401487
IKK-2 Inhibitor VIII
The IKK-2 Inhibitor VIII, also referenced under CAS 406208-42-2, controls the biological activity of IKK-2. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.
别名:
IKK-2 Inhibitor VIII, 2-Amino-6-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-4-(4-piperidinyl)-3-pyridinecarbonitrile, ACHP
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About This Item
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质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 10 mg/mL
运输
wet ice
储存温度
−20°C
SMILES字符串
N1CCC(CC1)c2c(c(nc(c2)c3c(cccc3O)OCC4CC4)N)C#N
InChI
1S/C21H24N4O2/c22-11-16-15(14-6-8-24-9-7-14)10-17(25-21(16)23)20-18(26)2-1-3-19(20)27-12-13-4-5-13/h1-3,10,13-14,24,26H,4-9,12H2,(H2,23,25)
InChI key
DYVFBWXIOCLHPP-UHFFFAOYSA-N
一般描述
A cell-permeable piperidinyl-pyridine compound that acts as a selective inhibitor of IKK-2 activity (IC50 = 8.5 and 250 nM for IKK-2 and IKK-1, respectively) with little effect towards IKK-3, Syk, and MKK4 (IC50 >20 µM). Exhibits good aqueous solubility (0.12 mg/ml in pH 7.4 isotonic buffer) and potent activity in various cellular assays in vitro (IC50<150 nM). Shown to be orally bioavailable both in rats and mice (BA = 60% and 16%, respectively) and effectively inhibit arachidonic acid-induced swelling in a murine ear edema model in vivo.
生化/生理作用
Cell permeable: yes
Primary Target
IKK-2
IKK-2
Product does not compete with ATP.
Reversible: no
Target IC50: 8.5 and 250 nM for IKK-2 and IKK-1, respectively
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
制备说明
Sonication is required for complete solubilization.
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Murata, T., et al. 2004. Bioorg. Med. Chem. Lett.14, 4019.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Jin Hua Liang et al.
mBio, 12(4), e0153021-e0153021 (2021-07-21)
Epstein-Barr virus (EBV) is associated with 200,000 cancers annually, including B-cell lymphomas in immunosuppressed hosts. Hypomorphic mutations of the de novo pyrimidine synthesis pathway enzyme cytidine 5' triphosphate synthase 1 (CTPS1) suppress cell-mediated immunity, resulting in fulminant EBV infection and
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