Cell Cycle/Checkpoint

<p>CDK7-IN-7: Selective CDK7 inhibitor, IC50 &lt; 50 nM (Patent CN112661745A).</p>

<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>

<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>IBU-DC Phosphoramidite is used for synthesis of oligonucleotides.</p>

<p>BTO-1: Plk inhibitor effective in regulating phosphorylation.</p>

<p>N6-Benzoyl-3'-O-DMT-adenosine is a purine analog with antitumor effects by hindering DNA synthesis and inducing apoptosis.</p>

<p>Pseudorabies virus-IN-1 is a potent inhibitor of pseudorabies virus (PRV) with an EC50 of 0.29 nM, acting by targeting PRV deoxyribonucleic acid polymerase (DNA pol) to suppress PRV replication. It effectively inhibits PRV replication even at low concentrations (MIC80: 1.6-8 nM) and is useful for research on PRV infections.</p>

<p>TFMU-ADPr triethylamine is a substrate for PARG activity measurement, releasing a fluorophore to indicate PAR hydrolase activity.</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>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>Mulnitorsen acts as an inhibitor of antisense non-coding mitochondrial RNA (ASncmtRNA) synthesis and serves as an antitumor agent [1].</p>

<p>2’-Deoxy-2’-fluorouridine 5’-monophosphate triethyl ammonium, a purine nucleoside analog, exhibits extensive antitumor effects against indolent lymphoid</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>Odulimomab: anti-LFA-1 antibody, inhibits T cell growth, protects against ischemic injury, used in transplant rejection research.</p>

<p>Ac-dA Phosphoramidite is a phosphinamide monomer utilized for oligonucleotide synthesis.</p>

<p>α2β1 Integrin Ligand Peptide TFA interacts with the integrin receptor on the cell membrane and enters the cell to mediate extracellular signaling.It is a</p>

<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.</p>

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

<p>PLK1-IN-2 is a PLK1 kinase inhibitor with an IC 50 value of 0.384 μM.</p>

<p>N7-Methyl-2’-O-(2-methoxyethyl) guanosine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

<p>NXL-101, an oral/IV antibiotic for Gram-positive bacteria like MRSA, was discontinued by Novexel in 2008.</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>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>5-(2-Hydroxyethyl)-2',3'-di-O-toluoyl-2'-deoxyuridine, a purine nucleoside analog, exhibits widespread antitumor activity specifically against indolent lymphoid</p>

<p>Apcin A HCL is an Apcin-derived APC inhibitor that binds Cdc20 and hinders ubiquitination, useful for synthesizing PROTAC CP5V.</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>Trimethoprim hydrochloride: oral, broad-spectrum antibiotic, DHFR inhibitor, treats UTIs, shigellosis, pneumocystis pneumonia, may block Influenza A with zinc.</p>

<p>Cyclothialidine is an inhibitor of DNA gyrase.</p>

<p>1-(β-D-Xylofuranosyl)-N6-Isopentenyladenine is an adenosine analog.</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>TC113, a c(RGDyK)-linked Gemcitabine, targets αvβ3 integrin, entering A549 cells, and inhibits WM266.4 and A549 cell growth.</p>

<p>CDK2/PIM1-IN-1 is an inhibitor of the kinases CDK2 (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM). It can induce apoptosis (cell death) and reduce the expression of TNF-α, which promotes tumors. CDK2/PIM1-IN-1 exhibits antitumor activity.</p>

<p>(+)-Glaucarubinone is a natural product that can be used as a reference standard.</p>

<p>'Rev 2’-O-MOE-A(Bz)-5’-amidite is a nucleoside analog specifically categorized within the purine subset, renowned for its wide-ranging antitumor efficacy</p>

<p>3’-Beta-C-Ethynyl-4-deoxyuridine is a purine nucleoside analog.</p>

<p>cis-Lomibuvir (cis-VX-222) is a selective HCV NS5B RdRp inhibitor with a Kd of 17 nM and an EC50 of 5.2 nM, targeting thumb pocket 2.</p>

<p>5’-DMTr-3’dA(Bz)-methylphosphonamidite, a purine nucleoside analog, exhibits wide-ranging antitumor activity, specifically targeting indolent lymphoid</p>

<p>NUAK1-IN-2 (Compound 24) is an inhibitor of NUAK1 with an IC50 of 3.162 nM, as well as an inhibitor of CDK2/4/6. It is applicable in research related to cancer, neurodevelopmental disorders, and Alzheimer's disease.</p>

<p>IV-361, an orally active and selective CDK7 inhibitor with a Ki value of less than or equal to 50 nM, demonstrates potent anti-cancer activity (US20190256531A1</p>

<p>Remdesivir metabolite, antiviral nucleoside analog, effective against SARS-CoV and MERS-CoV.</p>

<p>MEDI-578 is a CHO-expressed humanized monoclonal antibody targeting NGF/bNGF for the study of neurological and immune system disorders.</p>

<p>BIO5192 hydrate: potent α4β1 inhibitor, binds selectively (Kd&lt;10 pM, IC50=1.8 nM), boosts murine HSPC mobilization 30x.</p>

Importazole is an inhibitor of the transport receptor importin-β. It specifically inhibits importin-β likely by altering its interaction with RanGTP.

<p>6-Methoxy-9-β-D-ethynyl-purine: a purine analog with antitumor action, impeding DNA synthesis and inducing apoptosis.</p>

<p>dGMP is a substrate for DNA synthesis, phosphorylated to dGDP and dGTP, and linked to mitochondrial DNA depletion syndrome in humans.</p>

<p>Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.</p>

<p>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>

<p>PD-1/PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1/PD-L1 interaction.</p>

<p>PROTACMTP3 degrade-1 is a PROTAC degrader for MYC.</p>

<p>Nitrosofolic acid is a folic acid derivaive.</p>