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Featured Products 2012
Highlighted products added to the Tocris Bioscience range during 2012
February 2012
Selective D3 antagonist
4207 | SB 277011A
pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively. Brain penetrant.
Related Products: GSK 789472 U 99194 GR 103691Specific E3 ubiquitin ligase inhibitor
4375 | SMER 3
Specific inhibitor of a yeast SCF family E3 ubiquitin ligase (SCFMet30) in vitro and in vivo. Induces the expression of MET genes; blocks cell proliferation. Enhancer of Rapamycin (Cat. No. 1292).
Related Products: PYR 41 IU1 LactacystinPotent and selective DAPK1 inhibitor
4301 | TC-DAPK 6
ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) (IC50 values are 69 and 225 nM for DAPK1 and DAPK3 respectively, when assayed with 10 μM ATP). Displays selectivity for DAPK1 over a range of 48 other kinases, including Abl, AMPK, Chk1, Met and Src (IC50 > 10 μM).
Related Products: DAPK Substrate Peptide Necrostatin-1 U0126mGlu5 antagonist
4394 | VU 0360223
Potent antagonist of mGlu5 (IC50 = 61 nM).
Related Products: MTEP Fenobam Bay 36-7620N-WASP inhibitor
4434 | Wiskostatin
Inhibitor of neural Wiskott-Aldrich syndrome protein (N-WASP) activity. Interacts with the regulatory GTPase-binding domain of N-WASP; inhibits activation of Arp2/3 complex by maintaining N-WASP in an inactive conformation. Also inhibits PIP2-induced actin polymerization (EC50 ~ 4μM).
Related Products: 187-1, N-WASP inhibitor CK 666 Latrunculin AJanuary 2012
HDAC 6 inhibitor
3402 | Tubacin
Inhibits the second deacetylase domain (DD2). Does not inhibit HDAC6 histone deacetylase activity; reversibly inhibits α-tubulin deacetylation. Increases α-tubulin acetylation levels with no effect on histone acetylation or cell cycle progression.
Related Products: KD 5170 MC 1568 TC-H 106AMPA receptor modulator
3911 | S 18986
Positive allosteric modulator of AMPA receptors. Exhibits cognitive enhancing properties in rodent behavioral models. Brain penetrant.
Related Products: CX 546 Cyclothiazide PEPAOrally active vasopressin V1 antagonist
3924 | OPC 21268
Displays greater affinity for rat V1 than human V1 (Ki = 25 and 8800 nM respectively). Exhibits 1000-fold selectivity for V1 receptors over V2 receptors. Orally active.
Related Products: SR 49059 (d(CH2)51,Tyr(Me)2,Arg8)-Vasopressin DesmopressinPotent P2Y6 agonist
4376 | 5-OMe-UDP trisodium salt
EC50 = 0.08 μM. Displays greater potency at P2Y6 than UDP (Cat.No. 3111) (EC50 = 0.14 μM).
Related Products: PSB 0474 MRS 2693 trisodium salt MRS 2578Allosteric Akt inhibitor
4398 | SC 66
Interferes with pleckstrin homology domain binding to PIP3 and facilitates Akt ubiquitination. Exhibits anticancer activity in vitro and in vivo.
Related Products: GSK 690693 API-1 FPA 124Quick Order
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