BIOMOL Online September 2006
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Chemical Genomics Drug Discovery Epigenetics Neuroscience Signal Transduction Ubiquitons & Zomes

In this issue:

 
September 2006
Histone Acetyltransferase Reagents
Axl, Fak, Flt, Kit, Pyk Kinases
Tyrosine Hydoxylase Antibodies

Gankyrin Reagents
USP2, Deubiquitinating Enzyme
PR26, Proteasome Inhibitor
SP100, SUMOylation Substrate
FEATURED PRODUCT
Histone Acetyltransferase (HAT) Reagents
Garcinol structure
Garcinol (Cat. # GR-343)
Garcinol is a polyisoprenylated benzophenone derivative isolated from Garcinia indica.  It is a potent inhibitor of histone acetyltransferases (HATs) p300 (IC50 = 7 microM) and PCAF (IC50 = 5 microM) both in vitro and in vivo.  HAT activity-dependent chromatin transcription was inhibited by garcinol, but it had no effect on naked DNA transcription.  It is a potent inducer of apoptosis in HeLa cells where it down-regulates global gene expression.
Enzymes
CBP (Cat. # SE-452)
CBP and its paralog p300 play regulatory roles in transcription, DNA repair and replication, the cell cycle, p53 turnover, and nuclear import. 

p300
(Cat. # SE-451)
CBP and p300 have been shown to acetylate a variety of non-histone proteins including p53, DNA polymerase beta and nuclear import factors.


pCAF
(Cat. # SE-271)
In addition to the histones H3 and H4, pCAF has been shown to acetylate transcription factors p53 and p65. 


hGCN5
(Cat. # SE-272)
hGCN5L is the catalytic HAT subunit of the transcriptional coactivator complexes STAGA and TFTC.

Substrates
Histone H3 Peptide (Cat. # P-271)
Comprising residues 5-23 of the human histone H3 N-terminal tail, including Lys-14, a preferred acetylation site for the GCN5/pCAF family of histone acetyltransferases (HATs).

p53 Peptide
(368-386) (Cat. # P-198)
Derived from the C-terminal regulatory domain of p53, this peptide comprises five lysines, including three preferentially acetylated by p300 (K373, K381, K382).

For related products:
acetylated lysine antibodies | HDAC assays | HDAC enzymes | HDAC substrates | HDAC inhibitors

NEW PRODUCTS
Kinases

Axl Receptor Tyrosine Kinase

Axl (also known as Ark, Ufo, and Tyro7) is the prototype of a family of transmembrane receptor tyrosine kinases, which also includes Tyro3 and Mer, that bind to the vitamin K-dependent protein ligands growth arrest-specific gene 6 (Gas6), and protein S. Axl, Tyro3, and Mer are variably expressed in neural, lymphoid, vascular, and reproductive tissues and in different primary cells and tumor cell lines. Recent studies indicate that Axl plays an important role in vascular biology, cell growth and protection from apoptosis in normal and cancer cells. Axl activation results in autophosphorylation and phosphorylation of cytoplasmic substrates, including phosphatidylinositol 3-kinase (PI-3K), Akt, S6K, Src kinase, ERK, p38, STAT3, and NF-kappaB.

Axl (Cat. # SE-449)
Active Axl expressed in insect cells: amino acids 473 to 894.  GenBank ID: NM_021913.

FAK (Cat. # SE-448)
Active FAK expressed in insect cells: amino acids 411-686.  GenBank ID L13616. 

Flt1 (Cat. # SE-445
Active Flt1 expressed in insect cells: amino acids 783 to end.  GenBank ID AF063657. 

Flt3 (Cat. # SE-446
Active Flt3 expressed in insect cells: amino acids 564 to end.  GenBank ID NM_004119.

Kit (Cat. # SE-447)
Active Kit expressed in insect cells: amino acids 544 to end.  GenBank ID BC071593.

Pyk2 (Cat. # SE-450)
Active FAK expressed in insect cells: amino acids 411-686.  GenBank ID L13616.

Neuroscience
Tyrosine Hydroxylase Antibodies
Tyrosine hydroxylase (TH) is the rate-limiting enzyme in the synthesis of the catecholamines Dopamine and Norepinephrine. TH antibodies can therefore be used as markers for dopaminergic and noradrenergic neurons in the studies of depression, schizophrenia, Parkinson’s disease and drug abuse. TH antibodies can also be used to explore basic mechanisms of dopamine and norepinephrine signaling. The activity of TH is regulated, in part, by phosphorylation at Ser8, Ser19, Ser 31 and Ser40. Phosphorylation of Ser31 and Ser40 increase enzymatic activity. Phosphorylation at Ser19, while having no direct effect on activity, increases the rate of phosphorylation at Ser40. Phospho-specific TH antibodies can be used to great effect in studying this regulation and in identifying the cells in which TH phosphorylation occurs.
TH staining of light and dark-adapted retina Immunohistochemical staining of retina with the tyrosine hydroxylase (pS40) antibody. The left panel is a dark adapted retina, while the right panel shows labelling of two amacrine cells in a light-stimulated retina sample.
Tyrosine Hydroxylase (pS19), rabbit pAb (Cat. # SA-544)
Tyrosine Hydroxylase (pS31), rabbit pAb (Cat. # SA-545)
Tyrosine Hydroxylase (pS40), rabbit pAb (Cat. # SA-546)
Tyrosine Hydroxylase, mouse mAb (Cat. # SA-499)
Recognizes a broad range of mammalian TH.  Applications:  WB, IF, IHC.
 
Tyrosine Hydroxylase, sheep pAb (Cat. # SA-498)
Recognizes a broad range of mammalian TH.  Applications: WB, IF, IHC.
Tyrosine Hydroxylase, rabbit pAb (Cat. # SA-497)
Recognizes a broad range of mammalian TH.  Applications:  WB, IF, IHC.  
Ubiquitons & Zomes
Gankyrin

Gankyrin is an oncoprotein with potent cell cycle and apoptotic properties that is overexpressed in hepatocarcinogenesis and in hepatocellular carcinomas.  It is known to play a role in the regulation of the phosphorylation of the retinoblastoma protein by CDK4, and to enhance the ubiquitinylation of p53 by MDM2.
Gankyrin was recently found to be a component of the 26S proteasome. This suggests a biochemical pathway by which gankyrin may not only control  the rate of p53 ubiquitinylation through MDM2 but may also act as an adaptor protein that delivers p53 to the 26S proteasome for degradation. 

Gankyrin, His6-tagged (Cat. # UW9815)

Gankyrin, rabbit pAb (Cat. # PW8325)

USP2 Fragment [271-618], untagged (Cat. # UW9850)
USP2 is a deubiquitinating enzyme overexpressed in cancer cells. Inhibition of USP2 results in apoptosis of transformed prostate cells.

PR26 (Cat. # PW9790)  
The PR (proline and arginine rich) series of peptides have been shown to interact with subunit alpha7 of the 20S proteasome, interfering with the efficient movement necessary for the gating mechanism.
SP100 Fragment [241-360], GST-tagged  (Cat. # UW9825)
SP100 is an interferon-inducible protein that has been demonstrated to be SUMOylated.  The SP100 Fragment [241-360] can be SUMOylated at Lys297 in vitro using our SUMOylation Kit (Cat. # UW8955).
26S Proteasome

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