DNA-RNA Transcription Regulators

D5816

()-Depudecin >95% (HPLC), from microbial

Inhibitor of histone deacetylase pricing (HDAC) both in vivo and in vitro. Alters the spindle shaped morphology of v-Ha-rastransformed NIH3T3 cells to a flattened shape and induces an intricate actin stress fiber network in these cells and in MG63 osteosarcoma cells. Also exhibits anti-angiogenic activity. HDAC Inhibitor tested as an anti-cancer drug; butyric acid pro-drug pricing

A8236

AN-9 95% (HPLC)

A7236

Anacardic acid 98% (HPLC) Apicidin 98% (HPLC), from microbial

Anacardic acid is a HAT (Histone Acetyltransferase) inhibitor. Potent (nM) cell permeable inhibitor of histone deacetylase. Also, exhibits antiprotozoal and potential antimalarial properties. Apicidin has antiproliferative activity on HeLa cells accompanied by cell arrest at the G1 phase. In addition, it induces selective changes in the expression of p21 and gelsolin. BML-210 is a histone deacetylase inhibitor. Treatment of A549 cells with BML-210 results in a dosedependent increase in

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A8851

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B8063

BML-210 98% (HPLC), powder

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acetylated histone levels (EC50 = 36 M). In HeLa extracts, the IC50 for inhibition of HDAC activity is 80 M. PZ0130 CP-64434 hydrate 98% (HPLC) C9873 CPTH2 98% (HPLC), powder CP-064434 is an antibiotic; anti-proliferative HDAC inhibitor. pricing

CPTH2 is a histone pricing acetyltransferase (HAT) inhibitor modulating the Gcn5 network. Histone Acetyltransferase (HAT) inhibitor modulating Gcn5 network. Histone acetyltransferases (HATs) act as transcriptional coactivators. Histone acetylation plays an important role in regulating the chromatin structure and is tightly regulated by two classes of enzyme, histone acetyltransferases (HAT) and histone deacetylases (HDAC). Deregulated HAT and HDAC activity plays a role in the development of a range of cancers. Consequently, inhibitors of these enzymes have potential as anticancer agents. Diphenylacetohydroxamic acid pricing is a class IIa selective histone deacetylase inhibitor. Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8. Garcinol is a HAT (histone acetyltransferase) inhibitor. Garcinol is anti-inflammatory and anti-carcinogenic. Histone acetyltransferases provide opposing enzymatic mechanisms for chromatin remodeling and epigenetic control of gene expression. pricing

D6071

Diphenylacetohydroxamic acid 98% (HPLC) Droxinostat 98% (HPLC)

D6321

G5173

Garcinol 95%

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HATs are involved in regulation of transformation, transcription, differentiation, apoptosis, embryonic development and oncogenesis. IC50 p300 = 7 mM; IC50 PCAF = 5 mM (similar to anacardic acid). Garcinol is highly toxic compared to LTK-14, and does not discriminate between p300 and PCAF. I4159 ITSA-1 98% (HPLC), solid ITSA-1 is a suppressor of pricing Trichostatin A (TSA) and a molecular tool for dissecting gene regulation by distinct aceytlation events (histone and tubulin). ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but not other HDAC inhibitors. ITSA-1 rreverses TSA induced histone acetylation, overall deacetylation. ITSA-1 also reverses TSA induced cell cycle arrest and apoptosis. Effective range 50 M. M344 is a HDAC inhibitor; pricing subtype selective for HDAC6 over HDAC1. M344 inhibits HDAC (IC50 = 100 nM) and also inhibits hyperacetylation of histone H4, terminal cell differentiation, transcription (globin), and tumor cell death. MC1568 is a selective class II (IIa) histone deacetylas (HDAC II) inhibitor. Selective HDAC1 substrate (over HDAC6, class I over class II). HDAC inhibitor; more potent than the majority of HDAC inhibitors except for SAHA (gold standard). pricing

M5820

M344 98% (HPLC), solid

M1824

MC1568 97% (HPLC)

M2195

MOCPAC 95% (HPLC), solid PTACH 98% (HPLC), solid

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P5874

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S8446

SIRT1 human recombinant, expressed in Escherichia coli, N-terminal histidine tagged, >90% (SDSPAGE), buffered aqueous glycerol solution

Sirtuins are a family of NAD+ pricing 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 p53.1 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-Lys26.2 Salermide is a novel Sirtuin 1 pricing (Sirt1) and Sirtuin 2 (Sirt2) inhibitor (III histone deacetylases inhibitor). In vitro Salermide has a stronger inhibitory effect on Sirt2 than on Sirt1. Salermide induces massive apoptosis in tumor cells. The activity was ascribed to effect of Salermide to the reactivation of proapoptotic genes epigenetically repressed exclusively in cancer cells by Sirt1. Salermide is a stronger Sirtuin inhibitor than sirtinol (Cat. No.S7942). Histone deacetylase inhibitor with lower toxicity than pricing

S8825

Salermide 98% (HPLC)

S7817

Scriptaid 95% (H-NMR), solid

trichostatin A; used to enhance protein expression. S4068 Splitomicin 98% (HPLC), solid Trapoxin A 98% (HPLC), from Helicoma ambiens Sir2p (silent information regulator) and HDAC inhibitor. pricing

T2580

Trapoxin A is a pricing cyclotetrapeptide and a histone deacetylase (HDAC) inhibitor. It increases the level of chromatin acetylation associated with histone H3 at low nanomolar concentrations.1 Unlike the reversible HDAC inhibition induced by TCA, Trapoxin A irreversibly inhibites HDAC activity in crude cell lysates, and induces the accumulation of hyperacetylated core histones in a number of mammalian cell lines and tissues.2, Histone acetylation and methylation have been studied extensively for their anti-tumor activities in carcinogenesis and Trapoxin has been suggested as a potential anticancer agent for pre-clinical trials.3

T8552

Trichostatin A 98% Inhibits histone deacetylase at pricing (HPLC), from Streptomyces nanomolar concentrations; sp. 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. Trichostatin A 5 mM in DMSO (0.2 m-filtered), from Streptomyces sp. Trichostatin A (TSA) is a Streptomyces metabolite, which specifically inhibits pricing

T1952

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.1 Trichostatin A induces cell differentiation, cell cycle arrest, reversal of transformed cells morphology, and apoptosis and is able to modulate transcription.2,3 TSA has been used to establish a new cloning technique, which increases the success rates for mouse cloning.4