DNA-RNA Transcription Regulators

STAT3 Signaling Pathway
Signal Transducers and Activators of Transcription (STATs) are transcription factors that are phosphorylated by JAK kinases in response to cytokine activation. Upon activation, the STATs dimerize and are localized to the nucleus where they activate transcription of cytokine-responsive genes. There are at least three JAK kinases and at least six distinct STAT proteins involved in this complex signaling pathway. Cytokines that activate STAT3 include growth hormone, IL-6 family cytokines, and G-CSF. STAT3, as well as STAT5, induces progression through the cell cycle, prevents apoptosis and upregulates oncogenes, such as c-myc and bcl-x and may play a role in oncogenesis. STAT3 has been shown to play a critical role in hematopoiesis. The importance of STAT3 is underscored by the failure of mice lacking STAT3 to survive embryogenesis. Crosstalk from pathways other than JAK kinases also leads to phosphorylation and activation of STAT3 as indicated by a role of mTOR (mammalian target of rapamycin, or p70 S6 kinase) and MAP kinase pathways in STAT3 activation and signaling.

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Description	Biochem/physiol Actions	Product #
Actinomycin D from Streptomyces sp., ~98% (HPLC)	An antineoplastic antibiotic that inhibits cell proliferation by forming a stable complex with DNA and blocking the movement of RNA polymerase which interferes with DNA-dependent RNA synthesis. Induces apoptosis. Potent antitumor agent. For cell culture applications, actinomycin D is used as a selection agent and is used in banding techniques to differentiate between different regions of chromosomes.	A1410
Actinomycin D ≥95%, from Streptomyces sp., cell culture tested	An antineoplastic antibiotic that inhibits cell proliferation by forming a stable complex with DNA and blocking the movement of RNA polymerase which interferes with DNA-dependent RNA synthesis. Induces apoptosis. Potent antitumor agent. For cell culture applications, actinomycin D is used as a selection agent and is used in banding techniques to differentiate between different regions of chromosomes. Mode of Action: Complexes with DNA and interferes with RNA synthesis.	A9415
Actinomycin D from Streptomyces sp., ~95% (HPLC)	An antineoplastic antibiotic that inhibits cell proliferation by forming a stable complex with DNA and blocking the movement of RNA polymerase which interferes with DNA-dependent RNA synthesis. Induces apoptosis. Potent antitumor agent. For cell culture applications, actinomycin D is used as a selection agent and is used in banding techniques to differentiate between different regions of chromosomes.	A4262
AGK2 ≥97% (HPLC), solid	AGK2 is a SIRT2 inhibitor. AGK2 rescues dopamine neurons from α-synuclein toxicity in Parkinson's disease models. IC50 for SIRT2 = 3.5 uM. AGK2 is >15-fold more selective for SIRT2 than SIRT1 and SIRT3. AGK2 may be the most selective SIRT2 inhibitor available.	A8231
α-Amanitin from Amanita phalloides, ≥90% (HPLC), powder	The major toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but does not inhibit RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.	A2263
β-Amanitin from Amanita phalloides ~90% (HPLC)	Toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but not RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.	A1304
α-Amanitin oleate ~90% (HPLC)	The major toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but does not inhibit RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.	A7975
β-Amanitin–poly-L-lysine bound ~90%	Toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but not RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.	A8100
Apicidin ≥95%, from microbial, solid	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.	A8851
BATCP ≥98% (HPLC), solid	HDAC 6 selective substrate (over HDAC 1, Class II over Class I).	B4061
BIX 01294 ≥98% (HPLC), white solid	BIX 01294 is a selective histone methyl transferase inhibitor. In its inhibition of the histone lysine methyltransferases, BIX 01294 does not compete with cofactor S-adenosyl-methionine. The target enzyme is G9a, and it selectively impairs G9a HMTase and the generation of H3K9me2 in vitro.¹	B9311
CHIC-35 ≥97% (chiral, HPLC), solid	CHIC-35 is cell-permeable, metabolically stable, and very potent inhibitor of SIRT1; IC₅₀ of S-isomer is 60 nM; IC₅₀ of mixed isomers is 124 nM. There is no inhibition of SIRT3 or HDAC. The IC₅₀ for SIRT2 is 2.77 μM. Sirtuins are protein deacetylases, which represent a new class of histone deacetylases (HDAC) involved in gene silencing. SIRT modulators are potential therapeutics for cancer, diabetes, muscle differentiation, heart failure, neurodegeneration, and aging.	C8742
(−)-Depudecin >95% (HPLC), from microbial	Inhibitor of histone deacetylase (HDAC) both in vivo and in vitro. Alters the spindle shaped morphology of v-Ha-ras-transformed 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.	D5816
5,6-Dichlorobenzimidazole 1-β-D-ribofuranoside	Inhibitor of RNA synthesis; causes premature termination of transcription. CK2 (casein kinase-2) inhibitor.	D1916
Distamycin A hydrochloride from Streptomyces distallicus ≥90% (TLC)	Reported to specifically inhibit the initiation of RNA synthesis.	D6135
(−)-Epigallocatechin gallate ≥95%, from green tea	Antioxidant polyphenol flavonoid that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors.	E4143
(−)-Epigallocatechin gallate ≥80% (HPLC), from green tea		E4268
1-(4-Hexyphenyl)-2-propane-1-one ≥98% (HPLC), oil	Small molecular irreversible covalent inhibitor of thyroid hormone receptor-β (TRβ) interaction with coactivator (SRC2).	H6039
Hydralazine hydrochloride	Inhibits DNA methyltransferase and modulates epigenetic regulation of gene expression. Non-selective MAO-A/B inhibitor; antihypertensive; semicarbazide-sensitive amine oxidase inhibitor.	H1753
ITSA-1 ≥98% (HPLC), solid	ITSA-1 is a suppressor of 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 μM.	I4159
JFD00244 ≥98% (HPLC), solid	JFD00244 is a SIRT (sirtuin, human silent information regulator) inhibitor.	J4829
M344 ≥98% (HPLC), solid	M344 is a HDAC inhibitor; subtype selective for HDAC6 over HDAC1. M344 inhibits HDAC (IC₅₀ = 100 nM) and also inhibits hyperacetylation of histone H4, terminal cell differentiation, transcription (γ-globin), and tumor cell death.	M5820
MOCPAC ≥95% (HPLC), solid	Selective HDAC1 substrate (over HDAC6, class I over class II).	M2195
Pedibin precursor peptide >92% (HPLC), solid		M0688
Procainamide hydrochloride	Inhibits DNA methyltransferase and modulates epigenetic regulation of gene expression. Na⁺ channel blocker and Class IA anti-arrhythmic.	P9391
PTACH ≥98% (HPLC), solid	HDAC inhibitor; more potent than the majority of HDAC inhibitors except for SAHA (gold standard).	P5874
RG108 ≥98% (HPLC), solid	RG108 is a DNA methyltransferase (DMNT) inhibitor. It reactivates tumor suppressor gene expression (p16, SFRP1, secreted frizzled related protein-1, and TIMP-3) in tumor cells by DNA demethylation. RG108 also inhibits human tumor cell line (HCT116, NALM-6) proliferation and increased doubling time in culture.	R8279
Rifampicin ≥97% (HPLC), powder	Inhibits the assembly of DNA and protein into mature virus particles. Mode of Action: Inhibits initiation of RNA synthesis by binding to β-subunit of RNA polymerase.	R3501
Rifampicin plant cell culture tested, ≥97% (HPLC), crystalline	Inhibits the assembly of DNA and protein into mature virus particles. Mode of Action: Inhibits initiation of RNA synthesis by binding to β-subunit of RNA polymerase.	R7382
α-Sarcin from Aspergillus giganteus ≥95% (SDS-PAGE), lyophilized powder	RNase that inactivates the 60S ribosomal subunit.	S6907
Scriptaid ≥95% (H-NMR), solid	Histone deacetylase inhibitor with lower toxicity than trichostatin A; used to enhance protein expression.	S7817
SIRT1 human recombinant, expressed in Escherichia 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 p53.¹ 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	S8446
SIRT1 Assay Kit sufficient for 100 assays	Sirtuins (Sir2) are an evolutionarily conserved family of NAD⁺ dependent histone/protein deacetylases that tightly couple the cleavage of NAD⁺ and the deacetylation of protein substrates. The reaction products are nicotinamide, the deacetylated product, and a novel metabolite, 2′-O-acetyl-ADP-ribose. The proteins within this family are named after the first protein discovered from this family, Sir2 (Silent Information Regulator 2). Besides gene silencing, sirtuin proteins are important in other processes such as cell cycling regulation and fatty acid metabolism. SIRT1 is the human homolog of Sir2 and the one most studied to date. SIRT1 mediates p53 dependent process, transcription regulation, muscle differentiation, adipogenesis, and protection from axonal degeneration. SIRT1 also participates in early embryogenesis, neurogenesis, and cardiogenesis.	CS1040
SIRT6 human recombinant, expressed in Escherichia coli, N-terminal histidine tagged, >90% (SDS-PAGE), buffered aqueous glycerol solution	SIRT6 is a nuclear, chromatin-associated protein with an ADP-ribosyltransferase activity. SIRT6 promotes resistance to DNA damage and suppresses genomic instability in mouse cells in association with a role in base excision repair (BER). It has been shown that SIRT6 deficiency in mice leads to the development of an acute degenerative aging-like phenotype. Although SIRT6 is a member of the SIRT family of proteins, it is possible that SIRT6 is not an NAD⁺protein deacetylase.^1,²	S3947
Sirtinol ≥95% (HPLC)	Sirtinol inhibits yeast Sir2p transcriptional silencing activity in vivo, yeast Sir2p and human SIRT2 deacetylase activity in vitro. Sirtinol inhibits yeast Sir2p transcriptional silencing activity in vivo, yeast Sir2p, and human SIRT2 deacetylase activity in vitro.	S7942
Splitomicin ≥98% (HPLC), solid	Sir2p (silent information regulator) and HDAC inhibitor.	S4068
STAT1-α/β (699-709) >98% (HPLC), solid		S9188
STAT4 control peptide trifluoroacetate salt >90% (HPLC), lyophilized powder	Positive control peptide for the STAT4 rabbit polyclonal antibody.	S4690
Trichodion >95%, solid		T1945
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.	T8552
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.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	T1952
WP900 hydrochloride ≥95% (HPLC), solid	Synthetic left-handed enantiomer of (+)-daunorubicin, anti-tumor antibiotic, binds to right-handed B-form DNA under low salt conditions.	W4013

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