Featured Products 2017

Highlighted products added to the Tocris Bioscience range during 2017

April 2017

High affinity pan-RAR antagonist
5758 | AGN 193109

Kd values are 2, 2 and 3 nM at RARα, RARβ and RARγ, respectively. Does not bind retinoic X receptors.

Related Products: Retinoic acid BMS 493 ER 50891
Potent DDHD2 inhibitor
5865 | KLH 45

IC50 = 1.3 nM. Selective for DDHD2 over 40 other serine hydrolases, but does exhibit cross-reactivity with ABHD6. In vivo active. Increases brain triacylglycerol levels in mice.

Related Products: A 922500 WWL 123 JNJ DGAT2-A
Inhibitor of IL-1β post-translational processing
6107 | CP 424174

IC50 = 210 nM. Inhibits the formation of mature IL-1β. Indirectly inhibits NLRP3. Active in vivo and orally bioavailable.

Related Products: Z-VAD-FMK AS 2444697 CRID3 sodium salt
Photoactivatable cell permeable fluorescent dye
6149 | PA Janelia Fluor™ 549, SE

Supplied as NHS ester. Non-fluorescent until activated at 365 nm. Photochemical quantum yield of uncaging = 2.2%, with improved yield upon protein conjugation. Compatible with self-labeling tag systems. Suitable for single molecule tracking and super resolution microscopy in live cells. Can be multiplexed with PA Janelia Fluor™ 646, SE (Cat. No. 6150) to perform two-colour sptPALM in live cells. Cell permeable. Excitation maximum = 551 - 553 nm; emission maximum = 570 - 573 nm.

Related Products: Hoechst 33342 Sulforhodamine 101 Janelia Fluor™ 549, SE
Potent and selective VCP allosteric inhibitor
6180 | NMS 873

IC50 = 30 nM. Selective over all other AAA ATPases, HSP90 and kinases tested (IC50 >10 nM). Activates the unfolded protein response (UPR), and modulates autophagosome maturation. Exhibits antiproliferative activity in cancer cells in vitro. Reduces VCP-sensitaisation to trypsin digestion.

Related Products: Xanthohumol GSK 2606414 Azoramide

March 2017

Stable photoreleaser of L-glutamate
5785 | MDNI-caged-L-glutamate

Rapidly and efficiently releases glutamate (Cat. No. 0218) when photolysed (350 - 365 nm excitation). Water soluble and stable at neutral pH, and pharmacologically inactive at neuronal glutamate receptors (up to 200 μM). 5.5 times more photosensitive than MNI-caged L-glutamate (Cat. No. 1490). Laser activation of MDNI-glu evokes a rapid increase in intracellular Ca2+ concentration in astrocytes.

Related Products: L-Glutamic acid MNI-caged-L-glutamate RuBi-Glutamate
Potent and selective PRMT5 inhibitor
5777 | GSK 591

IC50 = 4 nM. Selective for PRMT5 over a panel of other PRMTs and lysine methyltransferases. Inhibits proliferation of mantle cell lymphoma (MCL) in vitro.

Related Products: UNC 2327 Furamidine MS 023
Potent CXCR2 antagonist
5872 | AZ 10397767

IC50 = 1 nM. Attenuates oxaliplatin-induced NF-κB activation, increases oxaliplatin cytotoxicity, and potentiates oxaliplatin-induced apoptosis in AIPC cells. Reduces the numbers of infiltrating neutrophils into both in vitro and in vivo tumor models. Orally bioavailable.

Related Products: SB 265610 SB 225002 NVP CXCR2 20
Selective fluorescent VMAT2 substrate
5911 | FFN 200

Selectively traces exocytosis in dopaminergic neuronal cell culture and brain tissue. Excitation and emission maxima are 352 and 451 nm, respectively.

Related Products: Tetrabenazine Reserpine FFN 206
Highly potent and SAM-competitive EZH2 inhibitor
6169 | PF 06726304

IC50 = 0.7 nM. Inhibits proliferation of Karpas-422 cells (non-Hodgkin's lymphoma) in vitro, halts tumor growth and reduces intratumoral H3K27Me3 levels in mice.

Related Products: 3-Deazaneplanocin A UNC 1999 UNC 0642

February 2017

Potent and selective S1P1 receptor antagonist
5833 | Ex 26

IC50 = 0.93 nM. Exhibits >3,000-fold selectivity for S1P1 over S1P2, S1P3, S1P4 and S1P5. Induces lymphocyte sequestration in peripheral lymph nodes and upregulates S1P1 receptor expression. Reduces disease severity in mice with EAE. Increases IFN-α production in stimulated dendritic cells in vivo.

Related Products: Sphingosine-1-phosphate VPC 23019 TY 52156
Potent mTOR inhibitor
5955 | eCF 309

IC50 = 15 nM. Exhibits >60-fold selectivity for mTOR over PI 3-kinases and is inactive against a panel of other kinases. Inhibits growth of ER-positive MCF7 breast cancer cells in vitro (EC50 = 8.5 nM). Cell permeable.

Related Products: Rapamycin Torin 1 AZD 3147
Potent PAK4 inhibitor; orally available
6005 | PF 3758309

IC50 = 1.3 nM; Kd = 2.7 nM. Inhibits proliferation and anchorage-independent growth of a panel of tumor cell lines in vitro. Suppresses growth of human HCT116 and A549 tumor cell xenografts in mice.

Related Products: IPA 3 PIR 3.5 FRAX 486
Potent glucokinase activator; orally bioavailable
6034 | AM 2394

EC50 = 60 nM. Reduces plasma glucose levels in an oral glucose tolerance test in ob/ob mice.

Related Products: GKA 50 LDN 193188 TC-G 1005
Ketamine metabolite; lacks ketamine side effects
6094 | 2R,6R-Hydroxynorketamine

Enhances AMPA receptor-mediated excitatory post-synaptic potentials in the CA1 region of hippocampal slices. Decreases intracellular D-serine (a NMDA co-agonist) concentrations in PC-12 cells (IC50 = 0.68 nM). Exerts antidepressant effects in mice.

Related Products: (R)-Norketamine 2S,6S-Hydroxynorketamine (S)-Norketamine

January 2017

Potent BRD9/7 inhibitor
6000 | TP 472

Kd values are 33 and 340 nM, respectively. Exhibits >30-fold selectivity for BRD9 over other bromodomains except BRD7. Cell permeable and active in vivo

Related Products: (+)-JQ1 I-BET 151 I-BRD9
Raf kinase and VEGFR-2 inhibitor
6015 | RAF 265

Inhibits c-Raf, wild type B-Raf and mutant B-Raf (V600E). Cytotoxic in certain melanoma cells lines. Effects enhanced by protein kinase D3 inhibition, preventing reactivation of MAPK signaling and increasing caspase activity. Orally bioavailable.

Related Products: SU 5416 SU 5402 GDC 0879
Endogenous amylin, calcitonin, CGRP and adrenomedullin agonist
6030 | Amylin (rat)

pEC50 values are 7.06-9.50 at hCTa, 8.11 at rCTa, 7.73-10.1 at hAMY1a, 9.74 at rAMY1a, 7.92 at hAMY1b, 7.78-9.9 at hAMY2a, 7.94 at hAMY2b, 8.09-10.8 at hAMY3a, 9.97 at rAMY and 8.19 at hAMY3b receptors. Suppresses insulin-stimulated glucose uptake. Delays gastric emptying and promotes satiety. Active in vivo.

Related Products: CGRP (rat) AC 187 Pramlintide
Potent soluble guanylyl cyclase (sGC) activator
6052 | BAY 58-2667

EC50 = 6.4 nM. Binds heme-free sGC. Exhibits antihypertensive effects in vivo.

Related Products: YC 1 BAY 41-2272 BAY 41-8543
Oct4 activator; enhances iPSC reprogramming efficiency
6066 | OAC-2

Enhances iPSC reprogramming four-fold and accelerates the appearance of iPSC colonies in combination with 4F (Oct4, Sox2, c-Myc and Klf4). Also induces cardiomyocyte-like cells from human fibroblasts, as part of the 9C cocktail (CHIR 99021, A83-01, BIX 01294, AS83541, SC1, Y-27632, SU 16f, JNJ10198409 and OAC-2)

Related Products: Y-27632 CHIR 99021 O4I1

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New Product Guide

New Product Guide (Fall/Winter 2016)

Our New Product guide highlights over 100 new products added in the second half of 2016. Request copy or view PDF today.

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