Ciclo celular / Checkpoint

<p>FRα-targeting peptide C7 TFA is a selective peptide ligand for the folate receptor alpha (FRα) that specifically binds to FRα-expressing cells and has tumor-targeting capabilities in vivo. It is applicable in research related to tumor diagnosis and therapy.</p>

<p>Cyclothialidine is an inhibitor of DNA gyrase.</p>

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

<p>JB-11 isethionate is a bioactive chemical.</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>Solidagonic acid inhibits HSET, prevents fission yeast cell death, and hinders L. sativa and L. multiflorum seedling growth.</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>JAMM inhibitor 2 targets thrombin, Rpn11, MMP2 with IC50s 10, 46, 89 μM, aids cancer research.</p>

<p>11H-Benzo[a]carbazole is a kinesin-like protein KIF11 inhibitor that can inhibit the viability of HeLa cells.</p>

<p>MS7131 is a DUBTAC inhibitor that recruits USP1. It effectively reduces histone H3 lysine 27 trimethylation and significantly inhibits the proliferation and colony-forming ability of cancer cells.</p>

<p>Agent 138: soluble benzothiazole, inhibits DNA gyrase/topoisomerase IV, targets Gram+ &amp; Gram- bacteria, binds plasma proteins.</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>DSPE-PEG5000-cRGD is a PEG compound composed of DSPE and an αvβ3 targeting peptide (cRGD). The cRGD peptide has the ability to specifically bind to the αvβ3 present on the surfaces of numerous cancer cells and new vascular cells. DSPE-PEG5000-cRGD is useful for drug delivery applications.</p>

<p>5'-GTP trisodium salt hydrate activates G proteins and is a precursor for DNA/RNA synthesis.</p>

<p>PROTAC CDK9 degrader-5 selectively degrades CDK9 isoforms 42, 55 with DC50 of 0.10μM, 0.14μM via proteasome.</p>

<p>NUAK1-IN-1 (Compound 9) is an inhibitor of NUAK1 with an IC50 of 5.012 nM, as well as a CDK4 inhibitor. It is suitable for research related to cancer, neurodevelopmental disorders, and Alzheimer's disease.</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>6-Amino-4-methoxy-1-(2-deoxy-β-D-ribofuranosyl)-1H-pyrazolo[3,4-d]pyrimidine, a pyrimidine nucleoside analog, exhibits a broad spectrum of biochemical and</p>

<p>3’-β-C-Methyl-2-thiouridine, a purine nucleoside analog, exhibits extensive antitumor activity, particularly against indolent lymphoid malignancies.</p>

<p>CDK12/13-IN-2 (Compound 24) is a covalent inhibitor of CDK12 and CDK13, exhibiting IC50 values of 15.5 nM and 12.2 nM, respectively. It effectively inhibits the proliferation of breast cancer cells and can be utilized in the research of triple-negative breast cancer.</p>

<p>Antibacterialagent 271 is an antimicrobial compound that significantly inhibits Escherichia coli, with a minimum inhibitory concentration (MIC) of 2.2 μM. It disrupts bacterial membrane integrity, reducing metabolic activity. By binding to DNA grooves, it inhibits replication and induces reactive oxygen species (ROS) accumulation, leading to bacterial death. Antibacterialagent 271 shows considerable potential in combating bacterial infections.</p>

<p>N4-(n-Palmitoyl)-4’-azido-2’-deoxy-2’-fluoro-arabinocytidine is a cytidine nucleoside analog.</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>Xanthosine-5'-Triphosphate (5'-XTP), a nucleotide derived from the deamination of purine bases, plays a crucial role in various biological processes.</p>

<p>CDK9ligand 3 is a ligand for CDK9 and can be utilized in the synthesis of PROTAC degraders, specifically PROTAC CDK9degrader-11.</p>

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

<p>CDK1-IN-2 (cdk1 inhibitor 2) is a CDK1 inhibitor with IC50 of 5.8 μM.</p>

<p>KWR137 is a WRN degrader with an IC50 of 8 nM. It exhibits significant antiproliferative activity against MSI-H cells, with a GI50 of 509 nM for SW48 cells and 824 μM for HCT116. Additionally, KWR137 demonstrates antitumor growth effects in xenograft mouse models. This compound is applicable for cancer research.</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>5-Methylcytidine 5′-triphosphate (5-Methyl-CTP), a modified nucleoside triphosphate, enhances translational properties and stability while reducing innate</p>

<p>Thailanstatin C from Burkholderia thailandensis blocks pre-mRNA splicing, IC50 6.84 μM.</p>

<p>Potent αVβ3 integrin blocker, stops osteoclast binding &amp; bone loss, hinders platelet aggregation. Ki=0.27 nM, IC50s: 0.1 nM (bone), 30 nM (platelets).</p>

<p>THZ1 2HCl: selective CDK7 allosteric inhibitor, IC50 3.2 nM, hinders cancer cell growth.</p>

<p>L-5-Methyluridine, an L-configuration of 5-Methyluridine, is an endogenous methylated nucleoside present in human fluids.</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>N1-Benzoyl pseudouridine, a purine nucleoside analog, inhibits DNA synthesis and induces apoptosis to combat lymphoid cancers.</p>

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

<p>Evybactin: a selective DNA gyrase inhibitor for Mycobacterium tuberculosis (MIC 0.25 µg/mL), first of its kind.</p>

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

<p>Selective β-catenin degrader, xStAx-VHL peptide, lowers its levels in cells and inhibits tumor growth.</p>

<p>PD-1/PD-L1-IN-51 (Compound III-4) is an inhibitor of PD-1/PD-L1 (IC50: hPD-L1 at 2.9 nM). It binds directly to PD-L1, blocking the interaction between PD-1 and PD-L1, and enhancing the release of IFN-γ. Additionally, PD-1/PD-L1-IN-51 exhibits antitumor activity.</p>

<p>m7GpppUmpG, a trinucleotide cap analogue, enables RNA synthesis with cap 0 or 1 structures.</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>Uridine analogue with antitumor effects; inhibits DNA synthesis, induces apoptosis in lymphoid cancers.</p>

<p>AD16 (Acetamide) acts as an inhibitor of LINE-1 retrotransposon endonuclease, exhibiting an IC50 value of 4.7 μM. It decreases LINE-1 retrotransposition in senescent cells and mitigates the resulting DNA damage and inflammation.</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>2’-O-(2-Methoxyethyl)guanosine 5’-triphosphate (ammonium), a purine nucleoside analog, exhibits extensive antitumor properties, particularly against indolent</p>

<p>2’-O-Acetyl-5’-O-benzoyl-3’-O-(2-methoxyethyl) uridine, an analog of uridine known for its potential antiepileptic properties, is utilized in researching</p>

<p>GRGDSPK TFA is an RGD peptide, competitive inhibitor of integrin-fibronectin, used to research integrins in bone dynamics.</p>

<p>L82-G17 is an uncompetitive LigI-selective inhibitor in human cells with utility as a probe of the catalytic activity and cellular functions of LigI.</p>

<p>N6-Methyladenine (6-(Methylamino)Purine) is a modified purine commonly found in genomes of prokaryotes, protists, and plants.</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>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>RNA binder 1 (Compound 4b) is an RNA-binding agent capable of crossing the blood-brain barrier. It selectively binds to the G-quadruplex structure of the G4C2 repeat sequence RNA of the C9orf72 gene. This compound significantly reduces levels of the toxic polypeptides poly(GA) and poly(GP) in cells derived from amyotrophic lateral sclerosis (ALS) patients, while it has no significant impact on the antisense polypeptide poly(PR), demonstrating selectivity for sense RNA. RNA binder 1 is useful for studying ALS and frontotemporal dementia (FTD).</p>

<p>Aclacinomycin A has a wide range of applications in life science related research.</p>

<p>POLRMT-IN-1 (compound S7) is an inhibitor of POLRMT, specifically utilized in cancer-related research.</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>TFMU-ADPr triethylamine is a substrate for PARG activity measurement, releasing a fluorophore to indicate PAR hydrolase activity.</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>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>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>Clofarabine-5'-diphosphatetrisodium (Clofarabine-DP trisodium) is the sodium salt form of Clofarabine-5'-diphosphate. As a metabolic product of Clofarabine, it results from phosphorylation by deoxycytidine kinase (dCK). Clofarabine-5'-diphosphate trisodium can undergo further phosphorylation to form Clofarabine-5'-triphosphate, demonstrating cytotoxicity in cancer cells by inhibiting DNA synthesis and repair.</p>

<p>BRP, a peptide related to BRINP2, exhibits anti-obesity activity through the activation of FOS. It triggers FOS activation in the central nervous system, and its effect is independent of leptin, GLP-1 receptor, and melanocortin 4 receptor.</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>BLINK15 is a blood-brain barrier-permeable Cdk5 inhibitor. It reduces CDK5 activity in CDK5/p35 (IC50= 29.34 nM) and CDK5/p25 (IC50= 12.08 nM) complexes. Additionally, BLINK15 exhibits antidiabetic and neuroprotective effects. It lowers blood glucose levels in type 2 diabetes (T2D) mice, enhances cognitive abilities, and diminishes neurodegenerative lesions.</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>16,16-dimethyl Prostaglandin A1 is a useful organic compound for research related to life sciences.</p>

<p>O-Glycoprotease is a specific endoprotease for O-glycoproteins, capable of catalyzing the hydrolysis of peptide bonds directly adjacent to O-glycan structures in natural mucin-type O-glycosylated proteins. The sequence of O-Glycoprotease is derived from Akkermansia muciniphila, and it is recombinantly expressed in E. coli with a C-terminal 6×His tag. This enzyme maintains high activity within a pH range of 5.5 to 7.5, is resistant to 1 M NaCl, but is highly sensitive to EDTA (0.5 mM EDTA) and can be inhibited by Zn2+.</p>

<p>Deoxythymidine-5'-triphosphate (dTTP) is a nucleoside triphosphate involved in DNA synthesis.</p>

<p>NXL-101, an oral/IV antibiotic for Gram-positive bacteria like MRSA, was discontinued by Novexel in 2008.</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>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>LY2812223: selective mGlu2 agonist; binds mGlu2/mGlu3 (Ki=144/156 nM).</p>

<p>Fluorocitabine HCl, a cytarabine analog, hydrolyzes into ara-FC and ara-FU, showing antitumor effects in leukemia and solid cancers.</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>CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 of 0.55 nM. It enhances the effects of DNA-damaging agents on tumor cells and exhibits synergistic anticancer activity with Gemcitabine.</p>

<p>8-iso Prostaglandin F1β,inducet vasoconstrictor effects in (PA), (PV) and (MA) through the activation of TXA2R, tyrosine kinase and Rho kinase.</p>

<p>PROTAC CDK9 degrader-7 is a proteolysis-targeting chimera (PROTAC) specifically designed to target and mediate the degradation of Cyclin-Dependent Kinase 9 (</p>

<p>PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0/G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)</p>

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

<p>DHFR-IN-18 (compound 19D) is a DHFR inhibitor utilized in leukemia-related research.</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>(Gly0.8Nap0.2)20 is a dual-target compound effective against fungal membranes and DNA. It exhibits antimicrobial properties.</p>

<p>BAY-728 serves as a negative control for BAY-805, a potent and selective inhibitor of USP21 [1].</p>

<p>N6-Benzoyl-9-β-D-arabinofuranosyladenine hydrate is the hydrated form of N6-Benzoyl-9-β-D-arabinofuranosyladenine, which is an adenine nucleoside analog. Such adenosine analogs often function as vasodilators for smooth muscle and have been shown to inhibit cancer progression. Popular related products include Adenosine phosphate, Acadesine, Clofarabine, Fludarabine phosphate, and Vidarabine.</p>

<p>5’-DMTr-3’dA(Bz)-methylphosphonamidite, a purine nucleoside analog, exhibits wide-ranging antitumor activity, specifically targeting indolent lymphoid</p>

<p>NUAK1-IN-2 (Compound 24) is an inhibitor of NUAK1 with an IC50 of 3.162 nM, as well as an inhibitor of CDK2/4/6. It is applicable in research related to cancer, neurodevelopmental disorders, and Alzheimer's disease.</p>

<p>DSPE-PEG2000-iRGD is a PEG compound composed of DSPE and the αv-integrin targeting peptide (iRGD). The iRGD peptide binds to αv-integrins and subsequently undergoes proteolytic cleavage within tumors, producing CRGDK/R, which interacts with neuropilin-1. This compound is characterized by its tumor-targeting and tumor-penetrating properties, making DSPE-PEG2000-iRGD suitable for drug delivery applications.</p>

<p>Substrate '[pSer2, pSer5, pSer7]-CTD (TFA)' for CDK7 phosphorylates RNA Pol II CTD at ser2, 5, 7.</p>

<p>CDK9-IN-25 (compound 4a), an imidazopyrazine derivative, functions as a CDK9 inhibitor with an IC50 of 0.24 μM.</p>

<p>N-Methylisatoic anhydride is a 2'-OH selective acylation agent of RNAs.</p>

<p>m7GpppCmpG, a trinucleotide cap analogue, enables RNA manufacturing with cap 0 or cap 1 structures.</p>

<p>PKMYT1-IN-6 (compound 98) is an inhibitor of PKMYT1, exhibiting an IC50 of less than 50nM.</p>

<p>Emofolin sodium, a synthetic folate analogue, inhibits DNA/RNA/protein synthesis by blocking dihydrofolate reductase.</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>5-Iminodaunorubicin: a quinone-altered anthracycline with antitumor effects, causing DNA breaks in cancer.</p>

<p>2’-Deoxy-2’-fluoro-N3-(n-dodecyl)uridine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

<p>5’-O-TBDMS-Bz-dA is a nucleoside with protective and modification effects.</p>

<p>Cy5-dATP is a Cy5 -labeled dATP . Cy5-dATP can be incorporated into a DNA primer [1] [2] .</p>

<p>Lobucavir inhibits the replication of the HIV virus in T cells, monocytes &amp; macrophages in vitro by inhibiting DNA polymerase and viral DNA synthesis.</p>

<p>HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt inhibits pre-miR-21 RNA, potential for cancer research.</p>

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

<p>TMX-2138 is a CDKs PROTAC degrader, with IC50 values of 8.7 nM for CDK1/cyclinB, 10.9 nM for CDK2/cyclinA, 7.0 nM for CDK5/p25, and 25.7 nM for CDK9/cyclinT1. It enhances the ubiquitination and degradation of CDKs and is utilized for ovarian cancer research.</p>

<p>DHFR-IN-20 (Compound LA1) is an inhibitor of dihydrofolate reductase (DHFR) targeting the malignant strains of the malaria parasite. It exhibits inhibition constants (Kis) of 0.16 nM, 0.30 nM, and 6.6 nM for PfDHFR-WT, PfDHFR-QM, and HsDHFR, respectively. Additionally, DHFR-IN-20 demonstrates antimalarial activity, with IC50 values of 1.4 nM against parasites carrying the wild-type (TM4/8.2) PfDHFR enzyme and 1.6 μM against those with the quadruple mutation (V1/S)PfDHFR.</p>

<p>AR-13324 analog mesylate is an inhibitor of Rho-kinase and a norepinephrine transporter and reduces intraocular pressure in normotensive monkey eyes.</p>

<p>CDK2, a Ser/Thr kinase, is akin to yeast cdc28 and human Cdk1, crucial for cell division.</p>

<p>7-Deazaxanthine (7DX) is an inhibitor of thymidine phosphorylase (TPase) and reduces TPase activity in a concentration-dependent manner, with an IC50 value of 40 μM. Additionally, 7-Deazaxanthine exhibits significant anti-angiogenic properties.</p>

<p>Centaureidin is a useful organic compound for research related to life sciences. The catalog number is T125588 and the CAS number is 17313-52-9.</p>