Cytoskeletal Signaling

KIF18A-IN-14 (Compound Example 81) is an inhibitor of KIF18A that exists in two forms, EX81-A and its enantiomer EX81-B. EX81-A and EX81-B inhibit the viability of OVCAR-3 cells with IC50 values of 0-0.01 μM and 0.01-0.1 μM, respectively. KIF18A-IN-14 can be utilized in tumor research, including studies on colon cancer, breast cancer, and lung cancer.

REDV TFA, the minimal active sequence of the CS5 site in the alternatively spliced type III connecting segment (IIICS) of fibronectin, mediates adhesion to the

Lyn-IN-1 (Bafetinib analog) is a selective and potent dual inhibitor of Bcr-Abl and Lyn

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

Defactinib analogue-1 (Compound 7) serves as a ligand for the target protein FAK, and is utilized in the synthesis of PROTAC FAK degrader 1.

Tubulysin D is a tetrapeptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis, and displays potent antitumor activity.

Triciribine (NSC-154020) is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2.

S516 is an active CKD-516 metabolite and is a potent inhibitor of tubulin polymerization(IC50 of 4.29 μM), has marked antitumor activity.

Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K/Akt/mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.

Dasatinib N-oxide is a key metabolite and potential impurity of the kinase inhibitor dasatinib.

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

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

FGFRs-IN-1 (Compound A16) is an orally active inhibitor targeting FGFR1/2/3/4, with IC50 values of 2.3, 7, 11, and 163 nM respectively. It also inhibits VEGFR1/2/3, Abl, and Flt3, with IC50 values of 61, 176, 112, 26, and 353 nM. The compound shows weak inhibition of CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and it inhibits epithelial-mesenchymal transition (EMT) in A549 cells stimulated by TGF-β1. Additionally, FGFRs-IN-1 demonstrates anti-inflammatory activity in mouse models of lung fibrosis induced by Bleomycin and liver fibrosis induced by CCl4.

HSP90-IN-27, also known as compound 19, is an inhibitor of HSP90 [1].

PF-431396 is a dual PYK2/FAK inhibitor (IC50: 11/2 nM).

Dynole 34-2 is a non-competitive inhibitor of dynamin1 and dynamin2 GTPases that inhibits receptor-mediated endocytosis and synaptic vesicle endocytosis.

Tonabersat (SB-220453) is a novel and orally available gap-junction modulator and CSD (Cortical spreading depression) inhibitor that,migraine and epilepsy.

Uprosertib (GSK2141795) is a potent, selective Akt broad-spectrum inhibitor for Akt1/Akt2/Akt3.Cost-effective and quality-assured.

Xentuzumab (BI836845) is a recombinant monoclonal antibody to humanised IGF ligand that inhibits AKT activation and can be used to study solid tumours.

EV206 is an effective inhibitor of Hsp70, exhibiting antiproliferative properties. This compound induces cell apoptosis (apoptosis) and enhances the protein expression of cleaved PARP and caspase-3. Additionally, EV206 demonstrates antitumor activity.