Cell Cycle/Checkpoint

<p>Compound PDK0016, with CAS No. 108-53-2, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound PDK0016 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.</p>

<p>PAT-LM1 is a human monoclonal antibody that targets NRB54/NONO. It is applicable in the study of hematological malignancies.</p>

<p>Uridine triphosphate 13C9,15N2 sodium is an isotopically labeled.UTP is a key in RNA synthesis molecule a substrate for RNA polymerase.</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>MRK-952 is a NUDIX hydrolase inhibitor. NUDIX enzymes play a role in cellular metabolism, homeostasis, and mRNA processing.</p>

<p>N3,5-Dimethyl-2’-O-(2-methoxyethyl) uridine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

<p>Stigmatellin is an antibiotic derived from the cell mass of the myxobacterium, effective against yeasts (yeasts), filamentous fungi (filamentous fungi), and several Gram-positive bacteria (Gram-positive bacteria). Additionally, it serves as a potent inhibitor of photosynthetic electron (photosynthetic electron) transfer. Stigmatellin utilizes various sugars, polysaccharides, and acids from the citric acid cycle as substrates, inhibiting RNA and protein synthesis. It has two different inhibitory sites: one located on the reducing side of photosystem II and the other at the cytochrome b6/f complex. Stigmatellin holds potential for use in antimicrobial and photosynthesis research.</p>

<p>CDK12-IN-4 is a pyrazolotriazine that inhibits CDK12 (IC50: 0.641 μM) with high ATP (2 mM) and spares CDK2/Cyclin E and CDK9/Cyclin T1 (IC50: &gt;20 μM).</p>

<p>CDK5-IN-1: Potent CDK5 inhibitor (&lt;10 nM) used in kidney disease research.</p>

<p>13-TP is an inhibitor of SARS-CoV-2. It effectively suppresses in vitro RNA synthesis catalyzed by the central replication-transcription complex (C-RTC, nsp12-nsp7-nsp82) of SARS-CoV-2. 13-TP fully inhibits RdRp polymerase activity and obstructs the complete extension of some primer RNAs.</p>

<p>5'-O-DMT-2'-O-TBDMS-rI, a modified nucleoside, finds application in deoxyribonucleic acid (DNA) or nucleic acid synthesis.</p>

<p>TMX-2138 is a CDKs PROTAC degrader, with IC50 values of 8.7 nM for CDK1/cyclinB, 10.9 nM for CDK2/cyclinA, 7.0 nM for CDK5/p25, and 25.7 nM for CDK9/cyclinT1. It enhances the ubiquitination and degradation of CDKs and is utilized for ovarian cancer research.</p>

<p>Sarecycline hydrochloride is a narrow-spectrum tetracycline antibiotic with antimicrobial and anti-inflammatory activity.</p>

<p>3’-Deoxy-N6-(m-methoxy benzyl)adenosine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

<p>Rifalazil (KRM-1648) is a benzophenazine antibiotic with antibacterial activity, useful for research on chlamydia infections.</p>

<p>LEB-03-146: WEE1 DUBTAC linking AZD1775 to OTUB1 via PEG2; stabilizes WEE1 in HEP3B cells.</p>

<p>Cimpuciclib is a cyclin-dependent kinase(CDK) inhibitor and antineoplastic.</p>

<p>5'-O-TBDMS-dU can be used in the synthesis of oligoribonucleotides.</p>

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

<p>m7GpppGmpG, a trinucleotide 5′ cap analog, exhibits capping efficiencies of 86% for the RNAs obtained [1].</p>

<p>PKMYT1-IN-3 (compound 8ma) is a potent, selective inhibitor of PKMYT1, demonstrating an IC50 of 16.5 nM and exhibiting antitumor activity.</p>

<p>AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.</p>

<p>5-O-TBDMS-N4-Benzoyl-2-deoxycytidine is a modified nucleoside utilized in the synthesis of deoxyribonucleic acid (DNA) or nucleic acid.</p>

<p>Ficellomycin is an aziridine antibiotic produced by Streptomyces ficellus. Which shows high in vitro activity against Gram-positive bacteria.</p>

<p>2-Methylbutyrylcarnitine (chloride) acts as a gut microbial metabolite that targets integrin α2β1 on platelets, facilitating the activation of cytosolic phospholipase A2 (cPLA2) and enhancing platelet hyperresponsiveness. This compound further augments platelet hyperreactivity and promotes thrombus formation in mice. It is also characterized as a branched-chain acylcarnitine.</p>

<p>LL-K8-22: potent CDK8/cyclin C degrader; DC50 ~2.5μM; hinders STAT1 phosphorylation; curbs E2F/MYC cancer pathways; for TNBC study.</p>

<p>Compound Ac13, also termed AURKA against 1, acts as an inhibitor of the Aurora kinase (AURKA) with an IC50 of less than 0.5 nM, targeting the acetylation of endogenous lysine (K162) and exhibiting anti-tumor cell proliferation activity. The kinase activity of AURKA, acetylated at K162 and induced by AURKA against 1, is reversibly restored in HCT116 cells transfected with SIRT3.</p>

<p>6-Amino-4-methoxy-2-(β-D-ribofuranosyl)-2H-pyrazolo[3,4-d]pyrimidine, a purine nucleoside analogue, exhibits widespread antitumor efficacy, particularly against</p>

<p>Pseudouridimycin: a C-nucleoside antibiotic, inhibits bacterial RNAP, targets Gram-negative and Gram-positive bacteria.</p>

<p>CDK9-IN-25 (compound 4a), an imidazopyrazine derivative, functions as a CDK9 inhibitor with an IC50 of 0.24 μM.</p>

<p>Ac-MRGDH-NH2 is a pentapeptide containing the RGD sequence. It is utilized in the synthesis of the diastereomeric prodrugs Λ- and Δ-[Ru(Ph2phen)2(κS,κN-(Ac-MRGDH-NH2))]Cl2. In these prodrugs, Ac-MRGDH-NH2 serves as a photolabile protecting group for the cytotoxic diruthenium aqua complexes [Ru(Ph2phen)2(OH2)2]2+, offering integrin targeting and photoactivation properties. Consequently, Ac-MRGDH-NH2 can be applied in studies exploring tumor-targeted photoactivatable chemotherapy.</p>

<p>ONX 0801 (BGC 945) trisodium is a targeted thymidylate synthase (TS) inhibitor specifically designed to act against tumors overexpressing the α-folate receptor.</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>9-(5(R)-C-Methyl-2,3,5-tri-O-benzoyl-D-ribofuranosyl)-6-chloropurine: A purine analog with antitumor effects, inhibiting DNA synthesis and inducing apoptosis.</p>

<p>EFdA-TP: potent HIV-1 RT inhibitor; acts via immediate/delayed chain termination (ICT/DCT) and multiple pathways.</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>DSPE-PEG1000-cRGD is a PEG compound composed of DSPE and the αvβ3-targeting peptide (cRGD). The cRGD peptide specifically binds to the αvβ3 receptors present on the surfaces of various cancer cells and angiogenic vascular cells. DSPE-PEG1000-cRGD is applicable in drug delivery.</p>

<p>M7GpppApG is a trinucleotide mRNA 5' cap analog utilized for in vitro RNA synthesis [1].</p>

<p>2’-Deoxy-2’-fluoroguanosine 5’-monophosphate triethyl ammonium, a purine nucleoside analog, exhibits broad antitumor activity specifically targeting indolent</p>

<p>Orbofiban Acetate is a compound that serves as an antagonist to the platelet GPIIb/IIIa receptor, effectively inhibiting platelet aggregation when administered</p>

<p>N4-(3,3,3-Trifluoropropanoyl)cytidine, a cytidine analog, inhibits DNA methyltransferases, possibly anti-metabolic and anti-cancer.</p>

<p>Rev 2’-O-MOE-5MeC(Bz)-5’-amidite, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

<p>DNA Gyrase-IN-17 (Compound 5C) is an inhibitor of DNA gyrase. It demonstrates significant antimicrobial activity against a range of Gram-positive and Gram-negative strains, including Enterococcus faecium, Escherichia coli, and Pseudomonas aeruginosa, with a MIC value of 62.5 μg/mL. By inhibiting bacterial DNA gyrase, DNA Gyrase-IN-17 disrupts DNA replication. This compound can be useful in the development of antibiotics, particularly for studying resistant strains.</p>

<p>6-Amino-4-hydrozino-1-(2-deoxy-β-D-ribofuranosyl)-1H-pyrazolo[3,4-d]pyrimidine, a pyrimidine nucleoside analog, boasts a broad spectrum of biochemical and</p>

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

<p>RNA splicing modulator 2 (compound 256) is a RNA splicing modulator [1] .</p>

<p>Biotin-PEG8-Vidarabine is an antiviral PEG linker targeting herpes and varicella zoster with adenosine analog Vidarabine.</p>

<p>RNA Pol II-IN-2 (20iii) strongly inhibits Pol II (Ki=9.5 nM), is more toxic to CHO/HEK293 than α-amanitin.</p>

<p>5’-O-DMT-Ri can be used in the synthesis of oligoribonucleotides[1].</p>

<p>GSK299423: Antibiotic possibly effective against bacteria with New Delhi metal-β-lactamase, targeting topoisomerases.</p>