Ciclo cellulare/Checkpoint

Abrilumab (MEDI-7183) is a fully human monoclonal antibody against α4β7 that inhibits the α4β7 integrin.

<p>CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM).</p>

<p>SU056 is a YB-1 inhibitor that induces cell-cycle arrest, apoptosis, and inhibits ovarian cancer cell migration.</p>

Potent Chk2 inhibitor with 3 nM IC50, 63-fold more selective over Chk1, affects 84 kinases, reduces DNA damage response and apoptosis in cells.

Clofarabine-5'-triphosphate is a metabolite of Clofarabine, produced via phosphorylation by deoxycytidine kinase (dCK). It exhibits cytotoxicity in cancer cells by inhibiting DNA synthesis and DNA repair.

<p>5’-O-DMT-Bz-Rc is a modified nucleoside and can be used to synthesize DNA or RNA.</p>

<p>WRN inhibitor 17 (Compound 250) is an orally active inhibitor of Werner syndrome ATP-dependent helicase (WRN), specifically targeting the helicase domain activity of WRN. It holds potential for use in cancer research.</p>

16,16-dimethyl Prostaglandin A1 is a useful organic compound for research related to life sciences.

<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>PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0/G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)</p>

<p>TFMU-ADPr triethylamine is a substrate for PARG activity measurement, releasing a fluorophore to indicate PAR hydrolase activity.</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>Anti-c-myc Antibody (9E10) is a chimeric mouse IgG1 antibody targeting human c-myc.</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>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>Carboxy-pyridostatin, as a fluorescent probe, can target G-quadruplex structures and trap cytoplasmic RNA G-quadruplex structures in cells.</p>

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

<p>GS-443902 trisodium, a strong RdRp blocker, inhibits RSV/HCV with IC50 of 1.1/5 μM and is Remdesivir's active form.</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>Nocarnickelamides B (Compound 2) is a linear peptide and an inhibitor of ROCK1/2. It exhibits dual inhibitory activity against ROCK1 and ROCK2, with IC50 values of 14.9 μM and 21.9 μM, respectively. This compound binds to the ATP binding site and inhibits ROCK-mediated cytoskeletal contraction markers, such as myosin light chain activation. Nocarnickelamides B can be utilized in glaucoma research.</p>