Ciclo celular/Ponto de verificação

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

Brodimoprim is an inhibitor of dihydrofolate reductase(DHFR).

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

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

CDK4/6-IN-15: Oral, selective CDK4/6 inhibitor, halts cancer cell growth, G1 arrest, suppresses Rb phosphorylation.

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].

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).

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

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.

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

(±)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

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.

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

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

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

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

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.

LX7101 is a potent inhibitor of both LIM kinase (LIMK) 1 and 2, and Rho-associated kinase 1 (ROCK1) and ROCK2, with IC50 values of 32, 4.3, 69, and 32 nM, respectively. It is selective, demonstrated by its lack of cross-reactivity in a panel of binding assays involving 78 receptors, transporters, and an additional 430 kinases, at a concentration of 10 μM. The topical administration of LX7101 (3 μl of a 1 mg/ml solution) to the eye has been shown to reduce intraocular pressure in a dexamethasone-induced mouse model of glaucoma.

ROCK2 inhibitor is a chemical compound associated with the therapeutic management of psoriasis.

DHODH-IN-14 is an analog of hydroxyfuran pyrimidine A771726.

Teclistamab(JNJ-64007957) is a human bispecific monoclonal antibody targeting the CD3 receptor on t-cells and the BCMA for relapsed and refractory multiple myeloma.

MOMA-341, ATP-competitive WRN allosteric inhibitor (Cys727 site), induces DNA damage and tumor regression in dMMR/MSI-H models, for solid tumors.

TAK 029 is a local glycoprotein IIb/IIIa receptor inhibitor.

AR-13503, a Netarsudil metabolite, is a ROCK inhibitor, potentially treating glaucoma and lowering eye pressure.

Cytarabine 5′-monophosphate (ara-CMP), an active metabolite of the nucleoside analog cytarabine formed by deoxycytidine kinase, is incorporated into DNA by DNA polymerase α, significantly slowing DNA synthesis. It inhibits nuclear and mitochondrial DNA replication in S. cerevisiae at 15 mM and improves survival in an L1210 murine leukemia model at 3.5-75.1 mg/kg.

5′-Guanylyl methylenediphosphonate (sodium) serves as a GTP analogue and acts as a specific, competitive inhibitor of the GTP reaction in protein synthesis [1].

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

Tnp 351 is a novel antifolate drug being assessed for chemotherapy of lung cancer.

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].

WRN Inhibitor 1 (example 7) is an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN), selectively targeting its helicase domain.

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

Amotosalen is a Dermatologic Agent.

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

GRK2 Inhibitor 2 (Compound 8h), with an IC50 of 19 nM for GRK2 and 137 nM for Aurora-A, enhances β-AR-mediated cAMP accumulation in GRK2-overexpressing HEK293

LDN-91946 is an effective and selective inhibitor of ubiquitin C-terminal hydrolase-L1 (UCH-L1) (Ki = 2.8 μM).

Netropsin dihydrochloride, a small MGB, blocks topoisomerase I/II, hindering cleavable complex stabilization.

Pelitrexol (AG2037) is a GARFT inhibitor, which can inhibit the activity of mTORC1, block the cell cycle in the s-phase, with antiproliferative activity,NSCLC .

Senexin A hydrochloride functions as a selective inhibitor of CDK8/19, with an IC 50 of 280 nM for CDK8, and specifically inhibits p21-induced transcription without affecting other biological effects of p21. Additionally, it suppresses CMV-GFP induction and the stimulatory activity of the consensus NF-κB-dependent promoters [1] [2].

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

CASK-IN-1 is a highly potent and selective CASK inhibitor with a K d value of 0.022 μM.

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

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

GW814408X, a kinase chemical genome group (KCGS) compound, inhibits the AURKC kinase, which is involved in cell cycle progression, checkpoint regulation, and cell division. It exhibits cell line-dependent toxicity, such as cytotoxic effects on HeLa cells, and acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, potentially impacting Fluc reporter assays [1].

Compound 6k, also known as Anti-hepatic fibrosis agent 2, is an orally active inhibitor of the COL1A1 enzyme and exerts anti-fibrogenic effects by targeting the