Cell Cycle/Checkpoint

<p>10-Formylfolic acid is a novel and potent inhibitor of dihydrofolate reductase, which can be used in leukemia research.</p>

<p>9-Isopropylolomoucine (N9-Isopropylolomoucine), a cell cycle protein-dependent kinase inhibitor, is a thiopurine.</p>

<p>TC-S 7005 is an effective inhibitor of Polo-like kinases (IC50s: 214 nM, 4 nM and 24 nM for Plk1, Plk2, and Plk3).</p>

<p>CRT-0105950 is an effective LIMK inhibitor that acts by suppressing cofilin phosphorylation and increasing αTubulin acetylation in cells.</p>

<p>CDK8-IN-1 is a selective CDK8 inhibitor (IC50: 3 nM).</p>

<p>AGX51 is an antagonist of inhibitor of DNA binding (ID) proteins. AGX51 treatment lead to pan-Id degradation, cell cycle arrest, and cell death.</p>

<p>Peldesine (BCX 34), an oral purine nucleoside phosphorylase blocker, halts T-cell growth; used in CTCL, psoriasis, HIV research. IC50: 800 nM.</p>

<p>6-Hydroxy-DOPA is an allosteric inhibitor of RAD52, it inhibits proliferation of BRCA-deficient cancer cells in vitro and also inhibits APE1.</p>

<p>NR2F6 modulator-1, a potent agent for NR2F6, affects immune response and tumor stem cell activity.</p>

<p>Chiauranib, a potent anticancer agent, inhibits angiogenesis kinases (VEGFR1-3, PDGFRα, c-Kit), Aurora B, and CSF1R with IC50 values of 1-9 nM.</p>

<p>Cytembena is a cytostatic and a carcinogenic compound that may increase the incidence of fibroadenomas.Cytembena broadly inhibits DNA biosynthesis.</p>

<p>Talviraline (Bay 10-8979) is an RNA-induced DNA polymerase inhibitor.Talviraline is a potent inhibitor of HIV-1-induced cell killing and HIV-1 replication in a</p>

<p>HA-1004 is a inhibitor of PKG, PKA, PKC and MLC.</p>

<p>dCeMM2 degrades glue by promoting CDK12-cyclin K ubiquitination and degradation via CRL4B ligase interaction.</p>

<p>TTP-8307 is an antiviral compound that inhibits the replication of rhinoviruses and enteroviruses and is used in the study of viral infections.</p>

<p>BioE-1115 is a selective and potent inhibitor of serine-threonine protein kinase (PASK, IC50 = 4 nM). BioE-1115 is a potent inhibitor of CK2α (IC50 = 10 μM).</p>

<p>CHD1Li 6.11 inhibits CHD1L protein (IC50: 3.3 µM), shrinks CRC tumors in vivo, and is orally active.</p>

<p>(S)-PF-06873600 is the S enantiomer of PF-06873600 which is an inhibitor of CDK.</p>

<p>Haspin-IN-3 is a potent haspin inhibitor with an IC50 of 14 nM.Haspin-IN-3 has anticancer activity.</p>

<p>Ryuvidine is a dual inhibitor of KDM5A and SETD8, an inducer of the DNA damage response, and can be used to study breast cancer and erythroderma.</p>

<p>GRK6-IN-1 (compound 18) is a potent GRK6 blocker, with an IC50 of 120 nM, showing promise for multiple myeloma research.</p>

<p>UMK57 is a CENP-Ei and MCAK enhancer, selectively promoting k-MT attachment error correction to inhibit chromosome missegregation of small molecule compounds,</p>

<p>Eprociclovir (A-5021) is a novel acyclovir analog that is a potent inhibitor of EHV1 replication and may be used for the treatment and/or prevention of</p>

<p>CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM).</p>

<p>hSMG-1 inhibitor 11e is an effective and selective inhibitor of hSMG-1 (IC50 &lt;0.05 nM) and can be used in studies about cancer treatment.</p>

<p>BML-259 inhibits CDK5/CDK2 (IC50: 64/98 nM) for cancer and neurodegeneration research.</p>

<p>SB-747651A dihydrochloride, an MSK1 inhibitor (IC50=11 nM), also targets PRK2, RSK1, p70S6K, ROCK-II; potential in inflammation study.</p>

<p>Lunresertib (RP-6306) is a potent, selective, and orally active PKMYT1 inhibitor with an IC50 of 14 nM.Cost-effective and quality-assured.</p>

<p>SEL120-34A inhibits CDK8 (IC50: 4.4 nM) &amp; CDK19 (10.4 nM), less on CDK9 (1070 nM), has antitumor properties.</p>

<p>CDK-IN-2 (CDK inhibitor II) is a potent and specific CDK9 inhibitor (IC50: &lt;8 nM).</p>

<p>DDRI-18 is an inhibitor that regulates the DNA damage response, has anticancer activity, and inhibits non-homologous end-joining (NHEJ) DNA repair.</p>

<p>ZIM, from 4-Aminoantipyrine, induces DNA and chromosomal damage, cell death, and phagocytosis, with potential in cancer therapy.</p>

<p>Cdk2 Inhibitor II is a selective and potent CDK2 inhibitor50 at 60 nM.</p>

<p>Talotrexin ammonium, a non-polyglutamic antifolate, inhibits cancer by targeting DHFR.</p>

<p>NSC16168 is a selective ERCC1-XPF inhibitor that inhibits DNA repair and potentiates the antitumor activity of cisplatin.</p>

<p>PS423 is a substrate-selective protein kinase PDK1 inhibitor that acts by binding to the PIF-pocket allosteric docking site.</p>

<p>ERCC1-XPF-IN-2: Nucleotide repair active, boosts cisplatin, inhibits ERCC1-XPF (IC50: 0.6 μM).</p>

<p>(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that inhibits the transcription of anti-apoptotic and pro-survival proteins.</p>

<p>SMN-C2, a SMN2 gene splicing regulator, is an RNA-binding ligand that regulates pre-mRNA splicing and has potential for studying spinal muscular atrophy.</p>

<p>Netivudine, a potent NRTI with anti-varicella activity, treats HIV by inhibiting reverse transcriptase, reducing viral load.</p>

<p>Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells.</p>

<p>PCSK9-IN-10: potent oral PCSK9 inhibitor (IC50 = 6.4 µM), upregulates LDLR, curbs atherosclerosis, for hyperlipidemia research.</p>

<p>COH34 (1-[(E)-(4-methylphenyl)sulfanyliminomethyl]naphthalen-2-ol) is a selective inhibitor of PARG with an IC50 of 0.37 nM and a Kd of 0.547 μM.</p>

<p>L82: A selective, non-competitive DNA Lig1 inhibitor with anti-proliferative effects on breast cancer cells. IC50=12 μM.</p>

<p>RP-6685 is a potent, selective DNA Polθ inhibitor with strong oral efficacy, an IC50 of 5.8 nM, and marked antitumor effects in mice.</p>

<p>SB 328437 ((S)-methyl 2-(1-naphthamido)-3-(4-nitrophenyl)propanoate) is an effective and selective antagonist of CCR3 (IC50 = 4.5 nM).</p>

<p>Denv-in-5 is an effective and selective dengue virus (DENV) inhibitor with EC50 values of 1.47, 9.23, 7.08, 8.91 μM for denV-I-IV and 0.1512 μM for HIV-1IIIB.</p>

<p>CDK-IN-11, a heterocyclic compound, promotes cardiomyocyte maturation [1].</p>

<p>WRN Inhibitor 3 (example 110), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).</p>

<p>WRN Inhibitor 4 (Example 107), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).</p>

<p>QR-6401, a selective macrocyclic CDK2 inhibitor, is orally active with IC50 values of 0.37 nM for CDK2/E1, 10 nM for CDK9/T1, 22 nM for CDK1/A2, 34 nM for CDK6/</p>

<p>CDK9-IN-8 is a highly potent and selective CDK9 inhibitor (IC50: 12 nM).</p>

<p>G4/HDAC-IN-1, a G4/HDAC dual inhibitor, IC50 1.1 µM, blocks TNBC growth, useful in cancer research.</p>

<p>CDK9-IN-29 (compound Z11) is a potent inhibitor of CDK9, exhibiting high kinase selectivity and an IC50 value of 3.20 nM.</p>

<p>CDK/HDAC-IN-3 is an orally active dual inhibitor of HDACs and CDKs, offering potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3,</p>

<p>c-Myc inhibitor 8 suppresses cell growth in various cancers and is used in research.</p>

<p>Sapacitabine (CS682) is a nucleoside analog precursor with anticancer activity used in the study of leukemia.</p>

<p>Nε-(1-Carboxyethyl)-L-lysine (CEL) is an advanced glycation end-product (AGE). Exposure to CEL reduces glutamate uptake and S100B secretion in the hippocampus.</p>

<p>BVDU 5′-Triphosphate is an antiviral agent labeled with 5′-Triphosphate that specifically targets viral DNA polymerase.</p>

<p>GGTI 2147 decreased Rac1 activity, down-regulated p65 expression, and ameliorated OGD/R-induced neuronal apoptosis.</p>

<p>5'-ODMT cEt m5U Phosphoramidite Amidite, a locked nucleic acid (LNA) analog, demonstrates exceptional safety and antisense activity [1] [2].</p>

<p>9-Deazaguanine is a nucleoside analogue exhibiting inhibitory activity against bovine purine nucleoside phosphorylase (PNP).</p>

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

<p>ATN-161 is an integrin α5β1 binding peptide and antagonist that inhibits VEGF-induced hCECs migration and angiogenesis.</p>

<p>Raluridine is an HIV treatment inhibiting RNA-directed DNA polymerase with IC50 of 1.8 microM, compared to FLT, AZT, ddI, and ddC.</p>

<p>(2S,3R)-Voruciclib is the (2S,3R)-enantiomer of Voruciclib. It is an orally active CDK inhibitor.</p>

<p>α2β1 integrin inhibitor</p>

<p>αvβ1 integrin-IN-2 (compound 32) is a potent inhibitor of ανβ1 and α5β1 integrins, exhibiting IC50 values of 0.9 nM and 33 nM, respectively.</p>

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

<p>DMA-IN-1 is a DNA adenine methyltransferase (DAM) inhibitor with an IC50 value of 48 μM.</p>

<p>CT1113, a potent inhibitor of both USP28 and USP25, effectively reduces MYC levels in vivo and demonstrates anti-tumor efficacy in a mouse pancreatic cancer CDX</p>

<p>Votoplam functions as a gene splicing modulator, employed in the inhibition of Huntington's disease [1].</p>

<p>NITD008 (7-Deaza-2'-C-acetylene-adenosine) is an adenosine nucleoside inhibitor with antiviral activity that inhibits dengue and Zika viruses.</p>

<p>Aurora Kinases-IN-4 (Compound 11c) is a covalent, ATP-competitive inhibitor of aurora kinase A with an IC50 value of 1.7 nM.</p>

<p>G-5758 is an orally active IRE1α inhibitor with an IC50 of 38 nM for XBP1s. It is used in studies involving multiple myeloma models [KMS-11], demonstrating good tolerance in rats at oral doses up to 500 mg/kg. G-5758 exhibits pharmacodynamic effects comparable to those induced by IRE1 knockdown.</p>

<p>ON 108600 is a chemical inhibitor targeting CK2 (Casein Kinase 2), TNIK, and DYRK1, demonstrating IC50 values of 0.016 μM and 0.007 μM for DYRK1A and DYRK1B, 0.</p>

<p>2'-Deoxypseudoisocytidine is a nucleoside analogue.</p>

<p>ROCK2 inhibitor is a chemical compound associated with the therapeutic management of psoriasis.</p>

<p>PD-1/PD-L1-IN-34 (Compound (1S,2S)-A25) effectively inhibits the PD-1/PD-L1 interaction (IC 50 = 0.029 μM) and demonstrates selective binding affinity to PD-L1</p>

<p>SZ-015268: CDK7 inhibitor, IC50=23.56 nM; hinders HCC70, OVCAR-3, HCT116, HCC1806 cell growth; strong anti-tumor effect.</p>

<p>ASC-69 (APY69) is a promising potent inhibitor of the PD-1/PD-L1 signaling pathway, classified as a small-molecule compound [1].</p>

<p>ML-099 is a pan Ras-related GTPases activator that activates Rac1, Ras, GTP-binding protein (Rab7), Rab2A and cell division cycle 42.</p>

<p>Alatrofloxacin is a prodrug of trovafloxacin.</p>

<p>L-739758 is a glycoprotein IIb/IIIa inhibitor.</p>

<p>CCT-271850 is an inhibitor of the spindle checkpoint function of Monospindle 1.</p>

<p>Palbociclib (PD 0332991) orotate, an orally active selective inhibitor of CDK4 and CDK6, exhibits IC50 values of 11 and 16 nM, respectively.</p>

<p>Lerociclib (G1T38) is a CDK4/6 inhibitor with anticancer and antitumor activities, inhibiting CDK4/CyclinD1 and CDK6/CyclinD3.</p>

<p>53BP1-binding protein 1 (53BP1) engages with dimethylated lysine 20 on histone 4 (H4K20me2) through its tandem tudor domains within a homodimer configuration, crucial for the DNA damage response. UNC2170, a micromolar 53BP1 ligand, selectively interacts with this site, demonstrating at least 17-fold preference for 53BP1 over similar proteins. This interaction occurs in a pocket formed by the 53BP1's tudor domains. Moreover, UNC2170 acts as an antagonist to 53BP1 in cellular lysates, effectively inhibiting class switch recombination, a process dependent on the functional 53BP1 tudor domain, thus confirming its cellular activity.</p>

<p>CDK9-IN-23 (Example 4) is a potent inhibitor of CDK9, exhibiting an IC50 value of less than 20 nM [1].</p>

<p>Aurora kinase inhibitor-8 is a highly selective inhibitor of Aurora kinase.</p>

<p>DUB-IN-7 (compound 43), a deubiquitinating enzyme (DUB) inhibitor, has utility in researching diseases driven by aberrant JAK2 activity, including leukemia [1].</p>

<p>m-Se3 is a potent, selective inhibitor of c-MYC transcription with demonstrated capability to inhibit tumor growth and exhibit anti-cancer activity [1].</p>

<p>3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one), a xanthone derivative, exhibits inhibitory effects on NADPH-catalyzed lipid peroxidation in human umbilical vein</p>

<p>WRN Inhibitor 2 (example 118), a potent inhibitor of the WRN (Werner Syndrome ATP-dependent helicase enzyme), exhibits a pIC50 value of 7.0 or greater [1].</p>

<p>Voruciclib hydrochloride is an orally active and selective inhibitor of CDK (Ki: 0.626 nM-9.1 nM).</p>

<p>ROCK-IN-9 (Compound T345), a ROCK inhibitor, exhibits cytotoxicity in HepG2 cells with an IC50 of 40.8 μM.</p>

<p>Gly-Arg-Gly-Asp-Ser (TFA), osteopontin domain, binds αvβ3 and αvβ5 integrins; IC50s: ~5 μM, ~6.5 μM.</p>

<p>CDK4/6-IN-17 (compound 12) is an orally bioavailable inhibitor of CDK4/6, demonstrating potent activity with IC50 values between 10-100 nM in BE(2) cells.</p>

<p>CCG-232964 is an orally active Rho/MRTF/SRF inhibitor that suppresses LPA-induced CTGF gene expression [1].</p>

<p>NU6300 is a covalent CDK2 inhibitor exhibiting irreversible and ATP-competitive properties and also functions as a GSDMD (Gasdermin D) inhibitor.</p>