Featured Products 2017

Highlighted products added to the Tocris Bioscience range during 2017

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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