New Products - Tocris Bioscience · PDF fileNew Products Tree of Heaven Ailanthus altissima...

New Products

Tree of HeavenAilanthus altissimaA Source of Ailanthone

Products by Pharmacology• 7-TM Receptors• Enzymes• Ion Channels

Products for Cell Biology• Epigenetics• Fluorescent Imaging• Signal Transduction• Stem Cells

Spring and Summer 2017 | Euro

New Products by Pharmacology

2 |

7-TM Receptors7-TM receptors are integral membrane proteins containing seven membrane-spanning helices that are coupled to G proteins on the intracellular face of the membrane. Upon ligand binding, the receptor undergoes a conformational change, activating the G protein and triggering signal transduction.

New Products – Spring and Summer 2017Welcome to our New Product Guide, containing the latest additions to our product range over the last six months. Products are categorized by biological targets for easy identification, or simply browse the guide to see what is newly available. Our products are of the highest purity and full respect for third party intellectual property rights comes as standard.

7-TM Receptors

HO

NH

SO

NHNS

F

Cl

N

AZ 10397767 (5872)Potent CXCR2 antagonist

HNN

O

HN

Cl

O

OMe

OMe

OMe

H

ML 339 (5943)Potent and selective hCXCR6 antagonist

S N OH

O

HN

ZQ 16 (6001)Selective GPR84 agonist

OMe

NO2

N

O

CO2H

NH2

O2N

MDNI-caged-L-glutamate (5785)Stable photoreleaser of L-glutamate

N N

N

HN O

O

HO

O

Ro 6842262 (5913)Potent LPA1 antagonist

O

NO

SO O

ML 233 (5966)Non-peptide apelin receptor agonist

Cys-Arg-Pro-Arg-Leu-Cys-Lys-His-Cys-Arg-Pro-Arg-Leu-Cys

MM 54 (5992)Potent apelin receptor antagonist

O

O

NC

NN

O

HN

SO

O

AZD 1283 (6085)High affinity P2Y12 antagonist

HN

F

O

NH

OH

O

Cl

Ex 26 (5833)Potent and selective S1P1 receptor antagonist

Featured 7-TM Receptor Products

Adenosine Receptors

Antagonists 6137 8-Cyclopentyl-1,3-dimethylxanthine High affinity adenosine A1 receptor antagonist 100 mg 130

5965 ISAM 140 High affinity A2B receptor antagonist 10 mg

50 mg

175

680

Calcium-Sensing Receptor

Agonists 6170 Cinacalcet Calcium-sensing receptor (CaSR) allosteric agonist; also CYP2D2 inhibitor and Ca2+ channel blocker; orally bioavailable

10 mg

50 mg

100

370

Chemokine Receptors

Antagonists 5872 AZ 10397767 Potent CXCR2 antagonist 10 mg

50 mg

210

835

5943 ML 339 Potent and selective hCXCR6 antagonist 10 mg

50 mg

140

505

Category Cat. No. Product Name Description Unit Size Euro

NEW PRODUCTS – SPRING AND SUMMER 2017

tocris.com | 3

Dopamine Receptors

Agonists 6171 MLS 1547 G protein-biased D2 receptor partial agonist 10 mg

50 mg

140

520

Free Fatty Acid Receptors

Agonists 5789 AM 4668 Potent FFA1 (GPR40) agonist 10 mg

50 mg

195

760

6001 ZQ 16 Selective GPR84 agonist 10 mg

50 mg

140

505

6082 AMG 837 hemicalcium salt Potent FFA1 (GPR40) partial agonist 10 mg

50 mg

195

760

Antagonists 5903 CATPB FFA2 antagonist/inverse agonist 10 mg

50 mg

160

630

GABAB

Ligands 5518 UMB 68 GHB receptor ligand 10 mg

50 mg

70

255

Glutamate (Metabotropic) Receptors

Modulators 5362 TASP 0433864 Selective mGlu2 receptor positive allosteric modulator 10 mg

50 mg

190

740

Other 5785 MDNI-caged-l-glutamate Stable photoreleaser of l-glutamate 10 mg 285

GPBA Receptors

Agonists 6026 Oleanolic acid Selective GPBA receptor (TGR5) partial agonist 50 mg 70

Lysophosphatidic Acid Receptors

Antagonists 5913 Ro 6842262 Potent LPA1 antagonist 10 mg

50 mg

210

820

Opioid Receptors

Modulators 5983 BMS 986187 Potent δ-opioid receptor positive allosteric modulator 10 mg

50 mg

180

705

Peptide Receptors

Agonists 6030 Amylin (rat) Potent endogenous peptide agonist for amylin, calcitonin, CGRP and adrenomedullin receptors

500 µg 240

5488 BML 111 FPR2 (lipoxin A4 receptor) agonist 10 mg 175

6031 Calcitonin (human) Endogenous calcitonin receptor agonist; inhibits bone resorption 500 µg 225

5966 ML 233 Non-peptide apelin receptor agonist 10 mg

50 mg

165

635

6090 Spexin Potent GAL2/3 agonist; exhibits anxiolytic effects in vivo 1 mg 210

Antagonists 6232 Bosentan High affinity dual ETA and ETB receptor antagonist; orally bioavailable

10 mg

50 mg

80

275

5992 MM 54 Potent apelin receptor antagonist 1 mg 245

5954 MSG 606 Potent human MC1 receptor antagonist; also MC3 and MC5 partial agonist

1 mg 245

Prostanoid Receptors

Antagonists 5701 AMG 853 Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonist

10 mg 275

Purinergic (P2Y) Receptors

Antagonists 5720 AR-C 69931 tetrasodium salt Highly potent P2Y12 antagonist 1 mg 230

6085 AZD 1283 High affinity P2Y12 antagonist 10 mg

50 mg

145

545

Sphingosine Receptors

Agonists 6176 FTY 720 Potent S1P receptor agonist; also immunosuppressant 10 mg

50 mg

95

355

Antagonists 5833 Ex 26 Potent and selective S1P1 receptor antagonist 10 mg

50 mg

165

635



4 |

EnzymesEnzymes are proteins that catalyze a chemical change in a substrate. Some enzymes act independently, but others require the assistance of coenzymes or cofactors in order to function correctly. Enzymes can be classified into numerous groups according to their substrate or the type of chemical reaction they catalyze.

Enzymes

N

N

N

O

N

O

N

O N

NCT 501 (5934)Potent and selective ALDH1A1 inhibitor

N

N

O

O

SNH

OO

N

S

N N

PDD 00017273 (5952)Potent and selective poly (ADP ribose)

glycohydrolase (PARG) inhibitor

N

NH

O

HN

O

N

NOHO

AM 2394 (6034)Potent glucokinase activator;

orally bioavailable

N

N

N NO

O

H2NN

O

H2N

eCF 309 (5955)Potent mTOR inhibitor

NNH

O

N

NH

N

HN

S

N

N

PF 3758309 (6005)Potent PAK4 inhibitor; orally available

O

O

O

HN

S

N

NH2O

PF 06281355 (6004)Selective myeloperoxidase (MPO)

inhibitor; orally bioavailable

O

N

SS

S

O2N

O

CCF 642 (6063)Protein disulfide isomerase (PDI) inhibitor

OH

O

N

O

OH

O

BAY 58-2667 (6052)Potent soluble guanylyl cyclase activator

HN

N

N

N

N

N O

ClS

N

FRAX 597 (6029)Potent group I PAK inhibitor

N

O N

O

HN N

N

O

PF 04449613 (5915)Potent PDE9 inhibitor; brain penetrant

Featured Enzyme Products

ATPases/GTPases

Inhibitors 5986 NAV 2729 Selective ARF6 inhibitor 10 mg

50 mg

180

705

Cyclases

Activators 5708 BAY 41-8543 Increases activity of guanylyl cyclase (sGC) stimulator 10 mg

50 mg

210

820

6052 BAY 58-2667 Potent soluble guanylyl cyclase (sGC) activator 10 mg 210

Cytochrome P450

Inhibitors 6108 Galeterone CYP17 inhibitor; also androgen receptor antagonist 10 mg

50 mg

145

560

Substrates 6204 7-Ethoxyresorufin Fluorometric CYP450 substrate 10 mg 165

Dehydrogenases

Inhibitors 5934 NCT 501 Potent and selective ALDH1A1 inhibitor 10 mg

50 mg

260

1030

Hydrolases

Inhibitors 5952 PDD 00017273 Potent and selective poly (ADP ribose) glycohydrolase (PARG) inhibitor; cell permeable

10 mg 270

Isomerases

Inhibitors 5125 CKD 602 Topoisomerase I inhibitor 10 mg

50 mg

70

255

Kinases

Activators 6034 AM 2394 Potent glucokinase activator; orally bioavailable 10 mg

50 mg

195

775

6114 PF 06409577 Potent and selective allosteric activator of AMPK 10 mg

50 mg

165

635



tocris.com | 5

New Compound Libraries

Tocris has launched a range of new compound libraries composed of biologically active molecules that have proven pharmacological activity against a wide range of targets. Use them in your phenotypic screening studies, drug repurposing campaigns or for validation of new molecular targets. Compounds are supplied pre-dissolved in DMSO, and full chemical and biological data are available. All compounds have the same proven solubility, purity and stability as all those in the Tocris catalog.

Tocriscreen Plus (Cat. No. 5840)A unique library of 1280 biologically active compounds, with many exclusive to Tocris (250 mL 10 mM DMSO solutions)

Tocriscreen Library of FDA Approved Compounds (Cat. No. 5932)A library of 160 FDA-approved compounds (250 mL 10 mM DMSO solutions)

Tocris also has available single plate Toolboxes for Kinase Inhibitors, Stem Cells and Epigenetics

For more information visit www.tocris.com/tocriscreen

Inhibitors 5955 eCF 309 Potent mTOR inhibitor 10 mg

50 mg

175

665

6029 FRAX 597 Potent group I PAK inhibitor 10 mg

50 mg

210

820

5632 AZ Dyrk1B 33 Potent and selective Dyrk1B kinase inhibitor 10 mg 260

5742 AZ PFKFB3 67 Potent and selective PFKFB3 inhibitor 10 mg

50 mg

140

505

6071 CZC 25146 Potent LRRK2 inhibitor 10 mg

50 mg

210

820

5834 LTURM 34 Potent DNA-PK inhibitor 10 mg

50 mg

195

760

5756 MLi-2 Potent and selective LRRK2 inhibitor 10 mg

50 mg

255

995

6005 PF 3758309 Potent PAK4 inhibitor; orally available 10 mg

50 mg

115

430

4546 rac-CCT 250863 Potent Nek2 inhibitor 5 mg 290

6015 RAF 265 Raf kinase and VEGFR-2 inhibitor 10 mg

50 mg

215

865

5909 RMM 46 MSK/RSK family kinase inhibitor 10 mg

50 mg

180

720

5968 Ro 3280 Potent and selective PLK1 inhibitor 10 mg

50 mg

225

900

5570 STOCK2S 26016 Lysine deficient protein kinase (WNK) signaling inhibitor 10 mg

50 mg

160

630

Lipases

Inhibitors 5851 JZP 361 Potent and selective reversible MAGL inhibitor 10 mg

50 mg

160

590

6020 URB 602 Non-competitive MAGL inhibitor 10 mg

50 mg

130

470



6 |

Enzymes – continued

Enzymes

N

N

N

O

N

O

N

O N

NCT 501 (5934)Potent and selective ALDH1A1 inhibitor

N

N

O

O

SNH

OO

N

S

N N

PDD 00017273 (5952)Potent and selective poly (ADP ribose)

glycohydrolase (PARG) inhibitor

N

NH

O

HN

O

N

NOHO

AM 2394 (6034)Potent glucokinase activator;

orally bioavailable

N

N

N NO

O

H2NN

O

H2N

eCF 309 (5955)Potent mTOR inhibitor

NNH

O

N

NH

N

HN

S

N

N

PF 3758309 (6005)Potent PAK4 inhibitor; orally available

O

O

O

HN

S

N

NH2O

PF 06281355 (6004)Selective myeloperoxidase (MPO)

inhibitor; orally bioavailable

O

N

SS

S

O2N

O

CCF 642 (6063)Protein disulfide isomerase (PDI) inhibitor

OH

O

N

O

OH

O

BAY 58-2667 (6052)Potent soluble guanylyl cyclase activator

HN

N

N

N

N

N O

ClS

N

FRAX 597 (6029)Potent group I PAK inhibitor

N

O N

O

HN N

N

O

PF 04449613 (5915)Potent PDE9 inhibitor; brain penetrant

Featured Enzyme Products (continued)

Lyases

Inhibitors 6101 SHIP 2a Cystathione γ lyase (CSE) inhibitor 10 mg

50 mg

140

520

Oxygenases

Inhibitors 6004 PF 06281355 Selective myeloperoxidase (MPO) inhibitor 10 mg

50 mg

160

630

Phosphatases

Inhibitors 5724 NQ 301 Selective CD45 inhibitor 10 mg

50 mg

130

485

Phosphodiesterases

Inhibitors 5695 Eggmanone Potent and selective PDE4 inhibitor; suppresses hedgehog signaling

10 mg

50 mg

160

630

5915 PF 04449613 Potent PDE9 inhibitor; brain penetrant 10 mg 225

Polymerases

Inhibitors 5312 BRACO 19 Telomerase inhibitor 10 mg

50 mg

180

720

Proteases

Inhibitors 6033 (R)-MG 132 Potent 20S proteasome inhibitor 10 mg 270

6019 Diprotin A Dipeptidyl peptidase IV (DPP-IV) inhibitor 10 mg 195

6088 SB 3CT Selective high affinity MMP2 inhibitor 10 mg 275

Reductases

Inhibitors 6063 CCF 642 Protein disulfide isomerase (PDI) inhibitor 10 mg

50 mg

140

505

Synthases/Synthetases

Inhibitors 5791 Bz 423 ATP synthase inhibitor; proapoptotic 10 mg

50 mg

155

590

6111 Zoledronic Acid Potent farnesyl diphosphate (FPP) synthase inhibitor 10 mg

50 mg

80

290

Transferases

Inhibitors 5762 BMS 795311 Potent cholesteryl ester transfer protein (CETP) inhibitor 10 mg 335



tocris.com | 7

O

O

N

N

N

N

NH2

CP 673451 (5993)Potent and selective PDGFR inhibitor

Enzyme-Linked Receptors

N

N NH2N

O

OH

N

HNO

N Cl

PF 06273340 (6115)Potent and selective pan-Trk inhibitor;

peripherally restricted

Featured Enzyme-Linked Receptor Products

Enzyme-Linked ReceptorsEnzyme-linked receptors are a group of multi-subunit transmembrane proteins that contain either intrinsic enzyme activity on their intracellular domain, or associate directly with an intracellular enzyme. Upon ligand binding, a conformational change is transmitted via a transmembrane helix. This activates the enzyme, initiating signaling cascades.

Licensing at TocrisTocris Bioscience has a long tradition of working with scientists to bring new discoveries out of the laboratory and into the commercial arena. We work in partnership with many scientists within both universities and pharmaceutical companies to bring life science tools to the global research community.

Tocris' policy has always been to never knowingly infringe third party intellectual property. It is our intention to remain a responsible and ethical supplier, and work with the scientific community.

Our ExpertiseOur licensing department has significant experience of drafting contracts and has successfully executed licenses with a multitude of licensors, including:

• Large pharmaceutical companies• Start-up/spin-out companies • University technology transfer offices• Individual researchers

Contact UsTo discuss licensing opportunities, please contact our licensing team at [email protected]

Integrins

Inhibitors 6058 ATN 161 α5β1 integrin receptor antagonist 10 mg 210

MET Receptors

Inhibitors 6056 GSK 1363089 Potent inhibitor of MET, VEGFR2, Ron and AXL 10 mg

50 mg

175

665

Receptor Tyrosine Kinases (RTKs)

Inhibitors 5993 CP 673451 Potent and selective PDGFR inhibitor 10 mg 225

6115 PF 06273340 Potent and selective pan-Trk inhibitor; peripherally restricted 10 mg 175

Toll-like Receptors

Agonists 6011 FSL 1 TLR2/6 agonist (also a putative TLR10 ligand) 100 µg 165



8 |

Ion Channels Ion channels are pore-forming membrane proteins that allow the passage of ions across the plasma membrane. Hundreds of different ion channels have been identified in the membranes of all mammalian cells; they can be broadly classified by different properties including the gating mechanism (e.g. voltage or ligand) or ion selectivity of their pore.

Ion Channels

NO2

O

O

O

O

O

O

OO

P

P

O

OO

OO

OO

PO

O

O

OO

O

O O

OO

OO

O

O

ci-IP3/PM (6210)Caged inositol triphosphate

O

NH

NO2

HO O

MONNA (5770)Potent TMEM16A (Anoctamin-1) blocker

Cl

NH2

O

(R)-Norketamine (5996)NMDA receptor modulator

Cl

NH2

O

(S)-Norketamine (6112)NMDA receptor modulator

Cl

NH2O

HO

2R,6R-Hydroxynorketamine (6094)Enhances AMPA currents; decreases D-serine

(a NMDA co-agonist); lacks ketamine-related side effects

Cl

NH2O

.HCl

HO

2S,6S-Hydroxynorketamine (6095)Decreases D-serine (a NMDA co-agonist);

antidepressant

N

OHO

O

N

F

PF 05105679 (6003)Selective TRPM8 blocker; orally bioavailable

Featured Ion Channels Products

Calcium Channels

Other 6210 ci-IP3/PM Caged inositol triphosphate 10 µg 200

Chloride Channels

Blockers 6076 Ani 9 Potent and selective TMEM16A (Anoctamin-1; ANO1) blocker 10 mg

50 mg

175

665

5770 MONNA Potent TMEM16A (Anoctamin-1) blocker 10 mg

50 mg

145

560

Glutamate (Ionotropic) Receptors

Other 5996 (R)-Norketamine NMDA receptor modulator; analgesic 10 mg 255

6112 (S)-Norketamine NMDA receptor modulator; analgesic 10 mg 255

6094 2R,6R-Hydroxynorketamine Enhances AMPA currents; decreases d-serine (a NMDA co-agonist); lacks ketamine-related side effects

10 mg 270

6095 2S,6S-Hydroxynorketamine Decreases d-serine (a NMDA co-agonist); antidepressant 10 mg 270

Potassium Channels

Activators 6233 Retigabine KV7 channel activator 10 mg

50 mg

95

325

Blockers 6086 AMP PNP Kir6 (KATP) channel blocker; non-hydrolyzable AMP analog 10 mg 145

Sodium Channels

Blockers 6159 4,9-Anhydrotetrodotoxin Potent and selective NaV1.6 channel blocker 100 µg 200

Transient Receptor Potential Channels

Antagonists 5995 AMG 517 Potent TRPV1 antagonist 10 mg

50 mg

175

680

Blockers 6003 PF 05105679 Selective TRPM8 blocker 10 mg 155



tocris.com | 9

Nuclear Receptors Nuclear receptors (also known as nuclear hormone receptors) are a large family of transcription factors that bind directly to DNA to regulate the expression of target genes. They regulate the cellular response to hormones such as sex steroids, vitamin D3, adrenal steroids and other metabolic ligands, and are involved in metabolism, development and reproduction.

TransportersTransporters are specialized membrane-spanning proteins that aid the movement of ions, peptides, small molecules, lipids and macromolecules across a lipid bilayer. There are three main classes of transporter: ABC transporters, P-type ATPases and the solute carrier family. Transporters can move substances either actively or passively.

Mitochondrial Na+/Ca2+ exchange inhibitor

ITH 12575 Cat. No. 5692

ITH 12575 is a mitochondrial Na+/Ca2+ exchange (mNCX) inhibitor. The compound reduces Ca2+ efflux from the mitochondria to the cytosol in HeLa cells (EC50 = 0.69 μM). ITH 12575 also protects against glutamate-induced excitotoxicity in rat hippocampal slices and oligomycin A/rotenone-induced oxidative stress in neuroblastoma cells in vitro.

Transporters

ITH 12575 (5692)

NH

S

O

Cl

ITH 12575 is a mitochondrial Na+/Ca2+ exchange (mNCX) inhibitor. The compound reduces Ca2+afflux from the mitochondria to the cytosol in HeLa cells (EC50 = 0.69 µM). 12575 also protectsagainst glutamate-induced excitotoxitiy in rat hippocampal slices and oligomycin A/rotenone-inducedoxidative stress in neuroblastoma cells in vitro.

LXR-Like Receptors

Agonists 6138 SR 9234 LXR inverse agonist 10 mg

50 mg

160

600

Retinoic Acid Receptors

Antagonists 5758 AGN 193109 Potent retinoic acid receptor (RAR) antagonist 10 mg 270

Na+/Ca2+ Exchanger

Inhibitors 5692 ITH 12575 Mitochondrial Na+/Ca2+ exchange (mNCX) inhibitor. 10 mg

50 mg

195

760

Neurotransmitter Transporters

Inhibitors 6131 (R)-Modafinil Dopamine uptake inhibitor 10 mg

50 mg

100

370

4447 Org 24598 Inhibitor of GlyT1; derivative of Org 24598 lithium salt (Cat. No. 4035).

10 mg

50 mg

190

740



New Products for Cell Biology

10 |

Potent ULK inhibitor

MRT 68921 Cat. No. 5780

MRT 68921 is a potent ULK inhibitor (IC50 values are 1.1 and 2.9 nM for ULK2 and ULK1, respectively). The compound inhibits autophagy in mouse embryonic fibroblasts

Cell Metabolism

N

HN

N

HN

HN

O

N

MRT 68921 (5780)Potent ULK inhibitor

MRT 68921 is a potent ULK inhibitor (IC50 values are 1.1 and 2.9 nM for ULK2 and ULK1, respectively).The compound inhibits autophagy in mouse embryonic fibroblasts

ApoptosisApoptosis is a form of programmed cell death that involves caspase-dependent intracellular signaling, resulting in phagocytosis of unwanted cells. The cell cycle is a regulatory network that controls cell proliferation and detects DNA damage. In the event that DNA damage cannot be repaired, the cell is destroyed through apoptotic mechanisms.

Cell Metabolism Cellular metabolism describes a set of chemical reactions that occur in living organisms in order to maintain life. Cellular metabolism involves complex sequences of controlled biochemical reactions, better known as metabolic pathways. These processes allow organisms to grow and reproduce, maintain their structures, and respond to environmental changes.

Apoptosis Inducers

Other 5804 Chaetoglobosin A Selectively induces apoptosis of CLL cells; antibiotic 1 mg 195

Autophagy

Inhibitors 5780 MRT 68921 Potent ULK inhibitor; inhibits autophagy 10 mg

50 mg

180

720

DNA, RNA and Protein Synthesis

Inhibitors 5962 3-AP Ribonucleotide reductase inhibitor; also an iron chelator 10 mg

50 mg

115

430

6070 Pladienolide B mRNA splicing inhibitor; antitumor 500 µg 325

5419 PCNA I1 Proliferating cell nuclear antigen (PCNA) inhibitor 10 mg

50 mg

145

560

Lipid Metabolism

Inhibitors 5850 HM 50316 High affinity FABP4 inhibitor 10 mg

50 mg

195

775

Neuronal Metabolism

Other 6250 Filipin III Polyene antibiotic; inhibits formation of pathological isoform of prion protein

1 mg 180




tocris.com | 11

EpigeneticsEpigenetics is the study of acquired changes or modifications in chromatin structure that arise independently of a change in the underlying DNA nucleotide sequence. Epigenetic modifications alter the accessibility of DNA to transcription machinery, thereby influencing gene expression.

PROTACs – New from Tocris

MZ 1 (#6154) is a PROTAC (PROteolysis TArgeting Chimera), a new tool for epigenetics research from Tocris. PROTACs are bifunctional small molecules, comprising binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker, that harness the ubiquitin/proteasome system (UPS) to selectively remove target proteins from cells.

Key features of MZ 1• Selectively induces degradation of BRD4 by the

proteasome• Catalytic mode of action• Negative control, cis MZ 1 (#6155), also available• Licensed from Alessio Ciulli at the University of

Dundee (UK)

UbPROTAC

Target Protein

NH2 NH2

NH2

Ub

E3 ligaseE3 ligase

E2 E2

Ternarycomplex

PolyubiquitinationProteasomePeptide fragments

UbUb Ub

Ub

Catalytic – PROTAC is recycled

How PROTACs Work: Schematic showing PROTACs catalytic mode of action. PROTACs allow the formation of a ternary complex between E3 ubiquitin ligase and a target protein which results in polyubiquitination of the target protein, its recognition by the proteasome and subsequent degradation. PROTACs act catalytically by repeatedly engaging and directing the ubiquitination of target molecules. (Adapted from Timworth et al. (2016) Med.Chem.Comm. 7 2206)

Bromodomains

Inhibitors 5970 BAY 299 Potent and selective BRD1 and TAF1 inhibitor 10 mg

50 mg

145

545

6000 TP 472 Potent BRD9/7 inhibitor 10 mg 190

Other 5999 TP 472N Negative control for TP 472 (Cat. No. 6000) 10 mg 190

Histone Deacetylases

Inhibitors 6010 BRD 4354 HDAC5 and HDAC9 inhibitor 10 mg

50 mg

165

635

6124 (R)-2-Hydroxyglutaric acid disodium salt

KDM4A inhibitor; oncometabolite produced by mutant IDH1 and 2; also NF-κB activator

50 mg 110

Lysine Methyltransferase

Inhibitors 6169 PF 06726304 Highly potent and SAM-competitive EZH2 inhibitor 10 mg 165

PROTACs

Other 6154 MZ 1 (+)-JQ1 based PROTAC that selectively degrades BRD4 in cells 5 mg 325

6155 cis MZ 1 Negative control for MZ 1 (Cat. No. 6154) 5 mg 325

Protein Arginine Methyltransferases

Inhibitors 6008 TP 064 Potent and selective PRMT4 inhibitor 10 mg

50 mg

140

530

5777 GSK 591 Potent and selective PRMT5 inhibitor 10 mg 275



12 |

Fluorescent ImagingFluorescent probes and dyes facilitate the visualization of subcellular components in live and fixed cells with high sensitivity and selectivity and enable monitoring of dynamic intracellular biochemical reactions. Fluorescent dyes may also be conjugated to antibodies for immunohistochemistry and flow cytometry use.

Fluorescent Imaging

O N+N

CO2-

O

O

N

O

O

Janelia FluorTM 549, SE (6147)Fluorescent dye; supplied as an NHS ester for couplingto primary amine groups; compatible with self-labeling

tag systems

Si N+N

CO2-

O

O

N

O

O

Janelia FluorTM 646, SE (6148)Fluorescent dye; supplied as an NHS ester for couplingto primary amine groups; compatible with self-labeling

tag systems

OH2N O

NH2

FFN 200 (5911)Selective fluorescent VMAT2 substrate

Cl NHO

HN

O

N+N

Et

SO3H-O3S

NH

O

NHO

Cl

Cl

IHR-Cy3 (5561)Potent fluorescent Smo antagonist

Featured Fluorescent Imaging Products

Fluorescent Imaging

Other 6065 2-NBDG Fluorescent glucose uptake indicator 5 mg 245

5436 Cyanine 5, SE Red fluorescent dye for the labeling of amines 10 mg 175

5824 Hoechst 33258 Fluorescent dye for labeling DNA 50 mg 65

6147 Janelia Fluor™ 549, SE Cell permeable fluorescent dye; supplied as NHS ester 5 mg 320

6148 Janelia Fluor™ 646, SE Cell permeable fluorescent dye; supplied as NHS ester 5 mg 320

5911 FFN 200 Fluorescent VMAT2 substrate 10 mg 240

5561 IHR-Cy3 Potent fluorescent Smo antagonist 1 mg 180

6046 Naloxone fluorescein acetate Fluorescent opioid antagonist; fluorescent-derivative of naloxone (Cat. No. 0599)

100 µg 175



tocris.com | 13

Signal TransductionSignal transduction, or intracellular signaling, is the transmission of molecular signals from a cell’s exterior to its interior. This process is initiated by cell surface receptors, and is required to ensure an appropriate cellular response. Signal transmission is propagated by either biochemical changes within the cell, or by membrane potential alterations.

Signal Transduction

N

N

MeO

MeO

S CN

O SO

O

GSK 319347A (5672)Potent and selective IKKε inhibitor

O

NH2N

NN

NH

Cl

F

Cl

(S)-Crizotinib (6025)Potent MTH1 inhibitor

N

N N

NO

S

HN

EtOO

O

NO

N

N

AX 15836 (5843)Potent and selective ERK5 inhibitor

O

N

NH2

N

HN

O

O

HCl

AMBMP (6043)Wnt canonical signaling activator;

also inhibits tubulin polymerization.

Featured Signal Transduction Products

Cytokine and NF-κB Signaling

Inhibitors 5846 IT 901 NF-κB c-Rel subunit inhibitor 10 mg

50 mg

190

740

4238 PF 184 Potent and selective IKKβ inhibitor 10 mg 270

5300 BI 605906 Selective IKKβ inhibitor 10 mg 270

6107 CP 424174 Inhibitor of IL-1β post-translational processing; indirectly inhibits NLRP3

10 mg

50 mg

140

505

5672 GSK 319347A Potent and selective IKKε inhibitor 10 mg 370

G Proteins (small)

Inhibitors 6025 (S)-Crizotinib MTH1 inhibitor 10 mg

50 mg

155

590

Hedgehog Signaling

Activators 5282 SAG 21k Hedgehog signaling activator; brain penetrant and orally bioavailable

10 mg 255

MAPK Signaling

Inhibitors 5843 AX 15836 Potent and selective ERK5 inhibitor 10 mg 285

6014 Org 48762-0 Selective p38α/β inhibitor; orally bioavailable 10 mg

50 mg

180

705

NO Donors/Precursors

Other 6077 DETA NONOate Nitric oxide donor 10 mg 50

PI 3-K/Akt Signaling

Inhibitors 5835 LTURM 36 PI 3-kinase δ inhibitor 10 mg

50 mg

195

760

6087 Perifosine PKB/Akt inhibitor; also modulates KV2.1 current 10 mg

50 mg

100

370

5919 PI 3065 Potent and selective PI 3-kinase p110δ inhibitor 10 mg

50 mg

215

865



14 |

ReagentsOur wide and expanding range of research reagents includes biochemicals, buffers, solvents, labels and stains, as well as stable isotopically labeled compounds.

Chemical dimerizer; cell permeable

HaXS8 Cat. No. 4991

NN

N

HN

NH2

O

NH

O O O

F F

F FO

OO

O

Cl

Reagents

HaXS8 (4991)Chemical dimerizer; cell permeable

HaXS8 is a cell permeable chemical dimerizer that promotes covalent and irreversible HaloTag™and SNAP-tag™ substrate dimerization (HaloTag is a trademark of Promega Corporation, andSNAP-tag is a trademark of New England BioLabs, Inc.)

HaXS8 is a cell permeable chemical dimerizer that promotes covalent and irreversible HaloTag™ and SNAP-tag™ substrate dimerization (HaloTag is a trademark of Promega Corporation, and SNAP-tag is a trademark of New England BioLabs, Inc.)

Signal transduction – continued

Transcription Factors

Other 5761 RG 102240 Gene switch ligand for use in inducible gene expression systems 10 mg

50 mg

145

560

Translocation, Exocytosis & Endocytosis

Other 5978 WL 47 - dimer High affinity caveolin-1 ligand 1 mg 145

Wnt Signaling

Activators 6043 AMBMP Wnt canonical signaling activator; also tubulin polymerization inhibitor

10 mg

50 mg

145

560

Inhibitors 5813 NSC 668036 Wnt signaling inhibitor; binds the PDZ domain of the Dishevelled (Dvl) protein

10 mg

50 mg

155

590

Reagents

Other 6117 CORM 2 Carbon monoxide-releasing molecule 100 mg 55

5407 GA3-AM Chemical dimerizer; cell permeable 10 mg

50 mg

80

275

4991 HaXS8 Chemical dimerizer 2 mg 270

6146 LAP Photocrosslinker for hydrogels 500 mg 130

Signal transduction – continued




tocris.com | 15

Scientific ReviewsProduct Guides & Listings Life Science Posters

• GPCRs• Kinases • Cancer Research• Neurodegeneration

• Vascular Reactivity• Gut Hormones • Cancer Metabolism• Addiction

• Ras Oncoproteins• Nicotinic ACh Receptors• Dopamine Receptors• Stem Cells

Life Science Literature from TocrisTocris also provides a wide range of scientific literature free of charge, including the following titles:

To download or request copies, please visit www.tocris.com/requestliterature

Stem Cells

N

HN

N N

N

N

LDN 193189 (6053)Promotes neural induction

of hPSCs; potent and selective ALK2 and ALK3 inhibitor

N

O

NN

NN

Lin28 1632 (6068)Induces differentiation of murine ESCs and

inhibits stemness; RNA binding protein Lin28inhibitor; also bromodomain inhibitor

Featured Stem Cells Products

Stem CellsStem cells are pluripotent or multipotent cells that are capable of self-renewal through mitotic cell division, and which may be induced to form more specialized cells of a tissue or organ by a process termed cellular differentiation. Key morphogens, such as Wnt, Hedgehog and Notch, influence stem cell self-renewal and differentiation.

Reprogramming

Other 6044 AS 8351 Induces reprogramming of fibroblasts into functional cardiomyocytes

10 mg

50 mg

100

370

6066 OAC-2 Oct4 activator; enhances iPSC reprogramming efficiency 10 mg

50 mg

110

390

Stem Cell Differentiation

Other 6053 LDN 193189 Potent and selective ALK2 and ALK3 inhibitor; promotes neural induction of hPSCs

10 mg

50 mg

195

760

6068 Lin28 1632 RNA binding protein Lin28 inhibitor; promotes mESC differentiation; also bromodomain inhibitor

10 mg

50 mg

160

600

Stem Cell Proliferation

Other 5779 NSC 23005 sodium Potently promotes HSC expansion; p18INK inhibitor 10 mg

50 mg

145

560


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