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IκB kinase (IKK)
The IκBs form a small family of related proteins with a core consisting of six or more ankyrin repeats, an N-terminal regulatory domain and a C-terminal domain that contains a PEST motif. There is strong biochemical and genetic evidence that the IKK complex, which consists of two catalytic subunits, IKKα and IKKβ, and a regulatory subunit, IKKγ, is the master regulator of NF-κB-mediated innate immune and inflammatory responses. The best-studied and major IκB protein is IκBα.IκB kinase activity is essential for activation of members of the nuclear factor-kB (NF-κB) family of transcription factors, which play a fundamental role in lymphocyte immunoregulation. Increased NF-κB activity as a result of constitutive IKK-mediated phosphorylation of IκBα has been observed in the development of atherosclerosis, asthma, rheumatoid arthritis, inflammatory bowel diseases, and multiple sclerosis.
Immunology/Inflammation
Amino Acids and Derivatives(42)
Antiviral(77)
CD110(2)
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IκB kinase (IKK)(41)
Lipoxygenase(53)
LTR(13)
MyD88(6)
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PD-1/PD-L1(38)
PGE synthase(14)
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IκB kinase (IKK)
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HOIPIN-8 sodium
产品货号 : M35672
cas no: 2519537-70-1
HOIPIN-8 is a potent inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. As a derivative of HOIPIN-1, it exhibits 255-fold greater inhibition of both petit-LUBAC and TNF-α-mediated NF-κB activation compared to HOIPIN-1. HOIPIN-8 is a promising tool to explore cellular functions of LUBAC.
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IKK2-IN-4
产品货号 : M34854
cas no: 354811-10-2
IKK2-IN-4 (compound 4) 是一种有效的 IKK-2 抑制剂，IC50 值为 25 nM。IKK2-IN-4 可抑制 LPS 诱导的 PBMC 中 TNFα 的产生。
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ACHP
产品货号 : M33778
cas no: 406208-42-2
ACHP (IKK-2 Inhibitor VIII) is a novel selective and potent IKK inhibitor with inhibitory effects on IKK-α and IKK-β. ACHP has anti-HIV-1 activity and inhibits HIV-1 long terminal repeat (LTR)-driven gene expression through inhibition of NF-κB activation, inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR, and inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR. ACHKP has anti-HIV-1 activity and inhibits TNF-α-induced recruitment of NF-κB (p65) to the HIV-1 LTR.
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GSK319347A
产品货号 : M33384
cas no: 862812-98-4
GSK319347A 是 TBK1 和 IKKε 的双重抑制剂，IC50 分别为 93 nM 和 469 nM。 GSK319347A 还抑制 IKK2，IC50 为 790 nM。
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HPN-01
产品货号 : M32960
cas no: 928655-63-4
HPN-01 是一种有效选择性的 IKK 抑制剂，对 IKK-α、IKK-β 和 IKK-ε 的 pIC50 6.4、7.0 和 <4.8。HPN-01 比 50 多种其他激酶显示出大于50倍的选择性，包括 ALK5、CDK-2、EGFR、ErbB2、GSK3β、PLK1、Src 和 VEGFR-2。
