Welcome to Tocris Bioscience

Tocris is the leading supplier of novel and exclusive tools for laboratory research. Our unique collection of over 4,000 life science reagents consists of GPCR ligands, neurotransmitters, ion channel modulators and signaling inhibitors.

High affinity and selective P2Y₁₄ antagonist

4862 | PPTN

K_B = 434 nM. Exhibits >10,000-fold selectivity for P2Y₁₄ over other P2Y receptors. Inhibits UDP-glucose and MRS 2690-induced porcine pancreatic artery contraction ex vivo. Also blocks UDP-glucose-induced chemotaxis of HL-60 leukemia cells in vitro.

Selective mIDH1 inhibitor; phenotypically lethal

5244 | TC-E 5008

K_i = 120-190 nM. Displays >60-fold selectivity for mIDH1 (found in ~75% of gliomas) over wild type IDH1. Also inhibits D-2-hydroxyglutaric acid in cells expressing mIDH1 (EC₅₀ = 2.4 μM). Does not display cytotoxicity towards non-cancerous human cells. Phenotypically lethal.

Potent cdk1/2 inhibitor

5654 | BMS 265246

IC₅₀ values are 6, 9 and 230 nM for cdk1, cdk2 and cdk4, respectively. Inhibits proliferation of HCT-116 colon cancer cells in vitro.

Potent and selective inhibitor of integrins α_vβ₃ and α_vβ₅

5870 | Cilengitide

IC₅₀ values are 4.1 and 70 nM for α_vβ₃ and α_vβ₅, respectively. Exhibits ~10-fold selectivity over gpIIb/IIIa. Increases endothelial monolayer permeability. Also exhibits antiangiogenic activity.

ADAM 17 (TACE) and MMP inhibitor; orally bioavailable

5960 | TMI 1

IC₅₀ values are 3, 4.7, 6.6, 8.4, 12, 26 and 26 nM for MMP-13, MMP-2, MMP-1, ADAM 17, MMP-9, MMP-7 and MMP-14, respectively. Suppresses TNF-α production in an acute LPS-mouse model. Reduces severity score in an in vivo model of rheumatoid arthritis. Displays selective cytotoxicity towards tumor cells and cancer stem cells in vitro. Induces tumor apoptosis in a breast cancer in vivo model. Orally bioavailable.

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