Cell Cycle/Checkpoint

<p>Erythromycin thiocyanate, a macrolide from Streptomyces erythreus, binds 50S ribosomes, halting protein synthesis in bacteria.</p>

<p>DSPE-PEG1000-iRGD is a PEG compound made from DSPE and the αv-integrin-targeting peptide (iRGD). The iRGD peptide initially binds to αv-integrins and undergoes proteolytic cleavage within tumors to produce CRGDK/R, which interacts with neuropilin-1, thereby facilitating tumor targeting and penetration. DSPE-PEG1000-iRGD is useful for drug delivery applications.</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>Heliquinomycin, a Streptomyces metabolite, inhibits DNA helicase (Ki=6.8 μM) and fights Gram-positive bacteria and various cancer cells.</p>

<p>N1-Methylxylo-guanosine, a purine analog, targets lymphoid cancer via DNA synthesis inhibition and apoptosis.</p>

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

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

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

<p>TFMU-ADPr triethylamine is a substrate for PARG activity measurement, releasing a fluorophore to indicate PAR hydrolase activity.</p>

<p>5'-ODMT cEt G Amidite is a safe, effective nucleic acid analog with strong antisense activity.</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-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>IBU-DC Phosphoramidite is used for synthesis of oligonucleotides.</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>Rifalazil (KRM-1648) is a benzophenazine antibiotic with antibacterial activity, useful for research on chlamydia infections.</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>Sarecycline hydrochloride is a narrow-spectrum tetracycline antibiotic with antimicrobial and anti-inflammatory activity.</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>5’-O-TBDMS-dA is a modified nucleoside and can be used to synthesize DNA or RNA.</p>

<p>CDK7-IN-7: Selective CDK7 inhibitor, IC50 &lt; 50 nM (Patent CN112661745A).</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>Endo-1,4-β-xylanase (CtXyn11A) is a type of xylan hydrolase that hydrolyzes the β-1,4-glycosidic bond of the xylan molecule.</p>

<p>m7GpppUmpG, a trinucleotide cap analogue, enables RNA synthesis with cap 0 or 1 structures.</p>

<p>5-Methylcytidine 5′-triphosphate (5-Methyl-CTP), a modified nucleoside triphosphate, enhances translational properties and stability while reducing innate</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>Ceftriaxone: cephalosporin antibiotic, effective against Gram-positive/negative bacteria, with anti-inflammatory/antioxidant properties.</p>

<p>Rnase T1, an endonuclease, degrades single-stranded RNA to yield 3'-GMP oligonucleotides.</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>Phen-DC3 Trifluoromethanesulfonate targets G-quadruplexes and inhibits FANCJ/DinG helicases; IC50s: 65±6/50±10 nM.</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>Fibronectin CS1 peptide inhibits tumor metastasis, lacking RGD domain; may aid cancer therapy.</p>

<p>Lorutengitide is a transcription-regulating peptide with antiproliferative activity.</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>Rachelmycin, a potent antibiotic and antitumor agent from Streptomyces zelensis, binds to DNA's minor groove.</p>

<p>N6-Methyl-2’-O-(2-methoxyethyl) adenosine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid 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>Garenoxacin (BMS284756) is a novel oral des-fluoro(6) quinolone for the treatment of Gram-positive and Gram-negative bacterial infections.</p>

<p>CDP, a trisodium salt, helps synthesize DNA/RNA by aiding phosphoryl transfer from ATP to CMP via UMPK.</p>

<p>Anti-EMMPRIN/CD147 Antibody is a human-derived antibody expressed in CHO cells, targeting Basigin. For an isotype control, refer to HumanIgG1kappa, Isotype Control.</p>

<p>11H-Benzo[a]carbazole is a kinesin-like protein KIF11 inhibitor that can inhibit the viability of HeLa cells.</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>MYC-IN-2 is a protein-protein inhibitor targeting the MYC protein, designed for use in cancer research.</p>

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

<p>5-Aza-xylo-cytidine, a purine analog with antitumor effects, inhibits DNA synthesis and induces apoptosis in lymphoid cancers.</p>

<p>KIF2C-IN-1 (Compound 7S9) is a selective and potent small molecule inhibitor of KIF2C. It stabilizes the interaction between KIF2C and microtubule proteins, preventing the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel in Paclitaxel-resistant triple-negative breast cancer (TNBC) cells and, when combined with Paclitaxel, significantly reduces tumor growth in mouse models.</p>

<p>Chrexanthomycin C, orally active, binds DNA (G4C2)4 G4, Kd 2.8 mM, potential in ALS research.</p>

<p>DHFR-IN-8 (compound 6r), a dihydrofolate reductase (DHFR) inhibitor, disrupts purine and thymidylate biosynthesis critical for cell proliferation and growth.</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>CDK9-IN-25 (compound 4a), an imidazopyrazine derivative, functions as a CDK9 inhibitor with an IC50 of 0.24 μM.</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>