric Smac mimetic inhibits XIAP, cIAP1/2 (IC50: 15/15/21 nM); binds BIR3 domain; degrades cIAPs; induces apoptosis in cancer cells; shrinks tumors in mice.</p>