420104
JAK3 Inhibitor II
The JAK3 Inhibitor II, also referenced under CAS 211555-04-3, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
別名:
JAK3 Inhibitor II, 4-[(3ʹ-Bromo-4ʹ-hydroxyphenyl)amino]-6,7-dimethoxyquinazoline, WHI-P154
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About This Item
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品質水準
アッセイ
≥97% (HPLC)
フォーム
solid
メーカー／製品名
Calbiochem®
保管条件
OK to freeze
protect from light
色
pale yellow
溶解性
DMSO: 100 mg/mL
輸送温度
ambient
保管温度
−20°C
SMILES記法
Brc1c(ccc(c1)Nc2ncnc3c2cc(c(c3)OC)OC)O
InChI
1S/C16H14BrN3O3/c1-22-14-6-10-12(7-15(14)23-2)18-8-19-16(10)20-9-3-4-13(21)11(17)5-9/h3-8,21H,1-2H3,(H,18,19,20)
InChI Key
CBIAKDAYHRWZCU-UHFFFAOYSA-N
詳細
A potent, cell-permeable, reversible, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 5.6 µM). Has no effect on either JAK1 or JAK2. Has also been shown to prevent the ionizing radiation-induced activation of c-Jun in DT-40 cells. Also acts as a potent inhibitor of glioblastoma cell adhesion and migration.
生物化学的／生理学的作用
Cell permeable: yes
Primary Target
JAK-3
JAK-3
Product competes with ATP.
Reversible: yes
Target IC50: 5.6 µM against JAK3
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
再構成
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
その他情報
Ghosh, S., et al. 2001. Acta Crystallogr. C.57, 76.
Sudbeck, E.A., et al. 1999. Clin. Cancer Res. 5, 1569.
Goodman, P.A., et al. 1998. J. Biol. Chem. 273, 17742.
Narla, R.K., et al. 1998. Clin Cancer Res.4, 2463.
Sudbeck, E.A., et al. 1999. Clin. Cancer Res. 5, 1569.
Goodman, P.A., et al. 1998. J. Biol. Chem. 273, 17742.
Narla, R.K., et al. 1998. Clin Cancer Res.4, 2463.
法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
保管分類コード
11 - Combustible Solids
WGK
WGK 3
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
420104-VMG:
420104-1.1ML:
420104-5MG:
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
E A Sudbeck et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 5(6), 1569-1582 (1999-07-02)
A novel homology model of the kinase domain of Janus kinase (JAK) 3 was used for the structure-based design of dimethoxyquinazoline compounds with potent and specific inhibitory activity against JAK3. The active site of JAK3 in this homology model measures
S Ghosh et al.
Acta crystallographica. Section C, Crystal structure communications, 57(Pt 1), 76-78 (2001-02-15)
The title compounds, C16H15BrN3(O3)(+).Cl(-).CH4O (WHI-P154) and C16H16N3(O3)(+).Cl(-) (WHI-P180), are potent inhibitors [WHI-P154 with IC50 = 5.6 microM and WHI-P180 with IC50 = 4.0 microM for epidermal growth factor receptor (EGFR) kinase inhibition] of the EGFR tyrosine kinase as well as
R K Narla et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 4(10), 2463-2471 (1998-10-31)
Glioblastoma multiforme is a highly invasive primary brain tumor with a disappointingly high local recurrence rate and mortality despite intensive multimodality treatment programs. Therefore, new agents that are capable of inhibiting the infiltration of normal brain parenchyma by glioblastoma cells
P A Goodman et al.
The Journal of biological chemistry, 273(28), 17742-17748 (1998-07-04)
Exposure of B-lineage lymphoid cells to ionizing radiation induces an elevation of c-jun proto-oncogene mRNA levels. This signal is abrogated by protein-tyrosine kinase (PTK) inhibitors, indicating that activation of an as yet unidentified PTK is mandatory for radiation-induced c-jun expression.
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