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>MRK-952 is a NUDIX hydrolase inhibitor. NUDIX enzymes play a role in cellular metabolism, homeostasis, and mRNA processing.</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>CDK5-IN-1: Potent CDK5 inhibitor (&lt;10 nM) used in kidney disease research.</p>

<p>PROTAC CDK9 degrader 4 is a CDK9 degrader that targets transcriptional regulation and has potential anticancer 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>Psammaplin A: marine-derived, inhibits HDAC/DNA methyltransferases, strong DAC1 blocker (IC50=0.9nM), antimicrobial against Gram-positive bacteria, anticancer.</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>DENV-IN-2 inhibits dengue virus replication (EC50: 0.016 nM), affects all serotypes (EC50: 0.013-0.029 nM). Derived from WO2018215315A1 6AB.</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>N3,5-Dimethyl-2’-O-(2-methoxyethyl) uridine, a purine nucleoside analog, exhibits broad antitumor activity, particularly against indolent lymphoid malignancies.</p>

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

<p>DHFR-IN-11 (compound 6b) is a DHFR inhibitor with demonstrated inhibitory efficacy against the M.</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>αVβ8-IN-1 is an αVβ8 integrin inhibitor that suppresses the growth of multiple tumour cell lines (EMT6, CT26, KPC, TKCC-10).</p>

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

<p>JH-XVI-178: potent CDK8/19 inhibitor with good pharmacokinetics, low clearance, moderate oral bioavailability.</p>

<p>AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.</p>

<p>LL-K8-22: potent CDK8/cyclin C degrader; DC50 ~2.5μM; hinders STAT1 phosphorylation; curbs E2F/MYC cancer pathways; for TNBC study.</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>huATN-658 (MNPR-101) is a humanized monoclonal antibody inhibitor targeting the urokinase-type plasminogen activator receptor (uPAR). It effectively disrupts the interaction between uPAR and integrins, thereby inhibiting tumor cell proliferation, invasion, and migration. huATN-658 shows potential for research in breast cancer, particularly in cases of triple-negative breast cancer.</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>Ac-MRGDH-NH2 is a pentapeptide containing the RGD sequence. It is utilized in the synthesis of the diastereomeric prodrugs Λ- and Δ-[Ru(Ph2phen)2(κS,κN-(Ac-MRGDH-NH2))]Cl2. In these prodrugs, Ac-MRGDH-NH2 serves as a photolabile protecting group for the cytotoxic diruthenium aqua complexes [Ru(Ph2phen)2(OH2)2]2+, offering integrin targeting and photoactivation properties. Consequently, Ac-MRGDH-NH2 can be applied in studies exploring tumor-targeted photoactivatable chemotherapy.</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>Chrysomycin A is an antibiotic that can be derived from Streptomyces.</p>

<p>SD49-7 is an inhibitor of histone lysine demethylase 4 (KDM4) with an IC50 of 0.19 µM.</p>

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

<p>Torvutatug is a human IgG1κ monoclonal antibody that acts against FOLR1.</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>LEB-03-146: WEE1 DUBTAC linking AZD1775 to OTUB1 via PEG2; stabilizes WEE1 in HEP3B cells.</p>

<p>5’-O-TBDMS-dA is a modified nucleoside and can be used to synthesize DNA or RNA.</p>

<p>WAY-647802 is a CDK inhibitor.</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>2’-Deoxy-2’-fluoroguanosine 5’-monophosphate triethyl ammonium, a purine nucleoside analog, exhibits broad antitumor activity specifically targeting indolent</p>

<p>PLK1-IN-2 is a PLK1 kinase inhibitor with an IC 50 value of 0.384 μM.</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>wrwyar-NH2 (TFA) serves as the control peptide for wrwycr-NH2.</p>

<p>Esperamicin A1, a powerful antitumor drug, comes from Actinomadura verrucosospora.</p>

<p>c-Myc inhibitor 7 degrades c-MYC, CK1α, GSPT1, IKZF1/2/3 proteins in tumors, for research on related diseases.</p>

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

<p>5'-O-DMT-2'-O-TBDMS-rI, a modified nucleoside, finds application in deoxyribonucleic acid (DNA) or nucleic acid synthesis.</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>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>Gly-Arg-Gly-Asp-Ser (GRGDS) GRGDS is a cell binding protein domain derived from the cell-binding region of fibronectin.</p>

<p>Selective Cdk4 degrader. Degrades Cdk4 in Molt-4 cells, with no effect on Cdk6 levels. Displays cereblon-dependent degradation.</p>

<p>5'-O-TBDMS-N2-ibu-dG: a nucleoside derivative with strong anti-BVDV activity, useful in lead compound synthesis.</p>

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

<p>Emofolin sodium, a synthetic folate analogue, inhibits DNA/RNA/protein synthesis by blocking dihydrofolate reductase.</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>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>dUTP trisodium (Deoxyuridine triphosphate) is a deoxyuridine phosphate having a triphosphate group at the 5'-position and can be used for PCR.</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>AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.</p>

<p>Mumefural, from Prunus mume fruit, hinders platelets, has anti-thrombotic properties, and boosts cognition.</p>

<p>Fluorocitabine HCl, a cytarabine analog, hydrolyzes into ara-FC and ara-FU, showing antitumor effects in leukemia and solid cancers.</p>

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

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

<p>ROCK-IN-32 is an effective Rho-kinase inhibitor.</p>

<p>Ascochlorin A, a compound with a dissociation constant (K D) of 3.29 μM, serves as a novel and potent human dihydroorotate dehydrogenase (hDHODH) inhibitor</p>

<p>5’(R)-C-Methyl-5-fluorouridine, a uridine analogue, possesses potential antiepileptic properties.</p>

<p>(S)-DI-87 is an isomer of DI-87, a oral dCK inhibitor，reduce dNTP production and cell cycle arrest. significantly inhibits tumor growth with thymidine.</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>2'-(2-Nitrobenzyl)-ATP trisodium is an rATP analogue that acts as a transcription terminator. It inhibits T7 RNA polymerase from continuing RNA chain extension.</p>

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

<p>JB-11 isethionate is a bioactive chemical.</p>

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

<p>8-NH2-ATP is an inactive derivative of adenosine triphosphate (ATP), synthesized from 8-NH2-Ado.</p>

<p>5-Caroxy uracil-1-yl acetic acid benzyl ester, a purine analog, inhibits DNA synthesis and induces apoptosis to combat lymphoid cancers.</p>

<p>Brr2-IN-2 (Compound 30) is an inhibitor of Brr2, exhibiting an IC50 of 42 nM against Brr2 ATPase.</p>

<p>'Rev 2’-O-MOE-C(Bz)-5’-amidite, a purine nucleoside analog, exhibits broad antitumor activity against indolent lymphoid malignancies.</p>

<p>1-(β-D-Xylofuranosyl)-N6-Isopentenyladenine is an adenosine analog.</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>Carboxy pyridostatin trifluoroacetate salt exhibits higher molecular specificity for RNA over DNA G4s.</p>

<p>13-TP is an inhibitor of SARS-CoV-2. It effectively suppresses in vitro RNA synthesis catalyzed by the central replication-transcription complex (C-RTC, nsp12-nsp7-nsp82) of SARS-CoV-2. 13-TP fully inhibits RdRp polymerase activity and obstructs the complete extension of some primer RNAs.</p>

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

<p>1-(β-D-Xylofuranosyl)-N6-(m-methoxybenzyl)adenine is an adenosine analog.</p>

<p>FF-10502, a pyrimidine analog of Gemcitabine, inhibits DNA polymerases α/β, targeting dormant cancer cells.</p>

<p>N7-Methylguanosine-5'-triphosphate-5'-adenosine (m7GpppA) diammonium, a dinucleotide cap analog, facilitates in vitro RNA transcription [1].</p>

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

<p>Erythromycin, a macrolide antibiotic, inhibits bacterial protein synthesis, effective against Streptococcus and Staphylococcus, and affects CYP3A4 metabolism.</p>

<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>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>α4β1 integrin (VLA-4) ligand (Kd ~ 12 nM). Non-fluorescent derivative of LDV FITC.</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>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>Gantofiban is a glycoprotein IIb/IIIa (GP IIb/IIIa) antagonist used in the treatment of cardiovascular disease and may be used to study thrombosis.</p>

<p>DA3: Fluorescent c-Myc inhibitor, targets c-MYC G-quadruplex (K D 16 μM), selective, suppresses c-MYC expression.</p>

<p>6-Amino-3-(furan-2-yl)-4-methoxy-1-(β-D-ribofuranosyl)-1H-pyrazolo[3,4-d]pyrimidine, a purine nucleoside analogue, exhibits broad antitumor activity by</p>

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

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

<p>6-Methoxypurine riboside is a purine analog with anti-lymphoma activity via DNA synthesis inhibition and apoptosis induction.</p>

<p>2'-Deoxy-2'-fluoro-1-uridine: an L-nucleoside, inhibits RNA viruses by blocking viral RNA polymerase.</p>

<p>UnyLinker 12 TEA is a versatile linker used in the synthesis of oligoribonucleotides.</p>

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