fak inhibitor y15

Mcl-1 Inhibitor 15 (Compound (Ra)-15), with a K i of 0.02 nM, is utilized in cancer research [1].

HIV-1 inhibitor-15 (compound 9d) is a potent and broad-spectrum inhibitor targeting HIV-1. It exhibits inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, and E138K with respective EC50 values of 1.7 nM, 4 nM, 2 nM, 6 nM, and 9 nM. In addition to its high efficacy, HIV-1 inhibitor-15 possesses favorable solubility, safety profiles, and oral bioavailability [1].

Carbonic Anhydrase Inhibitor 15 (Compound 8), with an inhibitory constant (K_i) of 8.5 nM for hCA II, exhibits analgesic effects [1].

BRD4 Inhibitor-15 (compound 13) is a highly potent and specific inhibitor of BRD4, effectively inhibiting it with an IC50 of 18 nM. By regulating the Bcl-2/Bax proteins and activating the caspase-3 signaling pathway, BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells. Additionally, it effectively down-regulates the c-Myc level in 22RV1 cells. Due to its properties, BRD4 Inhibitor-15 is a valuable compound for research related to prostate cancer [1].

KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor .

ATX inhibitor 15 (compound 30) is an indole-based carbamate derivative with a strong inhibitory effect on autotaxin (ATX), demonstrated by an IC50 of 2.17 nM. Additionally, ATX inhibitor 15 effectively inhibits ATX activity in vivo and suppresses the expression of pro-fibrotic genes. Furthermore, ATX inhibitor 15 exhibits protective effects in lung fibrosis induced by Bleomycin in mice [1].

Tubulin inhibitor 15 is a potent tubulin inhibitor with antiproliferative activity. Tubulin inhibitor 15 exhibits cytotoxicity in HepG2 cells [1].

KRAS inhibitor-15 (compound 3-19) is a potent inhibitor of KRAS G12C (IC50: 0.954 μM). KRAS inhibitor-15 exhibits p-ERK inhibition in MIA PaCA-2, A549 cells with IC50s of 2.03, >33.3 μM, respectively. KRAS inhibitor-15 has potential to be studied in pancreatic, colorectal and lung cancers.

9c(i472) is an inhibitor of 15-lipoxygenase-1 (15-LO-1; IC50 = 0.19 μM).1 It decreases LPS- and IFN-γ-induced NF- B activity in RAW-Blue cells when used at concentrations of 0.2, 1, and 5 μM. 9c(i472) reduces LPS- and IFN-γ-induced increases in Nos2 expression and lipid peroxidation in RAW 264.7 cells when used at a concentration of 5 μM.

Topoisomerase II inhibitor 15 (compound 2g) serves as a potent apoptotic inducer, exhibiting heightened selectivity for head and neck tumors [1].

KRAS G12D inhibitor 15 is a potent inhibitor specifically targeting the KRAS G12D mutation. It holds potential for research into numerous diseases or disorders, including cancer and its metastases[1].

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

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.

NaPi2b is primarily expressed in the small intestine, lungs, and testes and plays an important role in phosphate homeostasis. The inhibition of NaPi2b, responsible for intestinal phosphate absorption, is considered to reduce serum phosphate levels, making it a promising therapeutic approach for hyperphosphatemia

P-gp Inhibitor 15 (compound 7a), a nonsubstrate inhibitor of P-glycoprotein (Pgp), inhibits Pgp-ATPase activity and interferes with Pgp-mediated Rhodamine123 efflux. Additionally, this compound enhances the inhibitory effect of Paclitaxel on tumor progression in the KBV xenograft tumor model in nude mice [1].

GSK-3β inhibitor 15 (Compound 54), with an IC50 of 3.4 nM, effectively suppresses Aβ 1-42-induced phosphorylation of GSK-3β and tau protein, as well as LPS-induced iNOS expression. It demonstrates neuroprotective properties against Aβ 1-42-induced neurotoxicity, indicating its potential utility in Alzheimer's disease (AD) research [1].

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

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