推薦產品
product name
JAK抑制剂I, JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC₅₀ = 15 nM), JAK2 (IC₅₀ = 1 nM), JAK3 (Ki = 5 nM) and Tyk2 (IC₅₀ = 1 nM).
品質等級
化驗
≥98% (HPLC)
形狀
solid
製造商/商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
off-white
溶解度
DMSO: 5 mg/mL
運輸包裝
ambient
儲存溫度
−20°C
InChI
1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
InChI 密鑰
VNDWQCSOSCCWIP-UHFFFAOYSA-N
一般說明
一种有效、可逆、细胞可渗透和ATP竞争性的Janus蛋白酪氨酸激酶(JAKs)抑制剂。显示对JAK1(对于鼠JAK1,IC50=15 nM)、JAK2(IC50=1 nM)、JAK3(Ki=5 nM)和Tyk2(IC50=1 nM)的有效抑制活性。在高得多的浓度下抑制其他激酶。显示抑制IL2和IL4依赖性的CTLL细胞增殖,并阻断STAT5的磷酸化;并且与AG 490(目录编号658401)不同,进一步诱导表达活化的JAKs和STAT3的多发性骨髓瘤细胞的生长抑制。也可获得10 mM(500 µg/162 µl)JAK抑制剂I的DMSO溶液(目录号420097)。
一种有效、细胞可渗透、可逆和ATP竞争性的Janus蛋白酪氨酸激酶(JAKs)抑制剂。显示对JAK1(对于鼠JAK1,IC50=15 nM)、JAK2(IC50=1 nM)、JAK3(Ki=5 nM)和Tyk2(IC50=1 nM)的有效抑制活性。在高得多的浓度下抑制其他激酶。显示抑制IL2和IL4依赖性的CTLL细胞增殖,并阻断STAT5的磷酸化;并且与AG 490(目录编号658401)不同,进一步诱导表达活化的JAKs和STAT3的多发性骨髓瘤细胞的生长抑制。
生化/生理作用
主要靶标
鼠JAK1
鼠JAK1
产物与ATP竞争。
可逆性:是
细胞可渗透性:是
靶标IC50:15 nM,针对鼠JAK1;1 nM,针对JAK2;1 nM,针对Tyk2
靶标Ki:5 nM,针对JAK3
包裝
用惰性气体包装
警告
毒性:标准处理(A)
重構
复溶后,等分并冷冻(-20°C)。储备溶液在-20°C下可稳定保存至多3个月。
其他說明
Pedranzini, L., et al. 2006.Cancer Res.66, 9714.
Lucet, I.S., et al. 2005.Blood107, 176.
Thompson, J.E., et al. 2002.Bioorg.Med. Chem. Lett.12, 1219.
Lucet, I.S., et al. 2005.Blood107, 176.
Thompson, J.E., et al. 2002.Bioorg.Med. Chem. Lett.12, 1219.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
分析證明 (COA)
輸入產品批次/批號來搜索 分析證明 (COA)。在產品’s標籤上找到批次和批號,寫有 ‘Lot’或‘Batch’.。
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