Cell Cycle/Checkpoint

<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>Galidesivir hydrochloride is an inhibitor of viral RNA-dependent RNA polymerase (RdRp). It inhibits SARS-CoV-2 by tightly binding to its RdRp.</p>

<p>Zaurategrast is an effective and oral-effective inhibitor of the α4-integrin.</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>Kif15-IN-2 is a kinesin Kif15 inhibitor with potential anticancer activity and can be used in prostate cancer research.</p>

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

<p>Xylocydine is a novel Cdk inhibitor that induces apoptosis in HCC, suppresses tumor growth, and is non-toxic to other tissues.</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>UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.</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>AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.</p>

<p>Cdc7-IN-12, a sub-1 nM CDC7 inhibitor, may aid cancer research; hinders COLO205 cell growth (IC50: 100-1000 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>hDHODH-IN-1 is an inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an anti-inflammatory effect.</p>

<p>EHT 5372 inhibits DYRK kinases; IC50: 0.22-221 nM for DYRK1A/B, DYRK2/3, CLK1/2/4, GSK-3α/β.</p>

<p>Butylparaben sodium significantly impacts the later phases of spermatogenesis in the testes by impairing hormonal regulation and/or RNA and protein synthesis [1</p>

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

<p>T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.</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>ROCK-IN-10 (compound 50) serves as a powerful inhibitor of ROCK, exhibiting IC50 values of 6 nM for ROCK1 and 4 nM for ROCK2, respectively. It demonstrates over 100-fold selectivity towards ROCK1 and ROCK2 when compared to other kinases [1].</p>

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

<p>JNJ-26076713, an oral alpha V integrin blocker, may treat macular edema, AMD, and diabetic retinopathy.</p>

<p>Myt1-IN-2, a highly potent Myt1 inhibitor, exhibits remarkable anticancer properties with an IC50 value below 10 nM (WO2021195782A1; compound 28) [1].</p>

<p>Synstatin (92-119) serves as an anti-tumor agent by suppressing angiogenesis and cancer cell invasion, chiefly through the down-regulation of integrin αvβ3 and</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>CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).</p>

<p>PVZB1194, a biphenyl-type inhibitor of Kinesin spindle protein Eg5 (KIF11), exhibits anticancer potential by inducing cell cycle arrest and apoptosis through</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>USP1-IN-6 (Compound 11) functions as a potent USP1 inhibitor, exhibiting an IC50 value of less than 50 nM.</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>SB-267268: αvβ3 inhibitor (IC50: 0.68 nM human, 0.29 nM mouse), blocks αvβ3/αvβ5 integrins (Ki: 0.9 nM human, 0.5 nM monkey αvβ3, 0.7 nM human αvβ5).</p>

<p>CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor (IC50: 2.3 nM).</p>

<p>Inixaciclib is a potent CDK inhibitor, can be used to research anticancer.</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>Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist. It has a binding affinity of 18 nM and as a novel anticancer agent.</p>

<p>Litronesib is a selective inhibitor of mitosis-specific kinesin Eg5. It also has antitumor activity.</p>

<p>Tirofiban HCl is an antagonist of platelet glycoprotein-IIb/IIIa receptor.</p>

<p>ML 315, a selective dual inhibitor targeting CDK (Cyclin-Dependent Kinase) and DYRK (Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase) with IC50 values of 68 nM and 282 nM, respectively, is utilized in research pertaining to cancer and neurological diseases [1].</p>

<p>CDK4-IN-2 (A17) is a potent inhibitor of CDK4, exhibiting K i and IC 50 values of less than 10 nM and is utilized in cancer research [1].</p>

<p>Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective PKC inhibitor. It is also a potent CDK2 antagonist (IC50: 200 nM).</p>

<p>BMT-090605 HCl: AAK1 inhibitor (IC50=0.6 nM), also targets BIKE (IC50=45 nM) &amp; GAK (IC50=60 nM), with potential in neuropathic pain research.</p>

<p>αvβ6 Integrin Inhibitor 2 is a potent inhibitor of αvβ6 integrin, demonstrating an inhibition concentration (IC50) of 96.5 nM.</p>

<p>USP7-IN-12 (compound 1) is a potent, orally active inhibitor of Usp7, exhibiting an IC50 of 3.67 nM and demonstrating antiproliferative activity [1].</p>

<p>NTRC 0066-0 is a TTK inhibitor that can be used in cancer research.</p>

<p>Trovafloxacin: broad-spectrum fluoroquinolone, blocks DNA gyrase/topoisomerase IV and PANX1 channel (IC50=4μM).</p>

<p>Thymectacin (NB 1011) is a selective thymidine synthase (TS) inhibitor with anticancer activity for the study of colon cancer and solid tumors.</p>

<p>CF53: potent, selective oral BET inhibitor; Ki &lt;1 nM, Kd 2.2 nM, IC50 2 nM for BRD4 BD1; high affinity for BRD2/3/4/BRDT; effective anti-tumor agent.</p>

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

<p>SMN-C3 (MV8T2MCK57) is an orally active modulator of SMN2 splicing, and has the potential to treat spinal muscular atrophy (SMA).</p>

<p>AZD4573 is an effective and selective CDK9 inhibitor (IC50: &lt;4 nM). It enables transient target engagement for the treatment of hematologic malignancies.</p>

<p>LY3295668 (AK-01) is a selective inhibitor of Aurora A with Kis of 0.8 nM and 1038 nM for Aurora A and B, respectively.</p>

<p>DHX9-IN-2 is an inhibitor targeting ATP-dependent RNA de-helicase A (DHX9) with anticancer and antitumor activity for cancer research.</p>

<p>BDP9066 is a potent and selective MRCK inhibitor, inhibits MRCKβ and MRCKα/β, and can be used for the prevention and treatment of skin cancer.</p>

<p>Cdk1/2 Inhibitor III is a selective Cdk1/2 inhibitor with an IC50 value of 2.1 μM against CDK1/cyclin B.</p>

<p>αvβ1 integrin-IN-1 is a potent and selective inhibitor of αvβ1 integrin (IC50 of 0.63 nM) with antifibrotic effects.</p>

<p>Roxifiban acetate（DMP 754 acetate） is a potent GP IIb / IIIa antagonist that exhibits antiplatelet aggregation activity via immune mediation and can be used in</p>

<p>CFI-402257 is a selective inhibitor of Mps1/TTK kinase (Mps1 Ki = 0.09 nM; EC50 = 6.5 nM)and can be used in studies about hepatocellular carcinoma diseases.</p>

<p>Debio-0123: potent, specific oral WEE1 inhibitor; IC50 in low nanomolar; boosts DNA damage &amp; Carboplatin's anti-cancer effects.</p>

<p>Plogosertib (CYC140) is a PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib is antiproliferative and can be used to study solid and hematologic tumors.</p>

<p>PD-L1-IN-3 is a PD-1/PD-L1 inhibitor for the study of tumors and immune diseases.</p>

<p>CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively.</p>

<p>B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells.</p>

<p>(R)-Simurosertib ((R)-TAK-931) is an inhibitor of the ATP-competitive cell division cycle 7 (CDC7) kinase.</p>

<p>Sorivudine (BV-araU) is an antiviral blocking DNA synthesis in viruses like varicella, HSV-1, and Epstein-Barr.</p>

<p>Lomibuvir (VCH-222, VX-222) is an allosteric inhibitor of HCV NS5B with Kd 17 nM, blocks RNA elongation, EC50 5.2 nM for 1b/Con1.</p>

<p>CLK1/4-IN-1 inhibits Clk1/4 (IC50: 9.7/6.6 nM), curbing T24 cell growth (GI50: 1.1 μM). Potential cancer research tool.</p>

<p>PAIR2 is a selective IRE1α RNase partial antagonist, blocking its ATP site and preventing KIRA from hindering XBP1 splicing.</p>

<p>2-Amino-2'-fluoro-2'-deoxyadenosine is a component of nucleic acids.</p>

<p>CTX-712 is a potent inhibitor of cdc2-like kinase ( CLK ). CTX-712 inhibits inhibits cancer survival and cancer cell growth.</p>

<p>2'-Deoxycytidine (Deoxycytidine) hydrate is a component of nucleic acids.</p>

<p>KWR095 is an orally active inhibitor of WRN, demonstrating an IC50 of 0.032 μM against WRN ATPase. It disrupts the double-stranded helicase activity of WRN and inhibits tumor cell proliferation, exhibiting antitumor properties.</p>

<p>Terpendole E is an atypical L5 site inhibitor.</p>

<p>ATIC-IN-2 (Compound 1) is a competitive inhibitor of the bifunctional enzyme AICAR Tfase/IMPCH (ATIC), binding to inosine monophosphate cyclohydrolase (IMPCH) with a Ki of 0.13 μM.</p>

<p>DENV-IN-6, a potent anti-DENV (I-IV) and HIV-1 IIIB inhibitor with EC50 ranging 6.8-17.5 μM for DENV and EC50 0.0181 μM for HIV-1.</p>

<p>MtTMPK-IN-3 inhibits Mycobacterium tuberculosis kinase with IC50 0.12μM, MIC 12.5μM on Mtb, cytotoxic EC50 12.5μM on MRC-5 cells.</p>

<p>MtTMPK-IN-1 inhibits MtTMPK with 2.5 μM IC50, shows moderate anti-tuberculosis activity, and is low in cytotoxicity.</p>

<p>CDK7-IN-18: potent, pyrimidine-based CDK7 inhibitor with cancer research potential.</p>

<p>LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (Ki: 6.5 nM). It also has antitumor activity.</p>

<p>IRE1α kinase-IN-4 (compound 6) is a potent inhibitor of IRE1α, exhibiting a Ki value of 140 nM. It acts as an ATP-competitive ligand for IRE1α [1].</p>

<p>Polθ-IN-5 (Compound 139) is an inhibitor of DNA polymerase theta (Polθ) that exhibits antitumor activity.</p>

<p>GSK_WRN4 is a WRN helicase inhibitor with anti-cancer activity, inhibiting MSI tumor cell growth by inducing DNA double-strand breaks, useful in cancer research</p>

<p>GHP-88309 is an orally active, broad-spectrum anti-paramyxovirus agent that targets viral polymerase, interrupting viral RNA synthesis. It effectively inhibits respiratory syncytial virus (RSV), measles virus (MeV), and canine distemper virus (CDV) with an EC50 of 0.06-1.2 μM. In mouse models, GHP-88309 demonstrates significant anti-infective activity.</p>

<p>CDK4/6-IN-24 (Compound A) is an inhibitor of CDK4/6 with broad-spectrum antitumor activity. It can effectively inhibit various cancer cells, exhibiting an IC50 in the submicromolar range.</p>

<p>Valopicitabine is an effective prodrug of the effective anti-HCV drug 2'-C-methylcytidine and can be used as a promising antiviral drug for the study of chronic</p>

<p>Pol I-IN-1 is a powerful inhibitor of RNA polymerase I (Pol I), specifically targeting the large catalytic subunit RPA194, demonstrating an inhibition</p>

<p>L-2'-Fd4C is an L-nucleoside analogue with both anti-human immunodeficiency virus (HIV) and anti-hepatitis B virus (HBV) activity [1].</p>

<p>6K465 is a potent Aurora A kinase inhibitor that reduces c-MYC and N-MYC oncoproteins, showing antiproliferative effects in SCLC and breast cancer cell lines.</p>

<p>EFdA-TP tetrasodium is a potent HIV-1 inhibitor that blocks DNA synthesis as an ICT or DCT.</p>

<p>14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase with antibacterial activity.</p>

<p>PKMYT1-IN-9 is a highly selective, orally active inhibitor of PKMYT1 with an IC50 of 4.4 nM. It exhibits greater selectivity for PKMYT1 compared to WEE1, for which the IC50 is 32.4 μM. Additionally, PKMYT1-IN-9 demonstrates antitumor activity.</p>

<p>MtTMPK-IN-5 inhibits Mtb TMPK with IC50 of 34 μM and fights tuberculosis with MIC of 12.5 μM, aiding TB research.</p>

<p>CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).</p>

<p>CDK9/PARP-IN-1 (compound 37) is an inhibitor of CDK9 and PARP. It demonstrates IC50 values of 118 nM for CDK9 and 107 nM for PARP1. This compound exhibits a broad-spectrum anti-proliferative effect across various cancer cell lines.</p>

<p>Aurora A inhibitor 1: potent, selective, targets cancer-linked Aurora A overexpression, potential for cancer research. (WO2021147974A1, 49)</p>

<p>Werner syndrome RecQ helicase-IN-2 is a potent Werner syndrome RecQ DNA helicase (WRN) inhibitor, useful in research on colorectal and gastric cancers.</p>

<p>RAD51-IN-5 blocks RAD51; may aid mitochondrial disorder research. (WO2021164746A1, cmpd 3)</p>

<p>Mazethramycin is an antitumor antibiotic that exerts its effects by disrupting DNA replication and RNA synthesis within cells. It is utilized in cancer research.</p>

<p>Zorubicin, a Daunorubicin derivative, targets topoisomerase II, inhibits DNA polymerase, and researches acute leukemia, sarcomas.</p>

<p>TASIN-30 is an inhibitor of EBP, exhibiting a competitive EC50 value of 0.097 μM, and possesses a competitive EC50 value of 50 μM against DHCR7.</p>

<p>2′-OMe-ADP is a nucleotide analogue used in oligonucleotide synthesis.</p>