Apoptose

MSU-42011: oral RXR-like agonist, inhibits iNOS & p-ERK, antitumor in lung cancer model, effective preclinical treatment.

PRLX-93936 HCL is an analog of erastin and demonstrated synergistic effects against non-small cell lung cancer (NSCLC) cells with cisplatin.

MAO-B-IN-30 is a selective and potent MAO-B inhibitor that crosses the blood-brain barrier with antiproliferative activity and inhibits both MAO-A and MAO-B.MAO-B-IN-30 reduces the levels of TNF-alpha, IL-6, and NF-kB in organisms, and can be used to study Parkinson's-type neurological disorders.

NecroIr1, an iridium(III) complex, induces necroptosis in Cisplatin-resistant lung cells, targeting mitochondria and disrupting MMP.

TRAP-1 (XJZ-06-462) is a p53 transcription activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. In the p53Y220C pancreatic cell line, TRAP-1 rapidly upregulates p21 and other p53 target genes. TRAP-1 also inhibits cell proliferation, exhibiting IC50 values of 3.94 μM and 0.531 μM in BxPC-3 and A549 cell lines, respectively. Additionally, TRAP-1 modulates autophagy in lung cancer cells and provides protection against oxidative stress and apoptosis.

<p>Cathepsin B, a cysteine protease located within the subcellular endosomes and lysosomal compartments, mediates apoptosis and can be used in cancer research.</p>

Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small

TPP-resveratrol is a conjugate of Resveratrol and triphenylphosphine (TPP), noted for its anticancer activity. This compound enhances the efficacy of Resveratrol by facilitating its targeted delivery to mitochondria, thus inducing mitochondrial-mediated cell apoptosis (apoptosis).

(R)-Q-VD-OPh is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible inhibitor of pan-caspase, with potent antiapoptotic properties.

PUMA BH3 activates Bak, binds Bcl-2; triggers apoptosis via cytochrome C release; Kd 26 nM.

CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target inhibitor of CYP51/PD-L1, displaying IC50 values of 0.17 and 0.021 μM, respectively.

<p>PARP1-IN-16 (compound 12a) serves as a potent PARP1 inhibitor, exhibiting an IC50 value of 1.89 nM.</p>

<p>PTP1B-IN-30 (Compound 3j) is an inhibitor of PTP1B with an IC50 of 0.51 µM. It suppresses the proliferation of T47D cancer cells with an IC50 of 21.21 µM, induces cell cycle arrest at the S phase, and triggers apoptosis in T47D cells.</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>

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)

"(±)-Enterodiol, the racemate of Enterodiol, is metabolized from lignans found in whole-grain cereals, nuts, legumes, flaxseed, and vegetables by human intestinal bacteria. This compound exhibits apoptotic effects in colorectal cancer (CRC) cells and has been identified to possess anti-cancer activities [1] [2]."

<p>PQ401 (IGF-1R Inhibitor II) suppresses autophosphorylation of IGF-1R domain(IC50&lt;1 μM).</p>

<p>BRD6257 is an orally active inhibitor of protein phosphatase 1D (proteinphosphatase, Mg2+/Mn2+ dependent 1D, PPM1D) with an IC50 of 5 nM. It activates the p53 signaling pathway (EC50 of 51 nM), enhances p21 expression, and inhibits the proliferation of cancer cells MOLM13 (IC50 = 2.8 μM). BRD6257 demonstrates good metabolic stability in human and rat liver microsomes.</p>

Methylene Violet 3RAX is a cationic dye that is a potential photosensitizer in photodynamic therapy and has antitumor activity.

<p>Thalidomide-based E3 ligase ligand with PEG2-C2 linker; used as an immunomodulatory cancer treatment.</p>