PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL-induced apoptosis poses a huge problem in establishing clinically efficient TRAIL therapies.
ICAAc is a solvatochromic fluorescent pH probe.1 As the polarity of the solvent increases, the emission wavelength of ICAAc increases. It displays excitation/emission maxima of 466/553, 431/515, and 418/503 nm in water, dioxane, and hexane, respectively. The absorption maximum of ICAAc decreases with increasing pH. It displays absorption/emission maxima of 470/554 and 428/553 nm at pH 3 and 11, respectively, in aqueous Britton-Robinson buffer, and the fluorescence intensity increases as pH decreases. ICAAc can be used for live cell applications.
|1. Nagy, M., Racz, D., Nagy, Z.L., et al. Amino-isocyanoacridines: Novel, tunable solvatochromic fluorophores as phystiological pH probes. Sci. Rep. 9, 8250 (2019).
monoMICAAc is a solvatochromic fluorescent pH probe.1 As the polarity of the solvent increases, the emission wavelength of monoMICAAc increases. It displays excitation/emission maxima of 425/491, 437/515, and 472/554 nm in hexane, dioxane, and water, respectively. The absorption maximum of monoMICAAc decreases with increasing pH. It displays absorbance/emission maxima of 475/553 and 446/553 nm at pH 3 and 11, respectively, in aqueous Britton-Robinson buffer, and the fluorescence intensity increases as pH decreases. monoMICAAc can be used for live cell fluorescent applications.
|1. Nagy, M., Racz, D., Nagy, Z.L., et al. Amino-isocyanoacridines: Novel, tunable solvatochromic fluorophores as phystiological pH probes. Sci. Rep. 9, 8250 (2019).
CAY10761 is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4
|1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases/phosphodiesterases 1 inhibitors. Bioorg. Med. Chem. 17(22), 7816-7822 (2009).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Ghani, U., and Ullah, N. New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg. Med. Chem. 18(11), 4042-4048 (2010).|4. Amtul, Z., Rasheed, M., Choudhary, M.I., et al. Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles. Biochem. Biophys. Res. Commun. 319(3), 1053-1063 (2004).
Ald-Ph-amido-PEG11-C2-NH2 is an 11-unit polyethylene glycol (PEG) linker that is non-cleavable. It is specifically designed for use in the synthesis of antibody-drug conjugates (ADCs).