Cycle cellulaire/point de contrôle

H3B-968 is a potent inhibitor of Werner syndrome protein (WRN) with an IC50 of approximately 10 nM, effectively targeting its helicase, ATPase, and exonuclease

USP7-IN-1 is a selective and reversible ubiquitin-specific protease 7 (USP7) inhibitor (IC50 = 77 μM).

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

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

PLK1-IN-7 (compound 30e) is a potent inhibitor exhibiting an IC50 value of 0.66 nM and demonstrates significant antiproliferative and antitumor activities [1].

5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase (IC50s

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

CDK7-IN-22 (compound 101) is a selective CDK7 inhibitor that exhibits antitumor activity, demonstrating specificity for CDK7 [1].

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.

DNA gyrase B-IN-3 (Compound A), with an IC50 of less than 10 nM, acts as an inhibitor of bacterial DNA gyrase B and exhibits antibacterial activity against Gram

RNA polymerase II-IN-1 (19iv), an amatoxin, inhibits Pol II at 36.66 nM IC50, is more toxic to cancer cells, less to normal cells than α-Amanitin.

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

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

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

ROCK2-IN-2 is a selective inhibitor of ROCK2 (IC50 of <1 μM).

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].

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

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

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].

Spirofylline is an agent of bronchodilator, has the potential for asthma and bronchitis and emphysema treatment.

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

USP7-IN-13 (Compound 101), a USP7 inhibitor, exhibits an IC50 range of 0.2-1 μM and is applicable in researching multiple myeloma [1].

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

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

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.

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

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).

Mefenidil (McN-2378), a selective cerebral vasodilator, was shown to increase CBF in healthy brains without stimulating O2 uptake in a dog anesthesia model.

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

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.

LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM).

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

Lotrafiban hydrochloride is an platelet glycoprotein IIb/IIIa blocker with oral activity.

Zaurategrast (CDP323) is an oral α4-integrin antagonist that blocks VCAM-1 interactions and is used to study immune cell trafficking.

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

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].

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,

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

SB-743921, a kinesin spindle protein (KSP) inhibitor, is used potentially for the treatment of non-Hodgkin's lymphoma (NHL).

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

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

MU-380 is an effective and selective inhibitor of CHK1.

TC-A 2317 HCl inhibits Aurora A kinase (Ki 1.2 nM) over Aurora B (Ki 101 nM), displaying antitumor effects.

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

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

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/

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

Trovafloxacin: broad-spectrum fluoroquinolone, blocks DNA gyrase/topoisomerase IV and PANX1 channel (IC50=4μM).

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

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).

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

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

Butylparaben sodium significantly impacts the later phases of spermatogenesis in the testes by impairing hormonal regulation and/or RNA and protein synthesis [1

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

Alatrofloxacin is a prodrug of trovafloxacin.

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

ROCK-IN-8 (Example 4), a ROCK inhibitor, exhibits anti-inflammatory properties and is suitable for respiratory and gastro-intestinal disease research,

CDK4-IN-2 (A17) is a potent inhibitor of CDK4, exhibiting K i and IC 50 values of less than 10 nM and is utilized in cancer research [1].

TNH, a dimeric compound, possesses the ability to penetrate living cells and facilitate the recruitment of proteins into cellular structures [1].

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].

Leucettinib-92 is a multi-kinase inhibitor of DYRK and CLK families with differential nanomolar activity, supporting studies of kinase signaling regulation.

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

Myt1-IN-2, a highly potent Myt1 inhibitor, exhibits remarkable anticancer properties with an IC50 value below 10 nM (WO2021195782A1; compound 28) [1].

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

Cdc7-IN-12, a sub-1 nM CDC7 inhibitor, may aid cancer research; hinders COLO205 cell growth (IC50: 100-1000 nM).

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.

Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective PKC inhibitor. It is also a potent CDK2 antagonist (IC50: 200 nM).

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

Myt1-IN-3 is a potent inhibitor of Myt1 (IC50 <10 nM) [1].

DNA polymerase-IN-3 (Compd 5b), a coumarin derivative, demonstrates inhibitory activity against Taq DNA polymerase and has potential applications in

TAS-114 is a dUTPase and DPD inhibitor that modulates catabolic pathways to improve systemic availability of 5-FU.

IIIM-290 is an oral CDK inhibitor (IC50s: 90 and 94 nM for CDK2/A and CDK9/T1).

Diazoketone methotrexate is an analog of methotrexate with potential antitumor activity.

PD-321852, a Chk1 inhibitor, boosts gemcitabine's effect in pancreatic cancer cells, varying from minimal in Panc1 to >30-fold in MiaPaCa2.

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

5,11-methenyltetrahydrohomofolate blocks GAR & AIR transformylase; used as an anti-purine drug.

BI-1950: potent inhibitor of LFA-1, key in immune function and drug target.

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

PTC258 is a specific, orally active modulator of the splicing of the Elongator complex protein 1 gene (ELP1), enhancing its expression both in vitro and in vivo

CI 972 anhydrous is an inhibitor of purine nucleoside phosphorylase (PNP) (Ki: 0.83 μM) used as a T cell-selective immunosuppressive agent.

Antifolate C1 blocks purine creation, favors uptake via folate receptors/PCFT over RFC.

VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).

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

Methotrexate-gamma-aspartate has growth inhibitory effects. It is used in antibody-targeted liposomes.

CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor (IC50: 2.3 nM).

Inixaciclib is a potent CDK inhibitor, can be used to research anticancer.

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

AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.