10 products were found matching "Cay16275"!

The cystic fibrosis (CF) gene encodes a cAMP-regulated chloride channel, the CF transmembrane conductance regulator (CFTR). PPQ-102 is a cell-permeable pyrimido-pyrrolo-quinoxalinedione that reversibly inhibits CFTR chloride channels with an IC50 value of 90 nM. At 0.5-5 µM, PPQ-102 has been used to reduce the size...

Nourseothricin is a broad-spectrum antibiotic produced by Streptomyces variants that inhibits protein synthesis by inducing miscoding. It is commonly used as a dominant selection antibiotic for genetically modified bacteria, yeasts, fungi, protozoa, plants, and mammalian cells. Selection of recombinant strains is...

Polycomb complex protein BMI-1 is a polycomb ring finger oncogene that regulates the p16 and p19 cell cycle inhibitor genes. It is necessary for efficient self-renewing cell divisions of stem cells in several tissues and can be over-expressed in tumors. PTC-209 is a BMI-1 inhibitor (IC50 = ~ 0.5 µM) that...

Bruton's tyrosine kinase (BTK) is a member of the BTK/Tec family of protein tyrosine kinases involved in signal transduction pathways regulating proliferation, survival, migration, and tissue homing of B-cells. Ibrutinib is an irreversible inhibitor of BTK (IC50 = 0.5 nM) that selectively blocks B cell activation,...

PR-619 is a general inhibitor of deubiquitylating enzymes (DUBs), significantly reducing the activity of a panel of DUBs with EC50 values ranging from 5-20 µM. It is cell-permeable and reversible in its action. It is selective for DUBs over other proteases. PR-619 induces the accumulation of polyubiquitinated...

The immunoproteasome is a specialized, inducible proteasome that generates peptides presented on major histocompatibility complex (MHC) class I molecules to cytotoxic T cells. Stimulation of cells with inflammatory cytokines such as IFN-gamma leads to the replacement of constitutive catalytic proteasome beta...

Jumonji AT-rich interactive domain 1 (JARID1) demethylases mediate the removal of methyl groups from trimethylated lysine 4 on histone 3 (H3K4me3). PBIT is a reversible, cell-permeable inhibitor of JARID1 family demethylases (IC50s = 6, 3, 4.9, and 28 µM for JARID1A, JARID1B, JARID1C, and JARID1D, respectively). It...

RKI-1447 is an inhibitor of the Rho-associated kinases ROCK1 and 2 (IC50s = 14.5 and 6.2 nM, respectively) that functions by binding to the ATP binding site of the kinase. In cancer cells, RKI-1447 at a concentration of 100 nM has been found to suppress the activation of ROCK substrates myosin light chain (MLC)-2...

PD 0332991 is an orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM) with no activity against a panel of 36 additional protein kinases. It has been reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma...

S1RA is a sigma-1 (sigma1) receptor antagonist (Ki = 17 nM). It is selective for sigma1 receptors over sigma2 receptors (Ki = 9,300 nM), as well as a panel of 170 additional receptors at 1 µM. S1RA reduces capsaicin-induced mechanical allodynia, formalin-induced licking and biting behavior, and partial sciatic nerve...