Ciclo celular/Ponto de verificação

<p>MC-Val-Cit-PAB-Ispinesib (Compound 509) is a potent Eg5 inhibitor and a click chemistry reagent [1].</p>

<p>CDK7-IN-22 (compound 101) is a selective CDK7 inhibitor that exhibits antitumor activity, demonstrating specificity for CDK7 [1].</p>

<p>PF-6808472 is a cell-permeable covalent kinase probe, reacts with conserved lysine residues within the ATP-binding site of kinases.</p>

<p>COH1 is a ribonucleotide reductase (RR) inhibitor utilized in research pertaining to cancer, mitochondrial diseases, and neurodegenerative disorders [1].</p>

<p>Riviciclib, a CDK inhibitor (CDK9/T1, CDK4/D1, CDK1/B), has IC50s: 20, 63, 79 nM respectively, and fights cisplatin-resistant tumors.</p>

<p>α7β1 Integrin Modulator-1 is a potent modulator with research potential for muscular dystrophy [1].</p>

<p>DNA Gyrase-IN-8 is a potent inhibitor of DNA gyrase, demonstrating antimicrobial activity with an IC50 of 8.45 µM [1].</p>

<p>Tnp 351 is a novel antifolate drug being assessed for chemotherapy of lung cancer.</p>

<p>CI 972 anhydrous is an inhibitor of purine nucleoside phosphorylase (PNP) (Ki: 0.83 μM) used as a T cell-selective immunosuppressive agent.</p>

<p>KY386 is a potent and selective DHX33 helicase inhibitor with an IC50 value of 19 nM.</p>

<p>BMT-090605: AAK1 inhibitor (IC50=0.6 nM), also affects BIKE (45 nM) and GAK (60 nM), has antinociceptive properties.</p>

<p>PDD00031705 is a benzimidazolone core cell-inactive Poly (ADP-ribose) glycohydrolase (PARG) inhibitor.</p>

<p>USP7-IN-13 (Compound 101), a USP7 inhibitor, exhibits an IC50 range of 0.2-1 μM and is applicable in researching multiple myeloma [1].</p>

<p>PD 0332991, an unsymmetrical indolocarbazole compound, is cell-permeable and exhibits antiproliferative effects by functioning as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk4/D1 (IC 50 = 76 nM). Although it can inhibit other Cdks, such as Cdk2/E and Cdk1/B, effectiveness requires higher concentrations (IC 50 = 520 nM and 2.1 µM, respectively) and demonstrates minimal activity against CaMKII, PKA, or GSK-3β (IC 50 ≥ 12.4 µM). PD 0332991 efficiently inhibits tumor cell growth in HCT-116 and NCI-H460 cell lines with an IC 50 &lt; 3.0 µM, primarily through blocking Rb phosphorylation and inducing G1 cell cycle arrest.</p>

<p>3-Cyanovinylcarbazole phosphoramidite: an antiviral, hinders viral DNA synthesis, modifies ribonucleotides.</p>

<p>Methotrexate-gamma-aspartate has growth inhibitory effects. It is used in antibody-targeted liposomes.</p>

<p>5'-ODMT cEt N-Bz A Phosphoramidite Amidite, a locked nucleic acid (LNA) analogue, exhibits hybridization and mismatch discrimination capabilities similar to LNA, and shows resistance to exonuclease digestion [1].</p>

<p>CDK9-IN-9 is a potent and selective CDK9 inhibitor (IC50: 1.8 nM) with anti-cancer activity. It inhibits CDK2 (IC50: 155 nM).</p>

<p>DCB-3503, a tylophorine analog, may fight cancer and aid immunosuppression by hindering protein synthesis and modulating HSC70 ATPase function.</p>

<p>Halofuginone hydrochloride (RU-19110), a derivative of Febrifugine, functions as a competitive inhibitor of prolyl-tRNA synthetase, displaying a Ki value of 18.3 nM. This compound effectively inhibits type-I collagen synthesis, providing therapeutic benefits in osteoarthritis (OA) by impeding TGF-β signaling. Additionally, it serves as a potent pulmonary vasodilator, mainly through the activation of Kv channels and the inhibition of various calcium channels including voltage-gated, receptor-operated, and store-operated ones. Beyond its vascular effects, Halofuginone hydrochloride exhibits a broad spectrum of biological activities, including anti-malarial, anti-inflammatory, anti-cancer, and anti-fibrotic properties, supported by multiple studies.</p>

<p>Palmitoyl 3-carbacyclic phosphatidic acid, a palmitoylated Carba-like cyclophosphatidic acid and LPA (lysophosphatidic acid) analog, possesses distinct biological activities compared to LPA, including the inhibition of RhoA activation and melanoma cell migration. This compound has demonstrated efficacy in inhibiting experimental lung metastasis and reducing tumor nodule counts in a B16-F0 xenograft mouse model [1].</p>

<p>KSP-IA is a potent, specific, allosteric, and cell-active KSP inhibitor.</p>

<p>Antifolate C1 blocks purine creation, favors uptake via folate receptors/PCFT over RFC.</p>

<p>Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological and solid tumors.</p>

<p>L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.</p>

<p>WRN Inhibitor 1 (example 7) is an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN), selectively targeting its helicase domain.</p>

<p>hDHODH-IN-1 is an inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an anti-inflammatory effect.</p>

<p>CDK9-IN-19: Potent CDK9 inhibitor, anti-cancer, moderate pharmacokinetics, low hERG impact, effective in AML research.</p>

<p>PD-L1-IN-2, a Naamidine J derivative, serves as a promising antineoplastic immunomodulator by hindering PD-L1 activity.</p>

<p>5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor and other folate related enzymes inhibitor.</p>

<p>T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.</p>

<p>Pen is an oral cancer drug that blocks DNA synthesis by inhibiting key enzymes and integrating into DNA.</p>

<p>RAD51-IN-4, a potent RAD51 inhibitor, may be useful in researching mitochondrial defect-related conditions.</p>

<p>L 738167 is a potent antagonist of the long-acting fibrinogen receptor.</p>

<p>5,11-methenyltetrahydrohomofolate blocks GAR &amp; AIR transformylase; used as an anti-purine drug.</p>

<p>Lotrafiban hydrochloride is an platelet glycoprotein IIb/IIIa blocker with oral activity.</p>

<p>ICAM-1-IN-1 is a potent and selective E-selectin(IC50 = 7 nM) and ICAM-1(IC50 = 5 nM) inhibitor.</p>

<p>PLK4-IN-4 (compound 22), a potent inhibitor of PLK4, exhibits an IC50 value of 7.9 nM, suggesting its potential use in cancer research [1].</p>

<p>Myt1-IN-3 is a potent inhibitor of Myt1 (IC50 &lt;10 nM) [1].</p>

<p>5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase (IC50s</p>

<p>Wee1 Inhibitor I is an ATP-binding site-targeting Wee1 inhibitor.</p>

<p>VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).</p>

<p>Diazoketone methotrexate is an analog of methotrexate with potential antitumor activity.</p>

<p>8-Azahypoxanthine (NSC-22709) inhibits hypoxanthine-guanine-xanthine phosphoribosyltransferase and has antimalarial properties.</p>

<p>USP1-IN-6 (Compound 11) functions as a potent USP1 inhibitor, exhibiting an IC50 value of less than 50 nM.</p>

<p>AR-13503, a Netarsudil metabolite, is a ROCK inhibitor, potentially treating glaucoma and lowering eye pressure.</p>

<p>Mefenidil (McN-2378), a selective cerebral vasodilator, was shown to increase CBF in healthy brains without stimulating O2 uptake in a dog anesthesia model.</p>

<p>Lotrafiban: Oral GP IIb/IIIa inhibitor for treating coronary and cerebrovascular disease.</p>

<p>CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).</p>

<p>LNA-Adenosine (LNA-A) is a nucleoside analogue that acts as a ligand for adenosine A3 receptors.</p>