Cell Cycle/Checkpoint

<p>RNA Splicing Modulator 1 (Compound 233) is a modulator of RNA splicing, 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>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>CDK5-IN-1: Potent CDK5 inhibitor (&lt;10 nM) used in kidney disease research.</p>

<p>Lorutengitide is a transcription-regulating peptide with antiproliferative activity.</p>

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

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

<p>Torvutatug is a human IgG1κ monoclonal antibody that acts against FOLR1.</p>

<p>5-Methylcytidine 5′-triphosphate trisodium (5-Methyl-CTP trisodium), a modified nucleoside triphosphate, enhances translational properties and stability, while</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>UnyLinker 12 TEA is a versatile linker used in the synthesis of oligoribonucleotides.</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>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>Pseudouridimycin: a C-nucleoside antibiotic, inhibits bacterial RNAP, targets Gram-negative and Gram-positive bacteria.</p>

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

<p>3'-dUTP trisodium, a nucleotide analogue, inhibits RNA polymerases I/II and UTP integration into RNA (Ki=2.0 μM).</p>

<p>LXY3 (LXY2) is a VLA-3 blocking peptide that inhibits the interaction of neutrophil surface integrin α3β1 (VLA-3) with laminin in the basement membrane, thereby preventing neutrophil migration across the tumor vascular basement membrane barrier. LXY3 is employed to block the neutrophil-mediated release of nanoparticles from the perivascular pool into the tumor stroma and is frequently used for targeted imaging in breast cancer.</p>

<p>PROTAC CDK9 degrader 4 is a CDK9 degrader that targets transcriptional regulation and has potential anticancer activity.</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>Ac-dA Phosphoramidite is a phosphinamide monomer utilized for oligonucleotide synthesis.</p>

<p>JH-XVI-178: potent CDK8/19 inhibitor with good pharmacokinetics, low clearance, moderate oral bioavailability.</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>5’-O-DMT-N4-Bz-2’-F-dC is a nucleoside with protective and modification effects.</p>

<p>The Asp-Gly-Glu-Ala (DGEA) amino acid domain of type I collagen interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular</p>

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

<p>Heliquinomycin, a Streptomyces metabolite, inhibits DNA helicase (Ki=6.8 μM) and fights Gram-positive bacteria and various cancer cells.</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-DMT-ibu-dC can be used in the synthesis of oligodeoxyribonucleotides.</p>

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

<p>Chrysomycin A is an antibiotic that can be derived from Streptomyces.</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>DHFR-IN-11 (compound 6b) is a DHFR inhibitor with demonstrated inhibitory efficacy against the M.</p>

<p>pNP-ADPr: Used in PARG &amp; ARH3 activity assays; aids in PARP enzyme research.</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>Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.</p>

<p>5-Methylcytidine 5′-triphosphate (5-Methyl-CTP), a modified nucleoside triphosphate, enhances translational properties and stability while reducing innate</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>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>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>PDI-IN-4 (Compound 14d) is a protein disulfide isomerase inhibitor with an IC50 value of 0.48 μM. It prevents platelet aggregation and thrombosis by reducing the activation of GPIIb/IIIa, without causing significant cytotoxicity. PDI-IN-4 is applicable in thrombosis research.</p>

<p>Ceftriaxone: cephalosporin antibiotic, effective against Gram-positive/negative bacteria, with anti-inflammatory/antioxidant properties.</p>

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

<p>Ara-CTP, active Cytarabine metabolite, inhibits DNA synthesis, predicts leukemic chemosensitivity.</p>

<p>3'-Deoxy-GTP (3′-Deoxyguanosine 5′-triphosphate) trisodium, an analog of GTP, functions as an RNA chain terminator, thereby inhibiting RNA synthesis. It is capable of suppressing dengue virus DENV NS5 RdRp with an IC50 value of 0.02 μM.</p>

<p>c-Myc inhibitor 7 degrades c-MYC, CK1α, GSPT1, IKZF1/2/3 proteins in tumors, for research on related diseases.</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>Antibacterial Agent 144 (compound 8e) exhibits superior efficacy against multi-resistant Staphylococcus aureus compared to Chloromycin and Amoxicillin.</p>

<p>CDK9 inhibitor HH1 (8019-9719) is an inhibitor of the human CDK2-cyclin A2 complex with an IC50 value of 2 μM.</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>Py-MAA-Val-Cit-PAB-DX8951, a purine toxin, serves as an intermediate in the synthesis of antibody-drug conjugates [1].</p>