R&D Systems Inc. Tocris Bioscience Boston Biochem

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 103691
Specific 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 Lactacystin
Potent 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 U0126
mGlu5 antagonist
4394 | VU 0360223

Potent antagonist of mGlu5 (IC50 = 61 nM).

Related Products: MTEP Fenobam Bay 36-7620
N-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 A

January 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 106
AMPA 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 PEPA
Orally 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 Desmopressin
Potent 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 2578
Allosteric 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 124

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