ph-11

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.

VS-II-173 is a novel potent Pim1 and Pim3 inhibitor, selectively inducing AML cell death.

SI-2 hydrochloride (EPH 116 hydrochloride) is a highly promising inhibitor of SRC-3 SMI: SRC-3 (PPI)(IC50 values of 3-20 nM for breast cancer cell death), with acceptable oral availability.

Phosphostim, a gamma9deta2 T lymphocytes agonist, is used potentially for the treatment of renal cell carcinoma, HCV infection.

Azodicarbonamide is the first nucleocapsid inhibitor known to inhibit HIV-1 and various retroviruses by targeting the nucleocapsid CCHC domains. In a standard cellular antiviral assay, the compound inhibited HIV-1RF-induced CEM-SS cytopathy with an EC50 value of 38 µM.

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-NH-Boc is a non-cleavable, 11-unit polyethylene glycol (PEG) linker used in the synthesis of antibody-drug conjugates (ADCs).

Ald-Ph-amido-PEG11-C2-NH2, an 11-unit non-cleavable polyethylene glycol (PEG) linker, is specifically designed for the synthesis of antibody-drug conjugates (ADCs).

AKBA (3-O-Acetyl-11-keto-beta-boswellic acid), a natural component from frankincense, is a novel activator of Nrf2.

TRITC-dextran MW 500000 (Tetramethyl rhodamine isothiocyanate glucan, MW 500000) is a fluorescent dye with a molecular weight of 500 kD. It has an excitation wavelength of 555 nm. This compound is utilized in drug delivery due to the stability of TRITC across a broad pH range (pH 2–11) and its resistance to photobleaching.

TRITC-dextran MW 20000 is a fluorescent dye with a molecular weight of 20 kD and an excitation wavelength of 555 nm. This compound is capable of penetrating the vasculature and can be used to label plasma for visualizing the vascular system. Furthermore, TRITC-dextran MW 20000 is employed in drug delivery due to its stability across a wide pH range (pH 2–11) and its resistance to photobleaching.

TRITC-dextran (MW 70000) is a fluorescently labeled dextran with a molecular weight of approximately 70 kDa and an excitation wavelength of 555 nm, and due to the high photostability of TRITC across a pH range of 2–11 combined with strong resistance to photobleaching, TRITC-dextran (MW 70000) is frequently applied in drug delivery research, vascular permeability studies, and fluorescence-based tracking of macromolecular transport.

TRITC-dextran MW 40000 is a fluorescent dye with a molecular weight of 40 kD. Its excitation wavelength is 555 nm. This compound can penetrate blood vessels and label plasma to visualize the vascular system. It is utilized in drug delivery systems because TRITC maintains stability across a broad pH range (pH 2–11) and exhibits resistance to photobleaching.

TRITC-dextran MW 150000 is a fluorescent dye with a molecular weight of 150 kD. It has an excitation wavelength of 555 nm. This compound is utilized in drug delivery systems due to its stability across a broad pH range (pH 2–11) and resistance to photobleaching.

TRITC-dextran MW 2000000 is a fluorescent dye with a molecular weight of 2000 kD. It possesses an excitation wavelength of 555 nm and is utilized in drug delivery systems. Its stability over a wide pH range (pH 2–11) and resistance to photobleaching make it particularly useful for this application.

TRITC-dextran MW 4000 is a fluorescent dye with a molecular weight of 4 kD and an excitation wavelength of 555 nm. It is known for its vascular permeability and ability to label plasma for imaging the vascular system. This compound is utilized in drug delivery due to its stability across a broad pH range (pH 2–11) and resistance to photobleaching.