Cell Cycle/Checkpoint

<p>N1-Methylpseudouridine-5′-triphosphate tetralithium, also known as 1-Methylpseudouridine-5′-triphosphate tetralithium, is a nucleobase-modified nucleotide.</p>

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

<p>Methylcarbamyl PAF C-8 is resistant to degradation by PAF-AH and has a half-life of over 100 minutes in platelet-poor plasma, exhibiting platelet aggregation activity. In NRK-49 cells overexpressing PAF receptor, it induces the expression of c-myc, c-fos, and activates mitogen-activated protein kinase (MAPK). Furthermore, Methylcarbamyl PAF C-8 can induce G1 phase cell cycle arrest. This compound shows potential for research in cardiovascular and anti-cancer applications.</p>

<p>m7GpppGpG, a trinucleotide cap, protects mRNA from 5′ exonucleases &amp; aids splicing and translation.</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>PP-C8: PROTAC CDK12-Cyclin K degrader with DC50s 416/412 nM; synergizes with PARP inhibitor against TNBC.</p>

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

<p>Rnase T1, an endonuclease, degrades single-stranded RNA to yield 3'-GMP oligonucleotides.</p>

<p>Compound LG-12, known chemically as PD-1/PD-L1-IN-50, is an inhibitor of PD-1/PD-L1. It enhances the secretion of IFN-γ, promotes the activation of CD8+ T cells, and activates T cell-mediated anti-tumor immunity.</p>

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

<p>Sarecycline hydrochloride is a narrow-spectrum tetracycline antibiotic with antimicrobial and anti-inflammatory activity.</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>Rifalazil (KRM-1648) is a benzophenazine antibiotic with antibacterial activity, useful for research on chlamydia infections.</p>

<p>JB-11 isethionate is a bioactive chemical.</p>

<p>N1-Methyl-2’-O-(2-methoxyethyl) guanosine, a purine nucleoside analog, exhibits broad antitumor activity against indolent lymphoid malignancies.</p>

<p>Anticancer agent 84 inhibits c-MYC transcription by stabilizing G4 structures, aiding cancer research.</p>

<p>ROCK-IN-5 (I-B-37) inhibits kinases like ROCK/ERK/GSK; may aid in cardiac and neuro disease studies.</p>

<p>L-Inosine, an endogenous purine nucleoside from adenosine metabolism, has anti-inflammatory, antinociceptive, immunomodulatory, and neuroprotective properties.</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>3'-dUTP trisodium, a nucleotide analogue, inhibits RNA polymerases I/II and UTP integration into RNA (Ki=2.0 μM).</p>

<p>TLR7 agonist 12, a purine nucleoside analog, inhibits DNA synthesis and induces apoptosis in lymphoid cancers.</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>3’-Deoxy-N1-Methyl inosine, a purine nucleoside analog, exhibits broad antitumor activity against indolent lymphoid malignancies.</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>2’-O-Methyl-5-methyluridine 5’-triphosphate (triethylammonium), a thymidine analog, exhibits insertional activity in replicated DNA.</p>

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

<p>BTO-1: Plk inhibitor effective in regulating phosphorylation.</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>Diguanosine 5′-triphosphate (Gp3G) is a kind of homodinucleotide from by GTP:GTP guanylyltransferase.</p>

<p>N3-(2S)-propyluridine is a uridine analog with potential as an antiepileptic and for antihypertensive agent research.</p>

<p>Mulnitorsen acts as an inhibitor of antisense non-coding mitochondrial RNA (ASncmtRNA) synthesis and serves as an antitumor agent [1].</p>

<p>EFdA-TP: potent HIV-1 RT inhibitor; acts via immediate/delayed chain termination (ICT/DCT) and multiple pathways.</p>

<p>3’-O-(4,4’-Dimethoxy trityl)-2’-O-(2-methoxyethyl)-5-methyluridine, a purine nucleoside analog, exhibits extensive antitumor properties against indolent</p>

<p>Ascochlorin A, a compound with a dissociation constant (K D) of 3.29 μM, serves as a novel and potent human dihydroorotate dehydrogenase (hDHODH) inhibitor</p>

<p>5’-O-DMT-N4-Ac-2’-F-dC is a modified nucleoside and can be used to synthesize DNA or RNA.</p>

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

<p>CDK12-IN-6, a pyrazolotriazine, strongly inhibits CDK12 (IC50 1.19 μM at 2 mM ATP), but not CDK2/Cyclin E or CDK9/Cyclin T1 (both IC50 &gt;20 μM).</p>

<p>Nuclease S1 breaks down ssDNA and RNA, trims protruding ends of dsDNA.</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>JH-XVI-178: potent CDK8/19 inhibitor with good pharmacokinetics, low clearance, moderate oral bioavailability.</p>

<p>Trimethoprim hydrochloride: oral, broad-spectrum antibiotic, DHFR inhibitor, treats UTIs, shigellosis, pneumocystis pneumonia, may block Influenza A with zinc.</p>

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

<p>2-Amino-6-O-methyl-2’-O-methyl purine riboside, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid</p>

<p>Carbazole belongs to the class of carbazole-based organic compounds. Carbazole can form novel DNA small groove complexes, inhibiting the synthesis of new DNA or RNA.</p>

<p>Fradafiban (BIBU-52) is a nonpeptide GPIIb/IIIa antagonist with Kd 148 nM for human platelets.</p>

<p>M7GpppAmpG is a trinucleotide 5′ cap analog, exhibiting capping efficiencies of 90% for the produced RNAs [1].</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>SR15006 is Krüppel-like factor 5 (KLF5) inhibitor (IC50 = 41.6 nM).</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>Heliquinomycin, a Streptomyces metabolite, inhibits DNA helicase (Ki=6.8 μM) and fights Gram-positive bacteria and various cancer cells.</p>

<p>USP7-IN-10 hydrochloride, also known as compound 1, is a potent inhibitor of the enzyme ubiquitin-specific protease 7 (USP7), exhibiting an IC50 value of 13.39</p>

<p>(1S,3R,5R)-PIM447 (dihydrochloride) an inhibitor of PIM(IC50 of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3).</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>1-(β-D-Xylofuranosyl)-N6-(m-methoxybenzyl)adenine is an adenosine analog.</p>

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

<p>N4-Acetyl-5’-O-(4,4’-dimethoxytrityl)-5-methyl-2’-deoxycytidine, a purine nucleoside analog, exhibits broad antitumor activity particularly against indolent</p>

<p>Ganodermaones B is a renal fibrosis inhibitor. Ganodermaones B inhibits TGF-β1-induced collagen I and fibronectin expression .</p>

<p>Chrysomycin A is an antibiotic that can be derived from Streptomyces.</p>

<p>Xylocytidine is a biochemical.</p>

<p>Biotin-PEG7-C2-NH-Vidarabine-S-CH3 is a PEG linker with Vidarabine, an anti-herpes/zoster antiviral.</p>

<p>Mumefural, from Prunus mume fruit, hinders platelets, has anti-thrombotic properties, and boosts cognition.</p>

<p>Uridine analogue with antitumor effects; inhibits DNA synthesis, induces apoptosis in lymphoid cancers.</p>

<p>23-Oxa-OSW-1 (SBF-1), a derivative of OSW-1, serves as a potent inhibitor of the osterol-binding protein (OSBP) with demonstrated antitumor activity [1] [2].</p>

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

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

<p>JB300 is a PROTAC-based compound that serves as a highly selective degrader of Aurora A, with a DC50 of 30 nM. It is utilized in cancer research. JB300 comprises the PROTAC target protein ligand MK-5108 [pink part], E3 ligase ligand Thalidomide-O-COOH [blue part], and PROTAC Linker Boc-NH-PEG2-C2-NH2 [black part]. The conjugate of the E3 ubiquitin ligase ligand and linker is Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc.</p>

<p>5-Iminodaunorubicin: a quinone-altered anthracycline with antitumor effects, causing DNA breaks in cancer.</p>

<p>6-Amino-4-hydrozino-2-(β-D-ribofuranosyl)-2H-pyrazolo[3,4-d]pyrimidine is a purine nucleoside analogue with broad antitumor activity, particularly against</p>

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

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

<p>5’-O-DMTr-2’,2’-difluoro-dC(Bz)-methyl phosphonamidite is a purine nucleoside analog with extensive antitumor activity against indolent lymphoid malignancies.</p>

<p>WAY-647802 is a CDK inhibitor.</p>

<p>Brr2-IN-2 (Compound 30) is an inhibitor of Brr2, exhibiting an IC50 of 42 nM against Brr2 ATPase.</p>

<p>Anticanceragent 263 (compound 7) is an effective anticancer agent. It binds with the G-quadruplex DNA (G4) sequence 22-mer Pu22 (a c-Myc DNA analog). As a structural modulator, Anticanceragent 263 significantly enhances the formation of protein α-helices and has the capacity to form a supramolecular network. Furthermore, Anticanceragent 263 exhibits no cytotoxicity.</p>

<p>Compound 19962-37-9, with CAS No. 19962-37-9, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound 19962-37-9 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>Potent α1β1 integrin inhibitor, 0.8 nM IC50 for IV collagen binding. Selective over other integrins. Inhibits FGF2 angiogenesis; antitumor in mouse models.</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>CBP501 Affinity Peptide, a Chk kinase inhibitor, disrupts G2 arrest triggered by DNA-damaging agents and is utilized in cancer research [1].</p>

<p>CDK2/4-IN-1 (compound B-4a) serves as both a CDK2/4 inhibitor and a microtubule polymerization inhibitor, making it useful in cancer research.</p>

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

<p>Lysidine (2-Methyl-2-iMidazoline) is a nucleoside rarely seen outside of tRNA. Lysidine has better translation fidelity.</p>

<p>Dafsolimab (SPV-T3a), an IgG2a murine monoclonal antibody (anti-CD3), induces cell death by modulating and activating the CD3/T cell receptor complex and is</p>

<p>CGP-74514,CDK1 inhibitor (IC50=25 nM). Induces G2/M arrest, apoptosis. Used in bladder cancer research.</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>5’-O-DMT-Ri can be used in the synthesis of oligoribonucleotides[1].</p>

<p>N6-Methyladenine (6-(Methylamino)Purine) is a modified purine commonly found in genomes of prokaryotes, protists, and plants.</p>

<p>CDK9/EZH2-IN-1 is a dual-target inhibitor of CDK9 and EZH2 with IC50 values of 83.9 nM and 108.6 nM, respectively. It induces apoptosis and causes DNA double-strand breaks (DSB). Additionally, CDK9/EZH2-IN-1 inhibits the proliferation of MKN45, MDA-MB-453, and SW620 cancer cells, with respective IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM.</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>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>2’-Fluoro-2’-deoxy-arabinoadenosine 5’-triphosphate (triethylamine) is a purine nucleoside analog with significant antitumor properties, particularly effective</p>

<p>P8RI acetate mimics CD31, activates CDP8RI, and suppresses the immune response by restoring CD31 pathway.</p>

<p>N6-Ethyl-2’-beta-C-ethynyl adenosine is a purine nucleoside analog.</p>

<p>Py-MAA-Val-Cit-PAB-DX8951, a purine toxin, serves as an intermediate in the synthesis of antibody-drug conjugates [1].</p>

<p>MS133 is a human bispecific antibody targeting CD133/PROM1 and CD3E. It is used in the study of colon cancer.</p>

<p>Ditercalinium chloride, an anticancer agent, inhibits human DNA polymerase gamma activity and can deplete mitochondrial DNA in both mouse and human cells. Additionally, Ditercalinium chloride is a potential ligand against the COMMD10-AP3S1 fusion protein [1] [2].</p>

<p>Compound 7, also known as 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine, serves as an inhibitor of protein kinases, displaying IC50 values of 0.092 μM for PKC-α, 0.26 μM for ROCK, and 0.77 μM for ASK1. Additionally, this compound exhibits significant cytotoxicity towards PC-3 cancer cells, with an IC50 of 0.16 μM [1].</p>

<p>A20FMDV2 is a highly selective αvβ6 integrin inhibitor with an IC 50 of 3 nM, demonstrating 1,000-fold greater selectivity for αvβ6 compared to other RGD-directed integrins like αvβ3, αvβ5, and α5β1. This compound can be derived from the foot-and-mouth disease virus and is suitable for radiolabeling, enabling PET imaging of αvβ6 integrin-positive tumors.</p>

<p>6-Thioguanosine (6-Mercaptoguanosine) is an active nucleoside and low molecular weight gel.6-Thioguanosine has immunosuppressive properties.</p>

<p>Integrin Binding Peptide, derived from fibronectin, holds the potential as an essential component for preparing PEG hydrogels.</p>

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

<p>Filanesib (ARRY-520) inhibits KSP, triggering mitotic arrest and cell death in dividing tumor cells.</p>

<p>ML-60218 inhibits RNA pol III in yeast/humans with IC50s of 32/27 μM; disrupts and prevents viroplasms.</p>

<p>N7-Methylguanosine-5'-triphosphate-5'-adenosine (m7GpppA) diammonium, a dinucleotide cap analog, facilitates in vitro RNA transcription [1].</p>

<p>PY314 is a CHO-expressed humanized monoclonal antibody targeting TREM2 with antitumor activity for the study of metastatic renal cell carcinoma.</p>

<p>HEMTACWEE1degrader-1 is a WEE1-targeting heterobifunctional chimeric degrader (HEMTAC) facilitated by HSP90, exhibiting an HSP90 enzyme inhibitory activity with an IC50 of 16.76 nM. It enhances the ubiquitination and subsequent degradation of WEE1, effectively blocking the G2/M cell cycle transition. This compound shows anticancer properties in patient-derived xenograft (PDX) models of acute myeloid leukemia (AML). HEMTACWEE1degrader-1 is utilized in AML research.</p>