Custom Premix Selecting "Custom Premix" option means that all of the beads you have chosen will be premixed in manufacturing before the kit is sent to you.
Catalogue Number
Ordering Description
Qty/Pack
List
この品目はお気に入りに追加されました。
動物種
パネルタイプ
選択したキット
数量
カタログ番号
注文内容
Qty/Pk
価格
96-Well Plate
数量
カタログ番号
注文内容
Qty/Pk
価格
その他の試薬を追加 （MAPmatesとともに使用するにはバッファーおよび検出キットが必要です）
数量
カタログ番号
注文内容
Qty/Pk
価格
48-602MAG
Buffer Detection Kit for Magnetic Beads
1 Kit
Space Saver Option（チェックを入れると箱詰めから袋詰めに変更となりますのでご注意ください） Customers purchasing multiple kits may choose to save storage space by eliminating the kit packaging and receiving their multiplex assay components in plastic bags for more compact storage.
A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20 nM), and p70S6K (IC50 = 85 nM) in an ATP-competitive manner (Ki = 18 nM using AKT2), with much reduced potency toward RSK1 (IC50 >100 nM) and a panel of 13 other cellular kinases (IC50 >1 µM). Shown to reduce cellular phosphorylation of GSK-3β (IC50 range from 2.08 to 4.45 µM), S6R, FKHRL1, and inhibit the proliferation of cancer cells exhibiting constitutive Akt pathway activation both in vitro (IC50 range from 0.94 to 11.86 µM) and in mice in vivo (20 mg/kg via i.p. or 90 mg/kg via p.o.).
Catalogue Number
124033
Brand Family
Calbiochem®
Synonyms
p70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, S6K1 Inhibitor III, Chlorophenyl-pyrazolyl-phenyl-piperidine
References
References
Grimshaw, K.M., et al. 2010. Mol. Cancer Ther.9, 1100. Saxty, G., et al. 2007. J. Med. Chem.50, 2293.
Grimshaw, K.M., et al. 2010. Mol. Cancer Ther.9, 1100. Saxty, G., et al. 2007. J. Med. Chem.50, 2293.
データシート
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
23-May-2013 JSW
Synonyms
p70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, S6K1 Inhibitor III, Chlorophenyl-pyrazolyl-phenyl-piperidine
Description
A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20 nM), and p70S6K (IC50 = 85 nM) in an ATP-competitive manner (Ki = 18 nM using AKT2), with much reduced activity toward RSK1 (IC50 >100 nM) and a panel of 13 other cellular kinases (IC50 >1 µM), including PDK1, PI 3-Kβ, SGK, GSK-3β, and MEK1. Shown to effectively reduce the phosphorylation levels of GSK-3β, S6R, and FKHRL1 (IC50 range from 2.08 to 4.45 µM against GSK-3β pSer9 level), as well as inhibit the proliferation (IC50 range from 0.94 to 11.86 µM) of cancer cells exhibiting constitutive Akt pathway activation, including the PTEN-deficient MES-SA uterine sarcoma and U87MG glioblastoma cell lines. AT7867 treatments via i.p. or p.o. (20 mg/kg and 90 mg/kg, respectively, once every 3 days) are also reported to result in Akt pathway and tumor growth inhibition in mice bearing MES-SA (~40% of untreated control on day 10 by i.p. or p.o.) or U87MG (~50% of untreated control on day 10 by i.p.) xenograft in vivo.
Form
White powder
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₀H₂₀ClN₃
Structure formula
Purity
≥99% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Grimshaw, K.M., et al. 2010. Mol. Cancer Ther.9, 1100. Saxty, G., et al. 2007. J. Med. Chem.50, 2293.
