Ciclo celular / Checkpoint

<p>N1-Methylxylo-guanosine, a purine analog, targets lymphoid cancer via DNA synthesis inhibition and apoptosis.</p>

<p>FF-10502, a pyrimidine analog of Gemcitabine, inhibits DNA polymerases α/β, targeting dormant cancer cells.</p>

<p>Esperamicin A1, a powerful antitumor drug, comes from Actinomadura verrucosospora.</p>

<p>KIF2C-IN-1 (Compound 7S9) is a selective and potent small molecule inhibitor of KIF2C. It stabilizes the interaction between KIF2C and microtubule proteins, preventing the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel in Paclitaxel-resistant triple-negative breast cancer (TNBC) cells and, when combined with Paclitaxel, significantly reduces tumor growth in mouse models.</p>

<p>YKL-5-124 TFA is a potent CDK7 inhibitor (IC50: 53.5 nM), more than 100x selective over CDK9/2, not active on CDK12/13, and disrupts the cell cycle.</p>

<p>DNA Gyrase-IN-12 (Compound 6d) is an inhibitor of DNA gyrase. It exhibits antibacterial activity with MIC values ranging from 0.031 to 0.0625 μg/mL against Vancomycin-Intermediate Staphylococcus aureus (VISA) and Enterococcus faecium.</p>

<p>5-Methylcytidine 5′-triphosphate trisodium (5-Methyl-CTP trisodium), a modified nucleoside triphosphate, enhances translational properties and stability, while</p>

<p>Selective Cdk4 degrader. Degrades Cdk4 in Molt-4 cells, with no effect on Cdk6 levels. Displays cereblon-dependent degradation.</p>

<p>IRE1-IN-2 (compound G15) functions as a potent inhibitor of IRE1. It effectively suppresses lipid accumulation induced by FFA, exhibiting an IC50 value of 2.06 μM.</p>

<p>Torvutatug is a human IgG1κ monoclonal antibody that acts against FOLR1.</p>

<p>Clofarabine-5'-diphosphatetrisodium (Clofarabine-DP trisodium) is the sodium salt form of Clofarabine-5'-diphosphate. As a metabolic product of Clofarabine, it results from phosphorylation by deoxycytidine kinase (dCK). Clofarabine-5'-diphosphate trisodium can undergo further phosphorylation to form Clofarabine-5'-triphosphate, demonstrating cytotoxicity in cancer cells by inhibiting DNA synthesis and repair.</p>

<p>PT-129 is a RPOTAC degrader that targets the G3BP1/2NTF2 domain (protein-RNA interaction site), facilitating the breakdown of intracellular stress granules. It prevents the formation of stress granules in stressed cells and deconstructs existing ones, thereby disrupting ATF4 transmission and inhibiting cancer cell proliferation. Stress granules (SGs) are membraneless cytoplasmic compartments formed under stress, which aid in the transfer of ATF4 from fibroblasts to tumor cells, promoting fibroblast-related tumor growth. G3BP1/2 serve as central proteins in the SG network, and inhibiting them may reduce the stress resilience of cancer cells within the tumor microenvironment. PT-129 consists of a target protein ligand (red part) G3BP1/2-Targeting ligand-1, an E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a PROTAC linker (black part) Amino-PEG3-C2-acid; the E3 ligase ligand and linker form the complex Thalidomide-NH-PEG3-propionic acid.</p>

<p>Anti-c-myc Antibody (9E10) is a chimeric mouse IgG1 antibody targeting human c-myc.</p>

<p>C(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand for α5β1-integrin, exhibiting an IC50 of 2.9 nM [1].</p>

<p>NXL-101, an oral/IV antibiotic for Gram-positive bacteria like MRSA, was discontinued by Novexel in 2008.</p>

<p>DSPE-PEG3000-iRGD is a PEG compound comprising DSPE and the αv-integrin targeting peptide (iRGD). The iRGD peptide binds to αv-integrin and undergoes proteolytic cleavage within tumors to produce CRGDK/R, interacting with neuropilin-1. This results in tumor targeting and penetration capabilities. DSPE-PEG3000-iRGD is applicable in drug delivery.</p>

<p>α-Methyl-DL-aspartic acid specifically inhibits argininosuccinate synthase (ASS), the rate-limiting enzyme in 1-citrulline-to-1-arginine recycling.</p>

<p>PROTAC CDK9 degrader 4 is a CDK9 degrader that targets transcriptional regulation and has potential anticancer activity.</p>

<p>5’(R)-C-Methyl-5-fluorouridine, a uridine analogue, possesses potential antiepileptic properties.</p>

<p>JH-XVI-178: potent CDK8/19 inhibitor with good pharmacokinetics, low clearance, moderate oral bioavailability.</p>