fak inhibitor-14

Topoisomerase II inhibitor 14 is a potent topoisomerase II inhibitor with anticancer and antioxidant activities.Topoisomerase II inhibitor 14 induces apoptosis and blocks the cell cycle in S phase.Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO. Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO.

Y15 (1,2,4,5-Benzenetetramine tetrahydrochlor) is a potent and specificsmall-molecule FAK scaffolding inhibitor that inhibits its autophosphorylation activity, blocks tumor growth.

PI3K/mTOR Inhibitor-14 (compound Y-2) serves as a dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 171.4 nM and 10.1 nM , respectively, and demonstrates antitumor activities [1].

GSK-3β inhibitor 14 (1,5-Benzothiazepin-4(5H)-one, 2,3-dihydro-2-methyl-5-(phenylmethyl)-) is a weak GSK-3β inhibitor, IC50﹥ 100μM.

mTOR Inhibitor-14 (compound 14c) is a potent inhibitor of mTOR with minimal inhibition of CYP2C8 and has demonstrated the capability to inhibit tumor growth [1].

Compound (Ra)-10, also known as Mcl-1 inhibitor 14, is a potent inhibitor of myeloid cell leukemia-1 (MCL-1), exhibiting a K_i of 0.018 nM, and holds potential for use in anticancer research [1].

Tubulin inhibitor 14 is a potent inhibitor of NQO2 (quinone oxidoreductase 2) with an IC50 of 1.0 μM which also inhibits tubulin polymerization and the formation of endothelial cell capillary-like tubes. Tubulin inhibitor 14 is a microtubule destabilizer with potential tumor-selective as well as anti-angiogenic and vascular-destructive properties [1].

KRAS inhibitor-14 is a potent inhibitor of KRAS G12C (IC50: 0.249 μM). KRAS inhibitor-14 exhibited p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 1.12, >33.3 μM, respectively. KRAS inhibitor-14 has potential to be investigated in pancreatic, colorectal and lung cancers.

ATX inhibitor 14, an indole-based carbamate derivative, is a potent inhibitor (IC50: 0.41 nM) of self-adhesive proteins (ATX) and has shown potential for research in fibrosis-related diseases.

Chitin Synthase Inhibitor 14 (compound 4n), a potent chitin synthase (CHS) inhibitor, exhibits antifungal activity and is effective against drug-resistant fungal strains [1].

Carbonic anhydrase inhibitor 14 (Compound 8b) is a potent CA inhibitor, exhibiting K i values of 1203, 99.7, 9.4, and 27.7 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. Additionally, it effectively inhibits CDK2 with an IC 50 of 20.3 μM. Furthermore, Carbonic anhydrase inhibitor 14 demonstrates significant antitumor activity [1].

HIV-1 inhibitor-14 is a potent, broad-spectrum inhibitor of HIV-1 non-nucleoside reverse transcriptase (RT) (IC50=0.14 μM for HIV-1 RT). HIV-1 inhibitor-14 inhibits both wild-type and drug-resistant HIV-1 strains (EC50: 5.79-28.3 nM).

sEH inhibitor-14, a benzoxazolone-5-urea analogue, acts as an efficient soluble Epoxide Hydrolase (sEH) inhibitor, demonstrating significant activity with an IC50 value of 0.39 nM.

KRAS G12D inhibitor 14 is a potent inhibitor of KRAS G12D that binds KRAS G12D protein (Kd: 33 nM). KRAS G12D inhibitor 14 inhibits the active form of KRAS G12D (KRAS G12D-GTP), but not KRAS G13D.

FAK inhibitor 2, antitumor and anti-angiogenesis activitiesis ,is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 0.07 nM .

KRAS G12C inhibitor 14 is a potent KRAS G12C inhibitor with an IC 50 of 18 nM [1].

Compound 26F effectively optimizes enzyme inhibition (IC50 = 28.2 nM) while demonstrating relatively low cytotoxicity (IC50 = 3.32 μM). It induces apoptosis in MDA-MB-231 cells in a dose-dependent manner and efficiently arrests these cells in the G0/G1 phase.

FAK inhibitor 5 is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.