Ciclo celular / Checkpoint

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

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.

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.

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].

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

α2β1 integrin 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.

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

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

RAD51-IN-4, a potent RAD51 inhibitor, may be useful in researching mitochondrial defect-related conditions.

MC-Val-Cit-PAB-Ispinesib (Compound 509) is a potent Eg5 inhibitor and a click chemistry reagent [1].

Riviciclib, a CDK inhibitor (CDK9/T1, CDK4/D1, CDK1/B), has IC50s: 20, 63, 79 nM respectively, and fights cisplatin-resistant tumors.

Mps1-IN-6 (Compound 9) is a highly effective Mps1 inhibitor with an IC50 value of 6.4 nM and exhibits significant anti-proliferation and anti-tumor effects on

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

FAICAR (5-Formamidoimidazole-4-carboxamide ribotide), a purine nucleotide, plays a crucial role in metabolic processes.

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

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

12R-LOX-IN-1 (Compound 4a), with an IC50 of 28.25 µM, is an inhibitor of 12R-LOX.

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

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

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

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

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).

5'-ODMT cEt N-Bzm5 C Phosphoramidite is a strong modified nucleic acid analog for antisense oligos.

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

ROCK-IN-7 (compound 9) serves as a ROCK kinase inhibitor and is utilized in the investigation of ocular conditions, including glaucoma and retinal diseases [1].

Alatrofloxacin is a prodrug of trovafloxacin.

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

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.

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

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.

2'-Deoxypseudoisocytidine is a nucleoside analogue.

G-5758 is an orally active IRE1α inhibitor with an IC50 of 38 nM for XBP1s. It is used in studies involving multiple myeloma models [KMS-11], demonstrating good tolerance in rats at oral doses up to 500 mg/kg. G-5758 exhibits pharmacodynamic effects comparable to those induced by IRE1 knockdown.

(±)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.

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

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

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

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

DNA polymerase-IN-1 exhibits antiproliferative activity against tumor cells and inhibits Taq DNA polymerase as a DNA polymerase inhibitor.

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

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,

ROCK-IN-9 (Compound T345), a ROCK inhibitor, exhibits cytotoxicity in HepG2 cells with an IC50 of 40.8 μM.

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

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

Amotosalen is a Dermatologic Agent.

MS-444 (BE-34776) is an MLCK and HuR inhibitor with antitumor activity that can be used to study triple-negative breast cancer and colorectal cancer.

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].

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).

αvβ1 integrin-IN-2 (compound 32) is a potent inhibitor of ανβ1 and α5β1 integrins, exhibiting IC50 values of 0.9 nM and 33 nM, respectively.

Senexin C is a CDK8/19 inhibitor with anticancer activity.Senexin C inhibits the growth of MV4-11 leukemia cells.

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

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

DHX9-IN-4 is an ATP-dependent RNA helicase DHX9 inhibitor used in cancer research.

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

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

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

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

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

Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7. SY-1365 possesses therapeutic potential in both hematological and solid tumors.

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

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

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 .

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

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.

4′-DTMP (4-Demethyltrimethoprim) is a DHFR inhibitor with antimicrobial activity against Escherichia coli.

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

CDK9-IN-8 is a highly potent and selective CDK9 inhibitor (IC50: 12 nM).

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

DYRKs-IN-2 has antitumor activity. DYRKs-IN-2 is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively.

N-desmethyl Netupitant is a metabolite of Netupitant and a potential Substance-P receptor agonist.

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

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].

DHX9-IN-6 is a highly effective ATP-dependent RNA helicase A (DHX9) inhibitor, used in cancer research.

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.

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

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.

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

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

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

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

XY028-140 is a selective CDK4/6 inhibitor and degrader, acting via PROTAC with ligands for Cereblon and CDK in cancer cells.

Gossypolone is is a proposed major metabolite of gossypol. Gossypolone reduces Notch/Wnt signaling and induces apoptosis.

Plogosertib (CYC140) is a PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib is antiproliferative and can be used to study solid and hematologic tumors.

Roxifiban acetate（DMP 754 acetate） is a potent GP IIb / IIIa antagonist that exhibits antiplatelet aggregation activity via immune mediation and can be used in

H-1152 2HCl: ROCK inhibitor, IC50=12 nM, Ki=1.6 nM. Blocks PKA, PKC, PKG, Aurora A, CaMKII with higher IC50s.