Ciclo cellulare/Checkpoint

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

Thymidine-5’-O-(α,β-methylene)diphosphate (TMP-CP), a hydrolytically stable derivative of TDP, functions as an inhibitor of thymidine kinase (Ki = 23 µM).

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].

Bexotegrast (PLN-74809) inhibits αVβ1/αVβ6 integrins, preventing TGF-β1 activation to treat IPF and PSC.

RIOK2-IN-1 (com 4) is a selective RIOK2 inhibitor with a Kd of 150 nM, though it demonstrates low cellular activity with an IC50 of 14,600 nM.

(±)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.

Abetimus (LJP 394 free base), an immunosuppressant composed of four double-stranded DNA (dsDNA) oligonucleotides, can crosslink anti-dsDNA antibodies on B cell

Wee1 Inhibitor I is an ATP-binding site-targeting Wee1 inhibitor.

PD 121373, a Benzothiopyrano-indazole, inhibits nucleic acid synthesis, equally affecting DNA/RNA.

NSC15520 is an RPA inhibitor that inhibits helical destabilization of double-stranded DNA oligonucleotides and can be used to study DNA damage repair.

WRN Inhibitor 5 (Example 157), a cyclic vinyl sulfone-based compound, serves as an inhibitor of Werner Syndrome ATP-dependent helicase enzyme (WRN).

LDC3140 is a potent inhibitor of Cyclin-dependent kinase 7 (CDK7).

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

KIF18A-IN-7 is an orally active inhibitor targeting KIF18A, demonstrating potent inhibition with an IC50 value of 9.4 nM against the microtubule-dependent

Zaurategrast is an effective and oral-effective inhibitor of the α4-integrin.

Cytidine 3'-monophosphate, a ribonucleotide, results from the hydrolysis of cytidine 2',3'-cyclic monophosphate via RNase—a process that cytidine 3'-monophosphate itself inhibits. Additionally, it can be dephosphorylated to cytidine by 3'-nucleotidase.

CCT239065 is a novel, selective, and efficacious nanomolar pyridopyrazinone V600EBRAF and LCK inhibitor.

NVS-SM2 boosts SMN2 splicing, enhances exon 7 inclusion, and raises SMN protein levels orally.

<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>

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).