Ciclo celular / Checkpoint

<p>SNX7 (WAY-323879) inhibits CDKI pathway; useful for studying aging and related diseases.</p>

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

<p>Catumaxomab is a rat-mouse hybrid lgG2 monoclonal and bispecific antibody that binds to the antigens CD3 and EpCAM for malignant ascites in cancer patients.</p>

<p>FF-10502, a pyrimidine analog of Gemcitabine, inhibits DNA polymerases α/β, targeting dormant cancer cells.</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>CBR-2092 is a DNA-directed RNA polymerase and DNA topoisomerase inhibitor.</p>

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

<p>SMS 121 is a novel CD36 inhibitor that impairs fatty acid uptake and cell viability in acute myeloid leukaemia (AML) cells.</p>

<p>PT-129 is a RPOTAC degrader that targets the G3BP1/2NTF2 domain (protein-RNA interaction site), facilitating the breakdown of intracellular stress granules. It prevents the formation of stress granules in stressed cells and deconstructs existing ones, thereby disrupting ATF4 transmission and inhibiting cancer cell proliferation. Stress granules (SGs) are membraneless cytoplasmic compartments formed under stress, which aid in the transfer of ATF4 from fibroblasts to tumor cells, promoting fibroblast-related tumor growth. G3BP1/2 serve as central proteins in the SG network, and inhibiting them may reduce the stress resilience of cancer cells within the tumor microenvironment. PT-129 consists of a target protein ligand (red part) G3BP1/2-Targeting ligand-1, an E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a PROTAC linker (black part) Amino-PEG3-C2-acid; the E3 ligase ligand and linker form the complex Thalidomide-NH-PEG3-propionic acid.</p>

<p>CDK4/6-IN-23 (Compound 42) is a potent and selective inhibitor of CDK4/6, displaying an IC50 of 11 nM for CDK6. This compound significantly activates immune cells and enhances IL-3 production. In mice undergoing 5-FU chemotherapy, CDK4/6-IN-23 demonstrates dual bone marrow protection and immunomodulatory effects.</p>

<p>TAS-119 (TAS-2104) is an orally available, selective and potent inhibitor of Aurora A with an IC50 of 1.0 nM.TAS-119 also inhibits Aurora B with an IC50 of 95</p>

<p>Farletuzumab (MORAb-003), a humanized antibody, inhibits FRα-expressing cell growth for cancer research.</p>

<p>CTP Synthetase-IN-1 Ammonium salt is a CTPS inhibitor with potential antibacterial, anti-inflammatory, and antitumor activity for the study of SARS-CoV-2 viral infections</p>

<p>UnyLinker 12 TEA is a versatile linker used in the synthesis of oligoribonucleotides.</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>THZ1 2HCl: selective CDK7 allosteric inhibitor, IC50 3.2 nM, hinders cancer cell growth.</p>

<p>Clofarabine-5'-diphosphate (Clofarabine-DP) is a metabolite resulting from the phosphorylation of Clofarabine by deoxycytidine kinase (dCK). It can undergo further phosphorylation to become Clofarabine-5'-triphosphate, exhibiting cytotoxicity in cancer cells by inhibiting DNA synthesis and repair.</p>

<p>Ac-dA Phosphoramidite is a phosphinamide monomer utilized for oligonucleotide synthesis.</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>CDK6/9-IN-1, an oral dual inhibitor of CDK6/9, has IC50s of 40.5nM (CDK6) and 39.5nM (CDK9).</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>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>XY028-133 is a PROTAC-based CDK4/6 degrader for the study of tumors.</p>

<p>5'-O-DMT-ibu-dC can be used in the synthesis of oligodeoxyribonucleotides.</p>

<p>DNA Gyrase-IN-12 (Compound 6d) is an inhibitor of DNA gyrase. It exhibits antibacterial activity with MIC values ranging from 0.031 to 0.0625 μg/mL against Vancomycin-Intermediate Staphylococcus aureus (VISA) and Enterococcus faecium.</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>Gly-Arg-Gly-Asp-Ser (GRGDS) GRGDS is a cell binding protein domain derived from the cell-binding region of fibronectin.</p>

<p>IRE1-IN-2 (compound G15) functions as a potent inhibitor of IRE1. It effectively suppresses lipid accumulation induced by FFA, exhibiting an IC50 value of 2.06 μM.</p>

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

<p>JH-XVI-178: potent CDK8/19 inhibitor with good pharmacokinetics, low clearance, moderate oral bioavailability.</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>Anti-c-myc Antibody (9E10) is a chimeric mouse IgG1 antibody targeting human c-myc.</p>

<p>MRK-952 is a NUDIX hydrolase inhibitor. NUDIX enzymes play a role in cellular metabolism, homeostasis, and mRNA processing.</p>

<p>NXL-101, an oral/IV antibiotic for Gram-positive bacteria like MRSA, was discontinued by Novexel in 2008.</p>

<p>DSPE-PEG3000-iRGD is a PEG compound comprising DSPE and the αv-integrin targeting peptide (iRGD). The iRGD peptide binds to αv-integrin and undergoes proteolytic cleavage within tumors to produce CRGDK/R, interacting with neuropilin-1. This results in tumor targeting and penetration capabilities. DSPE-PEG3000-iRGD is applicable in drug delivery.</p>

<p>α-Methyl-DL-aspartic acid specifically inhibits argininosuccinate synthase (ASS), the rate-limiting enzyme in 1-citrulline-to-1-arginine recycling.</p>

<p>5’-O-TBDMS-dG is a modified nucleoside. 5’-O-DMT-2’-O-TBDMS-rI can be used in the synthesis of deoxyribonucleic acid or nucleic acid.</p>

<p>16,16-dimethyl Prostaglandin A1 is a useful organic compound for research related to life sciences.</p>

<p>TC113, a c(RGDyK)-linked Gemcitabine, targets αvβ3 integrin, entering A549 cells, and inhibits WM266.4 and A549 cell growth.</p>

<p>(+)-Glaucarubinone is a natural product that can be used as a reference standard.</p>

<p>N1-(2-Methyl)propyl pseudouridine, a purine analog, targets lymphoid cancer by inhibiting DNA synthesis and inducing apoptosis.</p>

<p>WRN inhibitor 17 (Compound 250) is an orally active inhibitor of Werner syndrome ATP-dependent helicase (WRN), specifically targeting the helicase domain activity of WRN. It holds potential for use in cancer research.</p>

<p>CD532 hydrochloride, potent Aurora A inhibitor (IC50=45 nM), hampers MYCN protein, changes AURKA's shape, aids cancer research.</p>

<p>CDK7-IN-5, a CDK7 inhibitor with an IC 50 value of less than 100 nM, exhibits potent anticancer properties (WO2015154022A1, Compound 104).</p>

<p>PROTAC CDK9 degrader-2, potent, selective, IC50 17 μM in MCF-7, wogonin-derived, targets CRBN.</p>

<p>5’-O-DMT-rU is a modified nucleoside and can be used to synthesize RNA.</p>

<p>Clofarabine-5'-triphosphate is a metabolite of Clofarabine, produced via phosphorylation by deoxycytidine kinase (dCK). It exhibits cytotoxicity in cancer cells by inhibiting DNA synthesis and DNA repair.</p>

<p>PROTACMTP3 degrade-1 is a PROTAC degrader for MYC.</p>

<p>N4-Benzoyl-3'-O-DMT cytidine analog inhibits DNA methyltransferases like Zebularine.</p>

<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>