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>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>SNX7 (WAY-323879) inhibits CDKI pathway; useful for studying aging and related diseases.</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>5’-O-DMTr-5-MedC (Ac)-methyl phosphonamidite, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies</p>

<p>2’-Deoxy-2’-fluoro-N3-[(pyrid-2-yl)methyl]uridine, a uridine analogue, exhibits potential for antiepileptic applications.</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>dCeMM3 is a glue degrader that induces ubiquitination and degradation of cyclin K by promoting CDK12-cyclin K interaction with CRL4B ligase.</p>

<p>N1-Methyl-2’-beta-C-methyl adenosine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

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

<p>Demycarosyl-3D-β-D-digitoxosylmithramycin SK, an analog of Mithramycin, exhibits potent anti-tumor activity.</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>5'-GTP trisodium salt hydrate activates G proteins and is a precursor for DNA/RNA synthesis.</p>

<p>PP-C8: PROTAC CDK12-Cyclin K degrader with DC50s 416/412 nM; synergizes with PARP inhibitor against TNBC.</p>

<p>3,6-DMAD hydrochloride functions as an inhibitor for the IRE1α-XBP1 pathway within the unfolded protein response mechanism.</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>XT17 is an anthrone compound with broad-spectrum antibacterial activity, exerting its effects by disrupting the cell wall and inhibiting DNA synthesis. It demonstrates weak hemolytic activity, low cytotoxicity to mammalian cell lines, and a low rate of resistance development. Additionally, XT17 shows in vivo efficacy in a mouse corneal infection model induced by Staphylococcus aureus or Pseudomonas aeruginosa. Further docking studies confirm that XT17 forms a stable complex with bacterial gyrase. XT17 is suitable for research in the field of anti-infective agents.</p>

<p>ChlaDUB1-IN-2 (Compound 27a) serves as an inhibitor of the deubiquitinating enzyme ChlaDUB1 from Chlamydia trachomatis, with an IC50 of 0.97 μM. It also inhibits the formation of Chlamydia trachomatis inclusions, exhibiting an IIC50 of 25.6 μg/mL.</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>CD532 hydrochloride, potent Aurora A inhibitor (IC50=45 nM), hampers MYCN protein, changes AURKA's shape, aids cancer research.</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>N4-(3,3,3-Trifluoropropanoyl)cytidine, a cytidine analog, inhibits DNA methyltransferases, possibly anti-metabolic and anti-cancer.</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>m7GpppCpG, a trinucleotide cap analogue, is used for synthesizing RNA with cap 0 or cap 1 structures.</p>

<p>6-Amino-4-hydrozino-1-(2-deoxy-β-D-ribofuranosyl)-1H-pyrazolo[3,4-d]pyrimidine, a pyrimidine nucleoside analog, boasts a broad spectrum of biochemical and</p>

<p>EC0488 was used to synthesize EC0531, which has folic acid receptor specificity and anti-tumor activity.</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>Psammaplin A: marine-derived, inhibits HDAC/DNA methyltransferases, strong DAC1 blocker (IC50=0.9nM), antimicrobial against Gram-positive bacteria, anticancer.</p>

<p>5-Iminodaunorubicin: a quinone-altered anthracycline with antitumor effects, causing DNA breaks in cancer.</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>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>Brr2-IN-2 (Compound 30) is an inhibitor of Brr2, exhibiting an IC50 of 42 nM against Brr2 ATPase.</p>

<p>5’-O-DMTr-2’-O-MOE inosine 3’-P-methyl phosphonamidite, a purine nucleoside analog, exhibits extensive antitumor activity specific to indolent lymphoid</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>N7-Methylguanosine-5'-triphosphate-5'-adenosine (m7GpppA) diammonium, a dinucleotide cap analog, facilitates in vitro RNA transcription [1].</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>G13KS: UCHL1 ligand, deubiquitinase inhibitor; reduces monoubiquitin in glioblastoma cells.</p>

<p>5'-ODMT cEt G Amidite is a safe, effective nucleic acid analog with strong antisense activity.</p>

<p>N1-Methyl-2’-O-(2-methoxyethyl) guanosine, a purine nucleoside analog, exhibits broad antitumor activity against indolent lymphoid malignancies.</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>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>Bz-rC Phosphoramidite is a phosphinamide monomer utilized for oligonucleotide synthesis.</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>CDK6/9-IN-1, an oral dual inhibitor of CDK6/9, has IC50s of 40.5nM (CDK6) and 39.5nM (CDK9).</p>

<p>(R)-N-(2,3-Dihydro-1H-indenyl)-2-amino adenosine, a purine analog, targets lymphoid cancer via DNA synthesis inhibition and apoptosis.</p>

<p>CDK7-IN-7: Selective CDK7 inhibitor, IC50 &lt; 50 nM (Patent CN112661745A).</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>IBU-DC Phosphoramidite is used for synthesis of oligonucleotides.</p>

<p>BTO-1: Plk inhibitor effective in regulating phosphorylation.</p>

<p>N6-Benzoyl-3'-O-DMT-adenosine is a purine analog with antitumor effects by hindering DNA synthesis and inducing apoptosis.</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>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>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>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>Odulimomab: anti-LFA-1 antibody, inhibits T cell growth, protects against ischemic injury, used in transplant rejection research.</p>

<p>Ac-dA Phosphoramidite is a phosphinamide monomer utilized for oligonucleotide synthesis.</p>

<p>α2β1 Integrin Ligand Peptide TFA interacts with the integrin receptor on the cell membrane and enters the cell to mediate extracellular signaling.It is a</p>

<p>Potent Chk2 inhibitor with 3 nM IC50, 63-fold more selective over Chk1, affects 84 kinases, reduces DNA damage response and apoptosis in cells.</p>

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

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

<p>N7-Methyl-2’-O-(2-methoxyethyl) guanosine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</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>5-(2-Hydroxyethyl)-2',3'-di-O-toluoyl-2'-deoxyuridine, a purine nucleoside analog, exhibits widespread antitumor activity specifically against indolent lymphoid</p>

<p>Apcin A HCL is an Apcin-derived APC inhibitor that binds Cdc20 and hinders ubiquitination, useful for synthesizing PROTAC CP5V.</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>Trimethoprim hydrochloride: oral, broad-spectrum antibiotic, DHFR inhibitor, treats UTIs, shigellosis, pneumocystis pneumonia, may block Influenza A with zinc.</p>

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

<p>1-(β-D-Xylofuranosyl)-N6-Isopentenyladenine is an adenosine analog.</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>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>(+)-Glaucarubinone is a natural product that can be used as a reference standard.</p>

<p>'Rev 2’-O-MOE-A(Bz)-5’-amidite is a nucleoside analog specifically categorized within the purine subset, renowned for its wide-ranging antitumor efficacy</p>

<p>3’-Beta-C-Ethynyl-4-deoxyuridine is a purine nucleoside analog.</p>

<p>cis-Lomibuvir (cis-VX-222) is a selective HCV NS5B RdRp inhibitor with a Kd of 17 nM and an EC50 of 5.2 nM, targeting thumb pocket 2.</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>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>Remdesivir metabolite, antiviral nucleoside analog, effective against SARS-CoV and MERS-CoV.</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>BIO5192 hydrate: potent α4β1 inhibitor, binds selectively (Kd&lt;10 pM, IC50=1.8 nM), boosts murine HSPC mobilization 30x.</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>6-Methoxy-9-β-D-ethynyl-purine: a purine analog with antitumor action, impeding DNA synthesis and inducing apoptosis.</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>Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.</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>PD-1/PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1/PD-L1 interaction.</p>

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

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