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.

Selective p300 histone acetyltransferase (HAT) inhibitor

5103 | Lys-CoA

IC₅₀ = 50-500 nM. Exhibits approximately 100-fold selectivity for p300 over PCAF (IC₅₀ = 200 μM). Inhibits p300-dependent transcription. Active in vivo.

Monocarboxylate transporter (MCT1) inhibitor

5658 | AR-C 141990

pK_i = 7.6. Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4. Inhibits graft versus host response and prolongs cardiac graft survival in a rat model. Immunosuppressant. Also inhibits brain penetration of GHB analog HOCPCA.

Potent and selective Brk inhibitor

6073 | P21d

IC₅₀ = 30 nM. Exhibits >650-fold selectively for Brk over Aurora B kinase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also active in vivo and orally bioavailable.

Potent and selective SAM-competitive EZH2 inhibitor

6128 | GSK 343

IC₅₀ = 4 mM. Exhibits >60 fold selectivity for EZH2 over EZH1 and a range of other methyltransferases. Inhibits proliferation of prostate cancer cell lines in vitro.

Potent apelin (APJ) receptor agonist

6293 | ELA-14 (human)

K_i = 0.93 nM. ELABELA analog. Activates Gα_il pathway and β-arrestin-2 recruitment . Reduces arterial pressure in rat hearts. Active in vivo. ELA-14 negative control (Cat.No. 6294) available.

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