Signalisation du cytosquelette

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

insulin receptor (IR) activator

(S)-3'-hydroxy-Blebbistatin is a more stable and less phototoxic derivative of (–)-blebbistatin, retaining the latter's properties as a selective, cell-permeable inhibitor of non-muscle myosin II ATPases. Unlike its predecessor, (S)-3'-hydroxy-Blebbistatin exhibits reduced fluorescence, improving its utility in live cell imaging applications by diminishing degradation into cytotoxic intermediates under blue light exposure (450-490 nm). It effectively inhibits the Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB across various species with IC50 values ranging from 0.5-5 µM and shows minimal inhibition against smooth muscle myosin with an IC50 of 80 µM. This compound plays a critical role in preventing apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells, mirroring the active (–)-blebbistatin enantiomer in mechanism and efficacy.

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

Pterostilbene-isothiocyanate (PTER-ITC) demonstrates strong anticancer properties in vitro, particularly disrupting the interaction between β-catenin and TCF-4

Porcn-IN-2 (Example 107) is a potent Wnt pathway inhibitor, exhibiting an IC50 of 0.05 nM.

β-Catenin modulator-1 (IIa-650) is a useful agent in cancer research for modulating β-Catenin [1].

PKC-theta inhibitor 1 is an inhibitor of PKCθ (Ki of 6 nM)

HDAC-IN-55(8j) is a small-molecule inhibitor that enhances E-cadherin expression and suppresses cancer cell proliferation [1].

CFI-402257 hydrochloride, a highly selective and orally bioavailable inhibitor targeting TTK/Mps1, demonstrates an in vitro IC50 value of 1.7 nM against TTK. This compound exhibits anti-cancer activity [1].

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

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).

β-Catenin-IN-6 is an inhibitor of the canonical Wnt/β-catenin signaling pathway, effectively impeding the proliferation of human colorectal cancer cells and

Litronesib is a selective inhibitor of mitosis-specific kinesin Eg5. It also has antitumor activity.

22-(4′-py)-JA, a semisynthetic derivative of junamycin A isolated from the Thai blue sponge (Xestospongia sp.), exhibits antimetastatic properties by inhibiting

Tubulin polymerization-IN-52 (compound SC23) effectively inhibits tubulin polymerization, exhibiting an IC50 value of 2.9 μM [1].

Oxaline, a fungal alkaloid derived from Penicillium oxalicum, impedes tubulin polymerization, leading to cell cycle arrest at the M phase [1] [2].

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

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