Cycle cellulaire/point de contrôle

T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.

HQ005, a potent CCNK degrader, exhibits an impressive DC50 value of 0.041 µM and functions as a molecular-glue degrader.

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

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

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

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

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

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

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.

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

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

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].

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,

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

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

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

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

WRN Inhibitor 4 (Example 107), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).

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].

XL413 hydrochloride (BMS-863233 Hydrochloride) is a potent, selective and ATP competitive inhibitor of Cdc7. XL413 hydrochloride also inhibits CK2 and PIM1.

CDK9-IN-19: Potent CDK9 inhibitor, anti-cancer, moderate pharmacokinetics, low hERG impact, effective in AML research.

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

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

WRN Inhibitor 3 (example 110), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN).

Lotrafiban: Oral GP IIb/IIIa inhibitor for treating coronary and cerebrovascular disease.

CDK-IN-11, a heterocyclic compound, promotes cardiomyocyte maturation [1].

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).

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

Emzadirib (RAD51-IN-2) is a potent RAD51 inhibitor with potential anticancer activity for the study of DNA damage repair.

FT206 is a carboxamide inhibitor of ubiquitin-specific protease[1].

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

'(S)-Cdc7-IN-18 from patent WO2020239107A1 inhibits CDC7, curbing MCM2 and tumor growth.'

α7β1 Integrin Modulator-1 is a potent modulator with research potential for muscular dystrophy [1].

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

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

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

USP1-IN-3 is a selective inhibitor of USPI that inhibits USPI-UAFI (IC50<30 nM). USP1-IN-3 can be used to study cancer.

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].

SJ26 is a Wnt1 inhibitor known for its anticancer activity. It inhibits the expression of WNT1 and the downstream signaling pathways mediated by WNT1 in a G-quadruplex structure-dependent manner, thereby suppressing the migratory activity of cancer cells.

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

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].

CCT-271850 is an inhibitor of the spindle checkpoint function of Monospindle 1.

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

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

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).

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

c-Myc inhibitor 8 suppresses cell growth in various cancers and is used in research.

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.

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

(±)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.

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/

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

BIO-7662 is an effective and highly selective antagonist of α4β1 integrin.

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].

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

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

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

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

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

53BP1-binding protein 1 (53BP1) engages with dimethylated lysine 20 on histone 4 (H4K20me2) through its tandem tudor domains within a homodimer configuration, crucial for the DNA damage response. UNC2170, a micromolar 53BP1 ligand, selectively interacts with this site, demonstrating at least 17-fold preference for 53BP1 over similar proteins. This interaction occurs in a pocket formed by the 53BP1's tudor domains. Moreover, UNC2170 acts as an antagonist to 53BP1 in cellular lysates, effectively inhibiting class switch recombination, a process dependent on the functional 53BP1 tudor domain, thus confirming its cellular activity.

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

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

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).

PF-6808472 is a cell-permeable covalent kinase probe, reacts with conserved lysine residues within the ATP-binding site of kinases.

UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.

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

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].

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

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

SHP2/CDK4-IN-1: dual inhibitor, oral, potent (IC50: SHP2 4.3 nM, CDK4 18.2 nM), hinders TNBC growth, strong antitumor effects in mice.

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

Aurora kinase inhibitor-8 is a highly selective inhibitor of Aurora kinase.

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

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

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

KM05382 inhibits CDK9 and the transcription of GAPDH.

(2S,3R)-Voruciclib is the (2S,3R)-enantiomer of Voruciclib. It is an orally active CDK inhibitor.

L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.

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].

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

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

Balapiravir HCl, an NS5B inhibitor, is used potentially for the treatment of HCV infection.

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

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

8-Azahypoxanthine (NSC-22709) inhibits hypoxanthine-guanine-xanthine phosphoribosyltransferase and has antimalarial properties.

α2β1 integrin inhibitor

CDK9-IN-2, a CDK9 inhibitor from patent WO/2012131594A1, IC50: 5 nM in A2058, 7 nM in H929 at 72hr.