Apoptose

<p>Ac-DMLD-CMK is a peptide designed to target the caspase3-Gsdme signaling pathway in mice. It specifically inhibits the activation of caspase 3 and Gsdme, preventing the cleavage of Gsdme by caspase 3, which reduces pyroptosis. This process helps alleviate damage to renal tubular epithelial cells and decrease the secretion of inflammatory cytokines. Ac-DMLD-CMK can lower serum creatinine and blood urea nitrogen levels in mice induced by Cisplatin, thereby mitigating the progression of renal dysfunction. It holds potential for research into chemotherapy-induced nephrotoxicity.</p>

<p>Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value</p>

<p>Compound 3b inhibits tubulin polymerization, IC50 12.38 µM, with anticancer properties and promotes cell apoptosis.</p>

<p>Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.</p>

<p>FLT3/TrKA-IN-1: Potent dual kinase inhibitor for FLT3 &amp; TrKA, promising for AML research.</p>

<p>MC3629, an inhibitor of the histone methyltransferase (EZH2), exhibits antitumor activity. This compound effectively inhibits the proliferation and self-renewal of SHH MB cancer cells while inducing cell apoptosis (apoptosis). MC3629 is also useful in research on tumor aggressiveness and resistance.</p>

<p>CDK-IN-9: A potent CDK inhibitor, gels to enhance CDK12/DDB1 binding, targets CDK2/E (IC50: 4 nM), induces apoptosis via dephosphorylation.</p>

<p>PLK1-IN-13 is a selective, orally active PLK1 inhibitor with an IC50 of 0.27 nM. It also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 induces cell cycle arrest at the G2 phase, promotes apoptosis, and downregulates the transcription of the cancer-associated oncogene c-MYC. This compound inhibits tumor growth and is applicable for research in acute myeloid leukemia (AML).</p>

<p>OICR12694 (JNJ-65234637) is an orally active inhibitor of B cell lymphoma 6 (BCL6) .</p>

<p>Anticancer agent 44 induces apoptosis, is selective, cytotoxic to cancer cells, and minimally toxic to human lymphocytes.</p>

<p>Ganoderic acid R: potent anticancer, induces apoptosis, cytotoxic to MDR and sensitive tumor cells.</p>

<p>NF-κB-IN-4 (compound 17) is a potent inhibitor of NF-κB pathway which can cross blood brain barrier (BBB).</p>

<p>Anticancer agent 64 (5m) induces apoptosis, has IC50 2.4μM in CCRF-CEM, activates caspases, cleaves PARP, affects mitochondria.</p>

<p>PD-1-IN-17 TFA is a potent PD-1 inhibitor, blocking 92% of splenocyte growth at 100 nM.</p>

<p>RIPK1-IN-28 (compound 13) is an orally active inhibitor of RIPK1. It exhibits inhibitory effects on human I2.1 and Hepa1-6 cells, with IC50 values of 0.4 and 1.2 nM, respectively.</p>

<p>Compound 28 is a nonsteroidal VDR agonist with 690 nM potency, inducing cell cycle arrest and apoptosis in MCF-7 cells.</p>

<p>RSK-IN-2 (Compound 3e) is an inhibitor of RSK, showing IC50 values of 37.89 nM for RSK2, 30.78 nM for RSK1, 20.51 nM for RSK3, and 91.28 nM for RSK4. It suppresses tumor cell proliferation, induces apoptosis, and causes cell cycle arrest at the G2/M phase.</p>

<p>TAI-95 is an inhibitor of highly expressed cancer protein 1 (Hec1).</p>

<p>VEGFR-2-IN-11 is a potent inhibitor of VEGFR-2 (IC50: 60.27 nM) with an IC50 value of 60.27 nM, which induces apoptosis and has anticancer activity.</p>

<p>NSC308848 is an effective apoptosis (cell death) inducer that operates in a Myc-dependent manner. It acts by inhibiting Myc transactivation and disrupting the DNA binding activity of Myc family proteins.</p>