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Tocris is the leading supplier of novel and exclusive tools for laboratory research. Our unique collection of over 3,000 life science reagents consists of GPCR ligands, neurotransmitters, ion channel modulators and signaling inhibitors.

Potent, selective CCR1 antagonist

3496 | BX 471

K_i = 1 nM for human CCR1. Exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4. Inhibits MIP-α/CCL3-induced intracellular Ca²⁺ mobilization. Orally active; effectively reduces disease severity in a rat model of multiple sclerosis. Decreases renal fibrosis in a mouse model of obstructive nephropathy.

Potent, selective LRRK2 inhibitor

4629 | GSK2578215A

IC₅₀ values are 8.9 and 10.1 nM respectively for LRRK2[G2019S] mutant and wild-type LRRK2 respectively. Displays selectivity for LRRK2 against a panel of 460 other kinases. Blocks Ser910 and Ser935 phosphorylation in vitro and in peripheral tissues in vivo. Brain penetrant.

Mcl-1 inhibitor

4762 | MIM1

Selectively targets the BH3-binding pocket. Induces caspase-3/7 activation and cell death in Mcl-1-dependent leukemia cells. Also blocks Mcl-1-mediated suppression of tBID-induced Bax activation in vitro.

Potent and selective EP₂ receptor antagonist

4818 | PF 04418948

IC₅₀ = 16 nM for human EP₂ receptors. Displays over 2000-fold selectivity for EP₂ receptors over EP₁, EP₃, EP₄, DP₁ amd CRTH₂ receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE₂-induced increases in intracellular cAMP; reverses PGE₂-invoked relaxation of mouse trachea (IC₅₀ = 2.7 nM).

Tankyrase inhibitor

4855 | WIKI4

Inhibitor of Wnt/β-catenin signaling (EC₅₀ ~ 75 nM). Inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC₅₀ ~15 nM); prevents the ubiquitination and degradation of axin.

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June 23 - 26, 2013

Bath, UK