Ciclo cellulare/Checkpoint

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

CDK7-IN-25 (CY-16-1) is a potent CDK7 inhibitor with an IC50 value of less than 1nM, utilized in cancer research [1].

Sovesudil (PHP-201) is a potent ROCK inhibitor with IC50 of 3.7 nM/2.3 nM for ROCK-I/II; lowers IOP without hyperemia.

Fosfluridine tidoxil, a thymidylate synthase inhibitor, is used potentially for the treatment of colorectal cancer, and breast cancer.

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

5'-ODMT cEt N-Bzm5 C Phosphoramidite is a strong modified nucleic acid analog for antisense oligos.

GSK2163632A is an insulin-like growth factor 1 receptor inhibitor that acts by binding to a novel region of the GRK active site cleft.

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

2'-Deoxypseudoisocytidine is a nucleoside analogue.

<p>CCT251455, the mitotic kinase monopolar spindle 1 (MPS1/TTK) inhibitor, is a potent (IC50=3 nM) and specific chemical tool.</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

3-Cyanovinylcarbazole phosphoramidite: an antiviral, hinders viral DNA synthesis, modifies ribonucleotides.

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

PVZB1194, a biphenyl-type inhibitor of Kinesin spindle protein Eg5 (KIF11), exhibits anticancer potential by inducing cell cycle arrest and apoptosis through

Tacaciclib is a cyclin-dependent kinase (CDK) inhibitor with observed antineoplastic activity [1].

KSP-IA is a potent, specific, allosteric, and cell-active KSP inhibitor.

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

L 738167 is a potent antagonist of the long-acting fibrinogen receptor.

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

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

Carotegrast, an orally available α4 integrin receptor inhibitor, has anti-inflammatories activities.

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].

MOMA-341 is a highly selective inhibitor targeting the Werner RecQ-like helicase (WRN). It exerts a dual mechanism of allosteric regulation and ATP competitive inhibition by binding to the cysteine 727 site of the WRN protein. In mouse models with mismatch repair deficiency (dMMR) or high microsatellite instability (MSI-H), MOMA-341 can induce DNA damage, cell apoptosis, and promote tumor shrinkage. This compound exhibits significant anti-tumor activity and has potential application prospects in the study of advanced and metastatic solid tumors.

<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>

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

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.

Amotosalen is a Dermatologic Agent.

<p>PLK1/p38γ-IN-1 (compound 14) serves as a dual inhibitor targeting both PLK1 and p38γ kinases, effectively suppressing the proliferation of human hepatocellular</p>

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

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

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

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

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

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

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].

CDK7-IN-14, a potent CDK7 inhibitor from pyrimidines, may treat transcriptionally dysregulated cancers (CN114249712A).

12R-LOX-IN-1 (Compound 4a), with an IC50 of 28.25 µM, is an inhibitor of 12R-LOX.

Xylocydine is a novel Cdk inhibitor that induces apoptosis in HCC, suppresses tumor growth, and is non-toxic to other tissues.

Kif15-IN-2 is a kinesin Kif15 inhibitor with potential anticancer activity and can be used in prostate cancer research.

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

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

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

(±)9(10)-DiHOME, the diol derivative of (±)9(10)-EpOME—a cytochrome P450-derived epoxide of linoleic acid also known as leukotoxin—is formed through the action of soluble epoxide hydrolase (sEH) in neutrophils. It exhibits toxicity towards Sf21 cells expressing sEH as well as tolacZ-expressing control cells, differing from leukotoxin which only harms sEH-containing cells. Furthermore, combined exposure to 9(10)- and 12(13)-DiHOME leads to cell death in rabbit renal proximal tubule cells by disrupting mitochondrial respiration, and causes lung injury, respiratory distress, and mortality in mice, highlighting its role as a toxic lipid mediator. Specifically, 9(10)-DiHOME has been associated with acute respiratory distress syndrome (ARDS), a severe and often deadly complication in patients with major burns. Elevated levels of this compound have been detected in the bronchoalveolar lavage fluid (BALF) of women, but not men, with chronic obstructive pulmonary disease (COPD), and its levels are also increased in patients with allergic asthma, indicating its significance in respiratory conditions.

PD-1/PD-L1-IN-27: potent anti-cancer, IC50 134nM, minimal T cell harm, boosts CD8+ T cells, reduces fatigue.

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

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 < 3.0 µM, primarily through blocking Rb phosphorylation and inducing G1 cell cycle arrest.

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

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

8-NH2-ATP tetrasodium, an inactive ATP variant, originates from 8-NH2-Ado tetrasodium, which triggers the apoptosis-associated cleavage of poly (ADP-ribose) polymerase [1] [2].

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