Ciclo cellulare/Checkpoint

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>GSK2646264 (Compound 44) inhibits SYK (pIC50=7.1) and kinases like LCK, LRRK2; penetrates skin.</p>

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

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

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

CDK8-IN-3 is an inhibitor of CDK8.

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

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].

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

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

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

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

AVG-233 is an RNA-dependent RNA polymerase (RdRp) inhibitor with antiviral activity for the study of respiratory syncytial virus infections.

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

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

USP1-IN-5 (compound 10) is a potent inhibitor of both USP1, with an IC50 of less than 50 nM, and MDA-MB-436 cells, where it also exhibits an IC50 of less than

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

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].

GSPT1 degrader-2 is a potent degrader of GSPT1 [1].

pppApG serves as an initial substrate for the synthesis of vRNA (viral RNA) and cRNA (complementary RNA), with applications in influenza virus research [1].