Reagents

An organism’s DNA contains distinct information units, genes, which code for the production of unique proteins that perform specific functions. Gene regulation is the process of determining which genes a cell will express. Protein synthesis is turned on or off in response to regulation mechanisms such as regulatory proteins that bind to specific sections of the DNA.
Gene regulation reagents have been developed for the investigation of protein synthesis and gene expression. They provide the ability to target and manipulate the function of specific genes in living cells, resulting in precise changes to a cell′s characteristics.
Researchers often use small molecules to alter the production of a specific protein in a cell in order to determine its function. This ability of small molecules to selectively modify gene expression makes them indispensable tools in functional genomics, target validation, drug development, and process improvement in biopharmaceutical manufacturing.
Sigma-Aldrich offers several enzyme inhibitors to further the study of gene regulation and expression.

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A9590 AP-1 Consensus Oligonucleotide  
PZ0127 CP-74416 methanesulfonate hydrate ≥98% (HPLC) CP-74416 is a primary Danofloxacin metabolite. The compound belongs to a group of quinolone antibiotic. CP-74416 is an inhibitor of the bacterial DNA gyrase.
SML0736 Dafadine A ≥98% (HPLC) Dafadine A is a selective inhibitor of C. elegans DAF-9 cytochrome P450, a key regulator of dauer formation, developmental timing and longevity. C. elegans has four life stages. In harsh environmental conditions, nematodes can convert to the L3 stage, known as the ""non-aging"" dauer stage, in which development ceases until improved conditions are sensed. Dafadine A can induce dauer formation and increased longevity in wild-type worms raised in nonstressful conditions. Dafadine A is the only inhibitor known to robustly inhibit DAF-9 in wild-type worms. It does not inhibit DAF-12 activity. Dafadine is active in mammalian systems, inhibiting CYP27A1, the mammalian functional ortholog of DAF-9 that oxidizes 4-cholesten-3-one to make 26-hydroxy-4-cholesten-3-one and Δ4-dafachronic acid, without inhibiting other sterol- and oxysterol-metabolizing P450s such as CYP7A1 or CYP7B1.
SML0826 FH1 ≥98% (HPLC) FH1 (BRD-K4477) was found to enhance hepatocyte functions and promote the differentiation of induced pluripotent stem cell–derived hepatocytes toward a more mature phenotype than what had previouslybeen obtainable. Human induced pluripotent stem (iPS) cells that are differentiated toward hepatocyte-like (iHep) cells typically show an immature hepatic phenotype and have limited use as a renewable source of functional human hepatocytes. Cultures treated with both FH1 (BRD-K4477) and another compound that induces proliferation, FPH1 (BRD-6125), contained larger colonies of iHep cells, which showed more pronounced hepatocyte morphologies with a more mature phenotype than previously obtainable.
SML0827 FPH1 ≥98% (HPLC) FPH1 (BRD-6125) induces functional proliferation of primary human hepatocytes in vitro. Human induced pluripotent stem (iPS) cells can be differentiated toward hepatocyte-like (iHep) cells, but replication is not great, and cells typically show an immature hepatic phenotype and have limited use as a renewable source of functional human hepatocytes. FPH1 induced hepatocyte colonies were used in conjunction with FH1 (BRD-K4477) to induce a more mature phenotype. Cultures treated with both FH1 and FPH1 contained larger colonies of hepatocyte-like (iHep) cells, which showed more pronounced hepatocyte morphologies with a more mature phenotype than previously obtainable.
SML0828 FPH2 ≥98% (HPLC) FPH2 (BRD-9424) induced functional proliferation of primary human hepatocytes in vitro. Human induced pluripotent stem (iPS) cells can be differentiated toward hepatocyte-like (iHep) cells, but replication is not great, and cells typically show an immature hepatic phenotype and have limited use as a renewable source of functional human hepatocytes. FPH2 induced hepatocyte doublings at a rate consistent with reported liver regeneration kinetics. FPH2 can be used in conjunction with FH1 (BRD-K4477), which induces a more mature phenotype.
SML1409 Madrasin ≥98% (HPLC) Madrasin is a potent and cell penetrant splicing inhibitor that interferes with the early stages of spliceosome assembly. Madrasin stalls spliceosome assembly at the A complex.
M2070 Merbarone ≥98% (HPLC), solid Selective topoisomerase II inhibitor. Blocks topo II-mediated DNA cleavage without stabilizing DNA-topo II-cleavable complexes. Induces apoptosis in CEM cells via caspase 3 dependent mechanism.
SML0442 ML239 ≥98% (HPLC) ML239 is an inhibitor of breast cancer stem cells found from a screen using stem cell-like human mammary epithelial cells (HMLE). ML239 inhibited cancer stem cells with an IC50 of 1.16 μM with 24-fold selectivity against the control cell line.
SML1219 ML243 ≥98% (HPLC) ML243 is a potent and selective inhibitor of cancer stem-like cells (CSCs) that selectively eradicate CSCs in heterogeneous cancer cell populations.
S8446 SIRT1 human recombinant, expressed in E. coli, N-terminal histidine tagged, ≥90% (SDS-PAGE), buffered aqueous glycerol solution Sirtuins are a family of NAD+ dependent deacetylases that remove an acetyl group from the e-amino group of lysine residues. The proteins within this family are named after the first protein discovered, from yeast, called Sir2 (Silent Information Regulator 2). The proteins are conserved from bacteria to higher eukaryotes. In humans, there are seven Sir2 family members (SIRT1 to SITR7). SIRT1 plays a pivotal role in the regulation of cellular differentiation, metabolism, cell cycle, apoptosis and regulation of p53. Several targets for SIRT1 were identified among them Lys382 of p53. Using RNA interference, additional targets were identified. It was demonstrated that reduced levels of human SIRT1 led to increased acetylation of Histone H4-Lys16, H4-Lys20, and Histone H3-Lys9 as well as histone H1-Lys26.
S6321 Suptopin-2 ≥98% (HPLC), solid Suptopin-2 affects cell cycle progression and stability of microtubules. It induces cell cycle arrest by regulating the nucleocytoplasmic transport of cyclin B1.1
Sutopin-2 is a suppressor of topoisomerase II inhibition. Reverses cell cycle arrest; bypass of checkpoint function. Has inherent fluorescence and a distinct advantage in identification of molecule targets; effective concentraion in the μM range.
T9194 Topoisomerase I from vaccinia virus buffered aqueous glycerol solution Topoisomerase I from vaccinia virus also refers as TOPO ®I is a type I DNA topoisomerase, which cleaves DNA at the preferred sequence [5′(C/T)CCTTI]. The product assists in releasing the supercoiling and torsional tension of DNA by cleaving and religating the phosphodiester bonds in a single strand of DNA.
Topoisomerase I relaxes supercoiled DNA molecules. The enzyme initiates transient breakages and rejoins of phosphodiester bonds in superhelical turns of closed-circular DNA. Enzyme activity is independent of right- and left-handed superhelices.
T8552 Trichostatin A ≥98% (HPLC), from Streptomyces sp. Inhibits histone deacetylase at nanomolar concentrations; resultant histone hyperacetylation leads to chromatin relaxation and modulation of gene expression. May be involved in cell cycle progression of several cell types, inducing cell growth arrest at both G and G/M phases; may induce apoptosis. Enhances the efficacy of anticancer agents that target DNA.
T1952 Trichostatin A, Ready Made Solution 5 mM in DMSO (0.2 μm-filtered), from Streptomyces sp. Trichostatin A (TSA) is a Streptomyces metabolite, which specifically inhibits mammalian histone deacetylase at a nanomolar concentration and causes accumulation of highly acetylated histone molecules in mammalian cells. For that reason, trichostatin A is a tool to study the consequences of histone acetylation in vivo. Trichostatin A induces cell differentiation, cell cycle arrest, reversal of transformed cells morphology, and apoptosis and is able to modulate transcription. TSA has been used to establish a new cloning technique, which increases the success rates for mouse cloning.