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>Mps1-IN-6 is a potent Mps1 inhibitor that demonstrates antiproliferative and antitumor activities, exhibiting an IC50 of 2.596 nM [1].</p>

<p>RNA Splicing Modulator 3 (Compound 236) is an effective RNA splicing modulator, exhibiting an AC50 value of less than 100 nM [1].</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>N1-Methyl-2’-beta-C-methyl adenosine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

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

<p>Rev dC(Bz)-5'-amidite, a purine nucleoside analog with antitumor effects, inhibits DNA synthesis and induces apoptosis in lymphoid cancers.</p>

<p>6-Thioguanosine (6-Mercaptoguanosine) is an active nucleoside and low molecular weight gel.6-Thioguanosine has immunosuppressive properties.</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>Uridine triphosphate 13C9,15N2 sodium is an isotopically labeled.UTP is a key in RNA synthesis molecule a substrate for RNA polymerase.</p>

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

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

<p>Xanthosine-5'-Triphosphate (5'-XTP), a nucleotide derived from the deamination of purine bases, plays a crucial role in various biological processes.</p>

<p>Subquinocin is a CYLD inhibitor that suppresses deubiquitinating enzymes (DUB) of the USP family. By inhibiting CYLD, Subquinocin enhances the activation of the NF-κB and IFN pathways. Additionally, Subquinocin facilitates the activation of IRF3 and/or IRF7 in the RIG-I-mediated interferon pathway.</p>

<p>5-Methylcytidine 5′-triphosphate trisodium (5-Methyl-CTP trisodium), a modified nucleoside triphosphate, enhances translational properties and stability, while</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>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-DMT-2'-O-TBDMS-rI, a modified nucleoside, finds application in deoxyribonucleic acid (DNA) or nucleic acid synthesis.</p>

<p>SD49-7 is an inhibitor of histone lysine demethylase 4 (KDM4) with an IC50 of 0.19 µM.</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>N4-(3,3,3-Trifluoropropanoyl)cytidine, a cytidine analog, inhibits DNA methyltransferases, possibly anti-metabolic and anti-cancer.</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>Importazole is an inhibitor of the transport receptor importin-β. It specifically inhibits importin-β likely by altering its interaction with RanGTP.</p>

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

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

<p>RNA splicing modulator 2 (compound 256) is a RNA splicing modulator [1] .</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>1-(β-D-Xylofuranosyl)-N6-(m-trifluoromethylbenzyl)adenine is an adenosine analog.</p>

<p>3,5’-Bis(O-t-butyldimethylsilyl)-2’-O-methyl-5-methyl cytidine, a cytidine analog, inhibits DNA methyltransferases (e.g., Zebularine), exhibiting potential anti</p>

<p>CDK7-IN-2 HCl hydrate is a potent, specific CDK7 enzyme inhibitor with significant anti-cancer effects.</p>

<p>αVβ8-IN-1 is an αVβ8 integrin inhibitor that suppresses the growth of multiple tumour cell lines (EMT6, CT26, KPC, TKCC-10).</p>

<p>WAY-230563 is a serine/threonine kinase inhibitor that blocks CHK1/CHK2-mediated cell cycle checkpoints, leading to G2/M phase arrest in tumour cells</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>Cy5-dATP is a Cy5 -labeled dATP . Cy5-dATP can be incorporated into a DNA primer [1] [2] .</p>

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

<p>huATN-658 (MNPR-101) is a humanized monoclonal antibody inhibitor targeting the urokinase-type plasminogen activator receptor (uPAR). It effectively disrupts the interaction between uPAR and integrins, thereby inhibiting tumor cell proliferation, invasion, and migration. huATN-658 shows potential for research in breast cancer, particularly in cases of triple-negative breast cancer.</p>

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

<p>Tirandamycin A is a useful organic compound for research related to life sciences and the catalog number is T124996.</p>

<p>Erythromycin dihydrate, a macrolide antibiotic from Streptomyces erythreus, targets 50S ribosomal subunits, blocking protein synthesis.</p>

<p>Psammaplin A: marine-derived, inhibits HDAC/DNA methyltransferases, strong DAC1 blocker (IC50=0.9nM), antimicrobial against Gram-positive bacteria, anticancer.</p>

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

<p>m7Gpppm6AmpG, a trinucleotide mRNA 5’ cap analog, facilitates RNA synthesis in vitro [1].</p>

<p>SP27, a selective PROTAC, degrades PLK4 with a DC50 of 19.5 nM and may be utilized in breast cancer research [1].</p>

<p>6-O-Methyl-2’-O-methylinosine is a purine nucleoside analog known for its broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

<p>Heliquinomycin, a Streptomyces metabolite, inhibits DNA helicase (Ki=6.8 μM) and fights Gram-positive bacteria and various cancer cells.</p>

<p>N6-Benzoyl-3'-O-DMT-adenosine is a purine analog with antitumor effects by hindering DNA synthesis and inducing apoptosis.</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>12R-LOX-IN-2 is a 12R-LOX inhibitor that inhibits the hyperproliferation of psoriatic cells and can be used in the study of psoriasis and other skin diseases.</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>3’-O-DMT-N2-isobutyryl-2’-O-(2-methoxyethyl)guanosine, a purine nucleoside analog, exhibits broad antitumor activity particularly against indolent lymphoid</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>Chrysomycin A is an antibiotic that can be derived from Streptomyces.</p>

<p>dTTP sodium hydrate, a DNA synthesis component, is a nucleoside triphosphate.</p>

<p>DG1 (Compound 8Nc), a Thymidylate Synthase (TS) inhibitor, impedes angiogenesis and alters metabolic reprogramming in NSCLC cells, while effectively suppressing</p>

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

<p>m7GpppCpG, a trinucleotide cap analogue, is used for synthesizing RNA with cap 0 or cap 1 structures.</p>

<p>CDK2-IN-7 is a CDK2 inhibitor for treating cancer ( IC 50 &lt; 50 nM).</p>

<p>CW-2 is a PARP1 PROTAC degrader known for its potent antiproliferative effects against MDA-MB-231 cells (IC50 = 0.72 μM) and cisplatin-resistant cells (A549/CDDP: IC50 = 3.52 μM). It exhibits synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts its antitumor effects by inducing DNA damage, disrupting DNA repair, and triggering mitochondrial-dependent apoptosis (apoptosis).</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>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>TTK/PLK1-IN-1 (Formula I) is a dual inhibitor of TTK (threonine tyrosine kinase) and PLK1 (polo-like kinase 1), with IC₅₀ values of 7 nM and 72 nM respectively.</p>

<p>Nogalamycin is an anthracycline antibiotic with antitumor properties produced by soil bacteria Streptomyces nogalater.</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>6-Methoxypurine-9-β-D-5’(R)-C-methylriboside, an analog of hypoxanthine—a purine base predominantly found in muscle tissue and a metabolite generated when</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>Rachelmycin, a potent antibiotic and antitumor agent from Streptomyces zelensis, binds to DNA's minor groove.</p>

<p>wrwycr-NH2 (TFA) is a peptide that exhibits cytotoxic properties against various cancer cells, inducing DNA damage and cell cycle arrest without causing endoplasmic reticulum stress. It possesses antitumor activity, and its efficacy is enhanced when used in combination with DNA-damaging agents.</p>

<p>Bz-rC Phosphoramidite is a phosphinamide monomer utilized for oligonucleotide synthesis.</p>

<p>Agent 138: soluble benzothiazole, inhibits DNA gyrase/topoisomerase IV, targets Gram+ &amp; Gram- bacteria, binds plasma proteins.</p>

<p>EC0488 was used to synthesize EC0531, which has folic acid receptor specificity and anti-tumor activity.</p>

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

<p>3,6-DMAD hydrochloride functions as an inhibitor for the IRE1α-XBP1 pathway within the unfolded protein response mechanism.</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>5’-O-DMT-2’-O-TBDMS-Ac-rC is a modified nucleoside and can be used to synthesize DNA or RNA.</p>

<p>N4-(n-Palmitoyl)-4’-azido-2’-deoxy-2’-fluoro-arabinocytidine is a cytidine nucleoside analog.</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>Ficellomycin is an aziridine antibiotic produced by Streptomyces ficellus. Which shows high in vitro activity against Gram-positive bacteria.</p>

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

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

<p>5'-O-DMT-2'-O-TBDMS-Bz-rC, a modified nucleoside, is utilized in the synthesis of DNA or RNA.</p>

<p>R-BC154 acetate: selective α9β1 antagonist, high-affinity integrin probe for α9β1/α4β1 activity study.</p>

<p>L-5-Methyluridine, an L-configuration of 5-Methyluridine, is an endogenous methylated nucleoside present in human fluids.</p>

<p>EFdA-TP tetraammonium is a potent HIV-1 RT inhibitor and DNA synthesis blocker, acting as an ICT or DCT.</p>

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