New Products June 2011
RXR agonist
4064 | Fluorobexarotene
RXR agonist (Ki = 12 nM; EC50 = 43 nM at RXRα receptors). Displays similar RAR agonist activity to bexarotene; exhibits an apparent RXR binding affinity 75% greater than bexarotene.
Related Products: LG 101506 UVI 3003 Docosahexaenoic acid
Akt kinase inhibitor
4144 | GSK 690693
ATP-competitive pan-Akt kinase inhibitor (IC50 values are 2, 13 and 9 nM for Akt1, 2 and 3 respectively). Also exhibits some inhibition for AMPK, PKA and PAK and PKC isoforms (IC50 < 100 nM). Displays antiproliferative and apoptotic effects in tumour cell lines.
Related Products: API-2 10-DEBC FPA 124
High affinity H3 receptor antagonist
4020 | JNJ 5207852
High affinity histamine H3 receptor neutral antagonist (pKi values are 8.9 and 9.2 in rat and human respectively). Brain penetrant and orally active. Has 3- and 100-fold higher affinity than thioperamide (Cat. No. 0644) for rat and human H3 receptors respectively. Suppresses slow-wave sleep; exhibits wake-promoting effects in rodent arousal models.
Related Products: Imetit Clobenpropit JNJ 10181457
Potent, selective Aurora kinase A inhibitor
4066 | TC-A 2317
Potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B). Selective over 60 other kinases (IC50 values > 1000 nM). Exhibits good cell permeability and antitumor activity.
Related Products: ZM 447439 Anti-Aurora A NSC 95397
PPARα/γ agonist
3965 | Tesaglitazar
Dual-specificity PPARα/γ agonist (IC50 values are 0.35 and 3.8 μM for PPARγ and PPARα respectively). Prevents atherosclerosis progression in E3L.CETP transgenic mice. Also reduces insulin resistance in obese Zucker rats. Orally active.
Related Products: CP 775146 WY 14643 Troglitazone
All new products this month
Alda 1, C 646, CCG 63802, Fluorobexarotene, GSK 690693, JNJ 5207852, KW 3902, MDA 19, MitMAB, Mitoxantrone, NPS 2390, OctMAB, Olopatadine, 3-pyr-Cytisine, Ro 3306, SB 297006, SKF 86466, TC-A 2317, Tesaglitazar
