Featured Products 2010

Highlighted products added to the Tocris Bioscience range during 2010

December 2010

mGlu2 antagonist
2913 | Ro 64-5229

IC50 = 0.11 μM. Selective and non-competitive. Inhibits GTPγ35S binding to mGlu2-containing membranes.

Related Products: DCG IV LY 341495 (RS)-APICA
Bcl-2 inhibitor
4038 | TW 37

Ki values are 0.29 μM and 1.11 μM for Bcl-2 and Bcl-XL respectively. Inhibits the angiogenic potential of endothelial cells in vitro. Induces S-phase arrest and apoptosis in pancreatic cancer cell lines; also inhibits the activation of Notch-1 and Jagged-1 in vitro and in vivo.

Related Products: HA14-1 Gambogic acid Bax channel blocker
Selective NOP receptor antagonist
3573 | SB 612111

Ki values are 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors respectively. Antagonizes the pronociceptive action of nociceptin (Cat. No. 0910) in an acute pain model. Potentiates the action of morphine in morphine-tolerant animals and blocks hyperalgesia in an inflammatory pain model.

Related Products: (±)-J 113397 UFP-101 PF 998425
Modulator of voltage-sensitive Ca2+ channels
3775 | Pregabalin

Anticonvulsant and antiepileptic; also used to treat neuropathic pain. Binds with high affinity and selectivity to the α2δ subunit of voltage-sensitive Ca2+ channels and modulates their activity. Displays anxiolytic-like activity in ethological and conflict models of anxiety. Analog of GABA (Cat. No. 0344).

Related Products: Gabapentin L-Ascorbic acid ω-Conotoxin GVIA
VLA-4 antagonist
3900 | TCS 2314

Integrin very late antigen-4 (VLA-4; α4β1) antagonist (IC50 = 4.4 nM). Blocks the activation of inflammatory cells.

Related Products: GR 144053 BIO 1211 MNS

November 2010

TRPM8 blocker
3989 | AMTB

TRPM8 channel blocker. Inhibits icilin-induced (Cat. No. 1531) TRPM8 channel activation in a rat model (pIC50 = 6.23).

Related Products: Icilin WS 12 WS 3
H3 receptor inverse agonist/antagonist
3743 | BF 2649

Histamine H3 receptor inverse agonist (EC50 = 1.5 nM) and antagonist (Ki = 0.16 nM). Exhibits nootropic effects in cognitive disorders; reduces locomotor hyperactivity induced by methamphetamine. Brain penetrant.

Related Products: (R)-(-)-α-Methylhistamine dihydrobromide Imetit dihydrobromide Proxyfan
High affinity CB1 antagonist
3921 | NIDA 41020

High affinity CB1 receptor antagonist (Ki = 4.1 nM). Exhibits significantly reduced lipophilicity compared to other CB1 antagonists.

Related Products: AM 251 AM 281 PF 514273
Inhibitor of P-gp-mediated MDR
4042 | PSC 833

P-glycoprotein (P-gp) modulator; inhibits P-gp-mediated multidrug-resistance (MDR). Reverses resistance to several cytotoxic drugs including mitoxantrone and doxorubicin (resistance factors are 2.0 and 6.5 respectively) in human MDR cancer cell lines. Non-immunosuppressive analogue of cyclosporin A (Cat. No. 1101).

Related Products: Ko 143 Pyrimethamine Reversan

October 2010

Positive allosteric modulator of hCaSR
3815 | R 568

Allosteric agonist of the human calcium-sensing receptor (hCaSR). Exhibits calcimimetic activity. Has the ability to restore function to hCaSR mutants that cause familial hypocalciuric hypercalcemia (FHH) and neonatal severe hyperparathyroidism (NSHPT). Exerts a suppressive effect on parathyroid (PT) hormone secretion; inhibits PT cell proliferation in rats with renal insufficiency.

Related Products: Parathyroid hormone (1-34) (human) BAPTA NAADP
Potent GSK-3β inhibitor
3869 | TCS 2002

IC50 = 35 nM. Oral adminstration inhibits cold water stress-induced tau hyperphosphorylation in the mouse brain.

Related Products: TWS 119 BIO-acetoxime BIO
Potent, selective and reversible CerK inhibitor
3960 | NVP 231

IC50 = 12 nM in vitro. Displays selectivity for ceramide kinase (CerK) over sphingosine kinases (IC50 ≥100 μM) and other lipid kinases.

Related Products: Ceramide Miglustat Fumonisin B1
Selective H4 receptor antagonist
4021 | JNJ 7777120

Displays high affinity (Ki = 4.5 nM) and is >1000-fold selective for H4 over other histamine receptors.

Related Products: 4-Methylhistamine Imetit Clobenpropit
S6K1 inhibitor
4032 | PF 4708671

Cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) (Ki = 20 nM; IC50 = 160 nM). Suppresses the S6K1-mediated phosphorylation of S6, Rictor and mTOR in response to IGF1; displays no effect on the activity of RSK and MSK in vivo. Exhibits no significant inhibition of S6K2 or other AGC kinases (e.g. Akt, PKA and ROCK) in vitro.

Related Products: SL 0101-1 10-DEBC Rapamycin

September 2010

Dynamin inhibitor
3982 | Mdivi 1

IC50 = 1 - 10 μM. Attenuates Dnm1- and Drp1-mediated mitochondrial division. Inhibits mitochondrial outer membrane permeabilization (MOMP) and attenuates apoptosis.

Related Products: CP 96345 Dynamin inhibitory peptide NSC 23766
Hsp70 inhibitor
3803 | VER 155008

IC50 = 0.5 μM. Inhibits cell proliferation of multiple human tumor cell lines in vitro. Also binds Hsc70 and Grp78; selective against Hsp90β.

Related Products: Pifithrin-μ Macbecin I 17-AAG
Positive allosteric modulator of mGlu2
3949 | CBiPES

IC50 = 98.2 nM. Mimics the action of LY 379268 (Cat. No. 2453); attenuates ketamine-evoked histamine release in vivo.

Related Products: LY 379268 LY 354740 LY 341495
Potent γ-secretase inhibitor
2870 | BMS 299897

IC50 = 12 nM. Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Exhibits no Notch toxicity. Brain penetrant.

Related Products: Compound W DAPT JLK 6
α5-selective GABAA inverse agonist
3817 | MRK 016

EC50 = 3 nM. Exhibits affinity at benzodiazepine binding site of recombinant human GABAA receptors (Ki values are 0.77 nM, 0.83 nM, 0.85 nM and 1.4 nM for α3-, α1-, α2-, and α5-containing respectively). Increases long-term potentiation (LTP) in mouse hippocampal slices. Exhibits no anxiogenic or proconvulsant activity.

Related Products: TB 21007 (+)-Bicuculline TCS 1205

August 2010

Selective inhibitor of TGF-βRI
3742 | SJN 2511

IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively. Selective for ALK5 over a range of kinases, including p38 MAPK, JNK1 and GSK3 (IC50 > 16 μM). Enhances the efficiency of cellular reprogramming.

Related Products: SB 431542 A 83-01 SB 525334
Subtype-selective GABAA receptor agonist
3941 | TCS 1205

In vitro Ki values are 14 and 121 nM for GABAA α2 and GABAA α1 respectively. Exhibits non-sedative anxiolytic activity in vivo.

Related Products: SR 95531 (+)-Bicuculline Muscimol
D3 antagonist and D2 partial agonist
3940 | GSK 789472

pEC50 values are < 5.5 and 8.3 respectively. Selective against the D4 receptor in both agonist and antagonist assays. Brain penetrant.

Related Products: (+)-PD 128907 U 99194 GR 103691
Potent and selective MCH1 antagonist
3359 | ATC 0065

IC50 = 15.7 nM. Displays > 96-fold selectivity over MCH2. Exhibits antidepressant and anxiolytic activity in vivo. Also displays affinity for 5-HT1A and 5-HT2B receptors (IC50 values are 62.9 and 266 nM respectively). Orally active.

Related Products: MCH (human, mouse, rat) ATC 0175 SNAP 94847
Selective GSK-3 inhibitor
3966 | AR-A 014418

IC50 = 104 nM. Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 μM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices.

Related Products: SB 216763 SB 415286 BIO-acetoxime

July 2010

Axin stabilizer
3532 | endo-IWR 1

Inhibitor of Wnt signaling. Induces an increase in Axin2 protein levels; promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes.

Related Products: IWP 2 PNU 74654 XAV 939
High affinity 5-HT1A receptor antagonist
3282 | NAD 299

Ki = 0.6 nM in vitro. Enhances the action of selective 5-HT reuptake inhibitors and reverses citalopram-induced inhibition of serotonergic cell firing.

Related Products: Xaliproden 8-Hydroxy-DPAT hydrobromide (S)-WAY 100135
GSK-3β inhibitor
3835 | TWS 119

IC50 = 30 nM. Induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).

Related Products: SB 216763 SB 415286 Kenpaullone
TRPV1 antagonist
3875 | BCTC

Inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). Displays analgesic properties in rat models of inflammatory and neuropathic pain. CNS penetrant.

Related Products: Anandamide (in TocrisolveTM 100) Capsazepine 5'-Iodoresiniferatoxin

June 2010

Selective nNOS inhibitor
3319 | ARL 17477

IC50 values are 1 and 17 μM for neuronal NOS and endothelial NOS respectively. Reduces ischemic cell damage after middle cerebral artery (MCA) occlusion in rats. Displays a synergistic neuroprotective effect when combined with either an NMDA or AMPA receptor antagonist.

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Positive allosteric modulator of M4 receptors
3383 | VU 152100

EC50 = 380 nM. Induces 21-fold shift in ACh potency at M4 receptor. Displays no activity at other mAChR subtypes.

Related Products: Galanthamine hydrobromide Cisapride Xanomeline
Selective S1P1 receptor agonist
3601 | CYM 5442

EC50 = 1.35 nM. Activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1. Induces acute lymphopenia in mice. Brain penetrant.

Related Products: SEW 2871 Sphingosine-1-phosphate JTE 013
Orally active p38α and p38β inhibitor
3916 | VX 702

KD values are 3.7 and 17 nM respectively.

Related Products: SB 239063 SB 203580 CGP 57380
Wnt production inhibitor
3533 | IWP 2

Inactivates Porcn, a membrane-bound O-acyltransferase (MBOAT), and selectively inhibits palmitoylation of Wnt. Blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation.

Related Products: PNU 74654 XAV 939 BIO

May 2010

Potent and selective H4 receptor antagonist
3640 | A 987306

pKi values are 8.24 and 8.47 in human and rat H4 receptors respectively. Displays 162-fold, 620-fold, and > 1600-fold selectivity over human H3, H1 and H2 receptors. Blocks zymosan-induced neutrophil reflux and attenuates thermal hypersensitivity in vivo (ED50 = 42 μmol/kg, ip).

Related Products: 4-Methylhistamine VUF 8430 JNJ 10191584
Potent P2X4 receptor antagonist
3579 | 5-BDBD

Blocks P2X4-mediated currents in Chinese hamster ovary cells (IC50 = 0.50 μM).

Related Products: PPADS Suramin TNP-ATP
Potent and selective IKs blocker
3899 | JNJ 303

IC50 = 64 nM. Displays no effects on other cardiac channels; IC50 values are 3.3, >10, 11.1 and 12.6 μM for INa, ICa, Ito and IKr channels respectively. Prolongs QT and causes unprovoked torsades de pointes (TdP).

Related Products: XE 991 E-4031 Linopirdine
Potent NPY Y5 antagonist
3562 | LU AA33810

Ki = 1.5 nM in vitro. Displays ≥ 3300-fold affinity for Y5 over Y1, Y2 and Y4 receptors. Also binds human 5-HT2B and 5-HT1A receptors (Ki values are 247 and 478 nM respectively). Exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity.

Related Products: L-152,804 BIIE 0246 BIBP 3226
Potent, dual orexin receptor antagonist
3818 | TCS 1102

Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively. Inhibits ADL-orexin B-mediated locomotion following i.p. administration in vivo. Brain penetrant.

Related Products: Orexin A (human, rat, mouse) Orexin B (human) Orexin B (mouse)

April 2010

Potent and selective PI 3-kinase γ (PI3Kγ) inhibitor
3578 | AS 605240

Displays 30-fold selectivity over PI3Kδ and PI3Kβ and 7.5-fold selectivity over PI3Kα. Suppresses the progression of joint inflammation and damage in both lymphocyte-independent and lymphocyte-dependent mouse models of rheumatoid arthritis.

Related Products: LY 294002 PI 103 PI 828
Potent and selective NPY Y5 antagonist
3677 | NPY 5RA972

IC50 values are 3.1, >10000, >10000 and >10000 nM for Y5, Y1, Y2 and Y4 receptors respectively. Does not block NPY-induced feeding in vivo. Orally active and brain penetrant.

Related Products: L-152,804 BWX 46 S 25585
Potent and selective ERβ agonist
3523 | FERb 033

Ki = 7.1 nM, EC50 = 4.8 nM. Displays 62-fold selectivity over ERα.

Related Products: DPN PHTPP WAY 200070
Potent and selective NOP antagonist
3661 | BAN ORL 24

IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively. Inhibits nociceptin-induced stimulation of [35S]-GTPγS binding and Ca2+ mobilization in CHO cells in vitro.

Related Products: (±)-J 113397 Nociceptin UFP-101
Potent and selective H4 antagonist
3753 | A 943931

pKi values are 7.15 and 8.12 at human and rat receptors respectively. Blocks inflammation in a peritonitis mouse model and displays efficacy in inflammatory pain and neuropathic pain models.

Related Products: 4-Methylhistamine JNJ 10191584 VUF 8430

March 2010

Subtype-selective α4β2 partial agonist
3754 | Varenicline

Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively. Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo.

Related Products: Dihydro-β-erythroidine 5-Iodo-A-85380
Potent VEGFR, PDGFRβ and KIT inhibitor
3768 | Sunitinib

Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively. Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.

Related Products: PD 161570 SU 5402 Ki 8751
Potent, selective CB2 agonist
3556 | SER 601

Ki values are 6.3 nM and 1.2 μM for CB2 and CB1 receptors respectively. Displays analgesic activity in the formalin test in mice.

Related Products: AM 630 JTE 907 HU 308
Potent and selective P2Y12 antagonist
3321 | AR-C 66096

Blocks ADP-induced inhibition of adenylyl cyclase in vitro (PKB =7.6) and inhibits ADP-induced aggregation of washed human platelets (pIC50 = 8.16).

Related Products: (±)-Clopidogrel MRS 2179 MRS 2365
Dual CK1/cdk inhibitor
3610 | (R)-DRF053

IC50 values are 220, 80 and 14 nM for cdk1/cyclin B, cdk5/p25 and CK1 respectively. Selective over GSK-3 α/β (IC50= 4.1 μM). Also shown to inhibit amyloid-β production in N2A-APP695 cells.

Related Products: PF 670462 D 4476 Purvalanol A

February 2010

High affinity and selective GPR30 antagonist
3678 | G-15

Ki = 20 nM. Displays no affinity for ERα and ERβ at concentrations up to 10 μM. Inhibits agonist-induced calcium mobilization in vitro (EC50 of ~185 nM) and antagonizes the antidepressive effects of estrogen in vivo.

Related Products: G-1 ICI 182,780 Tamoxifen
Selective Pim kinase inhibitor
3714 | TCS PIM-1 4a

IC50 values are 24 and 100 nM for Pim-1 and Pim-2 respectively. Displays selectivity over a panel of ~50 other kinases tested. Exhibits cytotoxicity in PC3 prostate carcinoma cells in vitro (IC50 = 17 μM).

Related Products: PIM-1 Inhibitor 2 TCS PIM-1 1
Selective mTOR inhibitor
3725 | KU 0063794

IC50 ~10 nM for mTORC1 and mTORC2 respectively. Displays no activity at PI 3-K or 76 other kinases tested. Suppresses cell growth and induces G1 cell cycle arrest in vitro.

Related Products: Compound 401 PI 103 Rapamycin
Primes ESCs for differentiation
3741 | Stauprimide

Interacts with NME2 and inhibits its nuclear translocation. Increases the efficiency of directed differentiation of mouse and human embryonic stem cells (ESCs) in vitro.

Potent, collagenase-selective MMP inhibitor
2916 | Ro 32-3555

Ki values are 3.0, 3.4, 4.4, 59, 154 and 527 nM for MMP-1, MMP-13, MMP-8, MMP-9, MMP-2 and MMP-3 respectively. Inhibits cartilage breakdown in vitro and in vivo and displays antiarthritic activity. Orally active.

Related Products: Batimastat Marimastat UK 370106

January 2010

PAM of δ-containing GABAA receptors
3679 | DS2

EC50 = 142 nM for α4β3δ receptors. Displays no effects on GABA responses mediated by α4β3γ2 and α1β3γ2 receptors.

Related Products: L-655,708 L-838,417 TB 21007
Potent and selective P2X7 antagonist
3701 | A 740003

IC50 values are 18 and 40 nM for rat and human receptors respectively. Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain.

Related Products: AZ 10606120 GW 791343 Ro 0437626
Potent and selective CCR3 antagonist
3650 | SB 328437

IC50 = 4 nM. Displays > 2500-fold selectivity over C5aR, LTD4, CCR7, CXCR1 and CXCR2 receptors. Inhibits eotaxin-, eotaxin-2- and MCP-4-induced Ca2+ mobilization.

Related Products: BMS CCR2 22 RS 504393 UCB 35625
Tankyrase inhibitor; inhibits wnt signaling
3748 | XAV 939

IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively. Antagonizes wnt signaling via stimulation of β-catenin degradation and stabilization of axin.

Related Products: PJ 34 DR 2313 NU 1025
Selective TRPV4 ligands
3745 | RN 1747 & 3746 | RN 1734

RN 1747 is a selective TRPV4 agonist (EC50 values are 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively) that also antagonizes TRPM8 at relevant concentrations (IC50 = 4 μM). RN 1734 is a selective TRPV4 antagonist (IC50 values are 2.3, 5.9 and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4 receptors respectively).

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