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.
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).
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).
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).