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LTβR-IN-1

CAS No. : 2189366-77-4

MCE 国际站：LTβR-IN-1

产品活性：LTβR-IN-1 是一种有效的、选择性淋巴毒素 β 受体 (LTβR) 抑制剂。LTβR-IN-1 选择性抑制依赖于 TNF12A 的 p52 的核易位，不影响 TNF-α 受体介导的 p65 的核易位。LTβR-IN-1 抑制受 TWEAK 或 Anti-LTβR 刺激的 p52 核易位，IC₅₀ 分别为 17 μM。LTβR-IN-1 以配体非依赖性方式调节 NF-kB 信号通路。

研究领域：NF-κB

作用靶点：NF-κB

In Vitro: LTβR-IN-1 (compound 919278) (1 nM-100 μM; 30 min) inhibits p52 nuclear translocation in response to stimulation with Anti-LTβR or TWEAK (20 ng/mL, respectively; 4 h) with IC₅₀s of 0.169 μM and 0.167 μM, respectively.
LTβR-IN-1 (3 nM-30 μM; 45 min) reduces the binding affinities of both CDK12 and its associated protein, CCNK in both TWEAK-stimulated and control U-2 OS cells, with IC₅₀s of 50-61 nM for CDK12 and 29-68 nM for CCNK, respectively.
LTβR-IN-1 reduces the mRNA abundance of MAP3K14 in with an IC₅₀ value of 0.32 μM in U-2 OS cells.
LTβR-IN-1 (1-10 μM; 30 min) decreases the phosphorylation of serine-2 (Ser2) on the C-terminal domain (CTD) of RNA polymerase (Pol) II.
LTβR-IN-1 regulates the noncanonical pathway in a ligandindependent manner and selectively inhibits the noncanonical pathway while sparing the canonical NF-kB signaling pathway.

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