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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEKK (MAP3K)-IKAM-1
IKAM-1

Chemical Structure : IKAM-1

CAS No.: 2345648-37-3

IKAM-1 (Compound 39-100)

货号: PC-38626Not For Human Use, Lab Use Only.

IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

IKAM-1 (Compound 39-100) is an orally bioavailable, small-molecule IKKβ activation modulator (IKAM) that selectively targets MAP3K1, inhibits TNF-α-induced IKKβ-mediated NF-κB activation in A549 cells with IC50 of 4.7 uM.
IKAM-1 (Compound 39-100) selectively binds to MAP3K1 and MAP3K12, inhibits MAP3K1 with IC50 of 4.2 uM, does not inhibit IKKβ but selectively inhibits MAP3K1 with micromolar potency in PANC1 cell lysates.
IKAM-1 (Compound 39-100) inhibits MAP3K1-mediated IKKβ phosphorylation and reduced levels of p-IKKβ in with an IC50 value of 2.3 uM, inhibits the growth of PC lines with lowmicromolar potencies.
IKAM-1 (Compound 39-100) reduces activated IKKβ levels, inhibits tumor growth, and reduces metastasis in mice pancreatic tumor models.

物理化学性质&存储条件

分子量 441.26
分子式 C19H14BrFN6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(3-bromo-4-fluorophenyl)-3-(3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl)urea

参考文献

1. Napoleon JV, et al. Proc Natl Acad Sci U S A. 2022 May 3;119(18):e2115071119.

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