Ciclo celular/Ponto de verificação

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

L 738167 is a potent antagonist of the long-acting fibrinogen receptor.

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

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

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

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

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

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

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

Halofuginone hydrochloride (RU-19110), a derivative of Febrifugine, functions as a competitive inhibitor of prolyl-tRNA synthetase, displaying a Ki value of 18.3 nM. This compound effectively inhibits type-I collagen synthesis, providing therapeutic benefits in osteoarthritis (OA) by impeding TGF-β signaling. Additionally, it serves as a potent pulmonary vasodilator, mainly through the activation of Kv channels and the inhibition of various calcium channels including voltage-gated, receptor-operated, and store-operated ones. Beyond its vascular effects, Halofuginone hydrochloride exhibits a broad spectrum of biological activities, including anti-malarial, anti-inflammatory, anti-cancer, and anti-fibrotic properties, supported by multiple studies.

α2β1 integrin inhibitor

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

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

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].

Lerociclib (G1T38) is a CDK4/6 inhibitor with anticancer and antitumor activities, inhibiting CDK4/CyclinD1 and CDK6/CyclinD3.

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

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

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

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.

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

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

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.

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

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

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

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

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

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.

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.

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.

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

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

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

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.

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

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.

Amotosalen is a Dermatologic Agent.

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).

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

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

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

Lamifiban is a nonpeptide glycoprotein IIb/IIIa antagonist. It prevents platelet loss during experimental cardiopulmonary bypass.

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

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

ICAM-1-IN-1 is a potent and selective E-selectin(IC50 = 7 nM) and ICAM-1(IC50 = 5 nM) inhibitor.

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

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

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