Epigenetics

Epigenetics
Epigenetics can be defined as acquired changes in chromatin structure that arise independently of a change in the underlying DNA
nucleotide sequence. Epigenetic modifications - including acetylation, methylation, phosphorylation, and ubiquitination, amongst others alter the accessibility of DNA to transcription machinery. Below you will find a sample of Tocris products related to epigenetics.
Product Description
Histone Demethylase Inhibitor
GSK J4 Cat. No. 4594
EtO2C
NH
N
N
N
N
GSK J4 is a histone demethylase JMJD3/UTX inhibitor
that blocks demethylation of histone H3K27. The
compound attenuates lipopolysaccharide (LPS)-induced
proinflammatory cytokine production in primary human
macrophages (IC50 = 9 µM for the inhibition of TNF-α
release). GSK J4 is cell permeable and an ethyl ester
derivative of GSK J1 (Cat. No. 4593).
(This probe is supplied in conjunction with the Structural Genomics Consortium)
Product Description
14.3.3 Proteins
Difopein (2145)
High affinity inhibitor of 14.3.3 proteins; induces
apoptosis
R18 (2144)
Inhibitor of 14.3.3 proteins; induces apoptosis
Bromodomains
I-BET 151 hydrochloride (4650)
BET bromodomain inhibitor
Size
Histone Acetyltransferases
Anacardic acid (3084)
Noncompetitive PCAF/p300 HAT inhibitor
10 mg
50 mg
C 646 (4200)
Selective p300/CBP HAT inhibitor
10 mg
50 mg
Histone Deacetylases
GSK J1 (4593)
Potent histone demethylase JMJD3/UTX inhibitor
10 mg
50 mg
GSK J4 (4594)
Histone demethylase JMJD3/UTX inhibitor; cell
permeable
10 mg
50 mg
MC 1568 (4077)
Selectively inhibits HDAC class II (IIa)
10 mg
50 mg
NCH 51 (3747)
Histone deacetylase inhibitor
10 mg
50 mg
Pyroxamide (4403)
Histone deacetylase inhibitor
10 mg
50 mg
Size
100 µg
Potent and Selective G9a/GLP Inhibitor
UNC 0646 Cat. No. 4342
1 mg
N
10 mg
50 mg
(+)-JQ 1 (4499)
Potent and selective BET bromodomain inhibitor
10 mg
PFI 1 (4445)
BET bromodomain inhibitor
10 mg
50 mg
DNA Methyltransferases
Decitabine (2624)
DNA methyltransferase inhibitor
10 mg
50 mg
Lomeguatrib (4359)
MGMT inhibitor
10 mg
50 mg
RG 108 (3295)
Non-nucleoside DNA methyltransferase inhibitor
10 mg
50 mg
NH
OMe
N
N
N
O
N
N
UNC 0646 is a potent and selective inhibitor of the
homologous protein lysine methyltransferases, G9a and GLP
(IC50 values are 6 and 15 nM for G9a and GLP, respectively).
The compound potently blocks G9a/GLP methyltransferase
activity in cells (IC50 = 10 nM in MCF7 cells) and exhibits
low cellular toxicity (EC50 = 4.7 µM in MCF7 cells). UNC
0646 is selective for G9a/GLP over a range of other
protein lysine methyltransferases and protein arginine
methyltransferases.
For a complete list of available products, please visit www.tocris.com
Product Description
L3MBTL1 MBT Domain Binder
UNC 926 hydrochloride Cat. No. 4516
Size
Hypoxia Inducible Factors
DMOG (4408)
Prolylhydroxylase inhibitor
10 mg
50 mg
O
IOX 2 (4451)
Potent, selective HIF1α prolyl hydroxylase-2
(PHD2) inhibitor
Br
N
10 mg
50 mg
N
.HCl
UNC 926 is a methyl-lysine reader antagonist that binds to
the MBT domain of the L3MBTL1 protein (Kd = 3.9 µM).
The compound selectively inhibits, in a dose-dependent
manner, the interaction between L3MBTL13XMBT-H4K20me1
in a peptide pull down assay.
Product Description
SBHA (3810)
Histone deacetylase inhibitor
Sodium 4-Phenylbutyrate (2682)
Histone deacetylase inhibitor
Size
50 mg
100 mg
TC-H 106 (4270)
Class I histone deacetylase inhibitor
10 mg
50 mg
Tranylcypromine hydrochloride (3852)
Irreversible inhibitor of MAO-A, MAO-B and LSD1
50 mg
Trichostatin A (1406)
Histone deacetylase inhibitor
1 mg
Tubacin (3402)
HDAC 6 inhibitor; inhibits α-tubulin
deacetylation
1 mg
Histone Methyltransferases
BIX 01294 (3364)
G9a-like protein and G9a histone lysine
methyltransferase inhibitor
Chaetocin (4504)
Selective histone methyltransferase SUV39H1
inhibitor
10 mg
50 mg
1 mg
JAK
Cucurbitacin I (1571)
Selective inhibitor of STAT3/JAK2 signaling
NSC 33994 (4338)
JAK2 inhibitor
10 mg
50 mg
MBT Domains
UNC 1215 (4666)
Potent and selective L3MBTL3 domain inhibitor
10 mg
50 mg
UNC 926 hydrochloride (4516)
Binds the MBT domain of L3MBTL1 polycomb
group protein
Poly(ADP-ribose) Polymerase
BYK 49187 (3735)
PARP-1 and PARP-2 inhibitor
10 mg
50 mg
UNC 0638 (4343)
Selective G9a and GLP histone lysine
methyltransferase inhibitor
10 mg
50 mg
UNC 0646 (4342)
Potent and selective G9a/GLP inhibitor
10 mg
50 mg
10 mg
50 mg
1 mg
NU 1025 (1401)
Potent PARP inhibitor
10 mg
50 mg
PJ 34 hydrochloride (3255)
Potent PARP inhibitor
10 mg
50 mg
XAV 939 (3748)
Tankyrase inhibitor; inhibits Wnt signaling
10 mg
50 mg
Protein Serine/Threonine Phosphatases
Okadaic acid (1136)
Protein phosphatase 1 and 2A inhibitor
25 µg
NSC 87877 (2613)
Potent inhibitor of shp2 and shp1 PTP
50 mg
BET Bromodomain Inhibitor
I-BET 151 hydrochloride UNC 0224 (3861)
Potent G9a histone lysine methyltransferase
inhibitor
1 mg
Cat. No. 4650
N
O
.HCl
N
NH
MeO
N
N
O
Scan this QR code with your smartphone to
view all products for epigenetics research on
the Tocris website.
I-BET 151 is a BET bromodomain inhibitor that blocks
recruitment of BET to chromatin. The compound induces
apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic
cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM
for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines
respectively) and reduces BCL2 expression in NOMO1 cells.
I-BET 151 improves survival in two rodent models of MLLfusion leukemia in vivo.
(Sold for research purposes under agreement from GlaxoSmithKline)
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© 2013 Tocris Cookson, Ltd. Tocris is an R&D Systems company

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