| Bioactivity | LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor. LTβR-IN-1 also selectively inhibits the nuclear translocation of p52 depended on TNF12A, instead of the nuclear translocation of p65 mediated by TNF-α receptor. LTβR-IN-1 regulates the NF-kB signaling pathway IN a ligand-independent manner[1]. | ||||||||||||
| Target | LTβR; p52 translocation; MAP3K14; NF-κB | ||||||||||||
| Invitro | LTβR-IN-1 (化合物 919278) (1 nM-100 μM；30 分钟) 抑制 p52 核转位以响应 Anti-LTβR 或 TWEAK (分别为 20 ng/mL；4 小时) 的刺激，IC50 分别为 0.169 μM 和 0.167 μM[1]。LTβR-IN-1 (3 nM-30 μM；45 分钟) 在受 TWEAK 刺激和对照 U-2 OS 细胞中均降低了 CDK12 及其相关蛋白 CCNK 的结合亲和力，IC50 分别为 50-61 nM 和 29-68 nM[1]。LTβR-IN-1 降低 U-2 OS 细胞中 MAP3K14 的 mRNA 丰度，IC50 μM 为 0.32 μM[1]。LTβR-IN-1 (1-10 μM；30 分钟) 降低 RNA 聚合酶 (Pol) II 的 C 末端结构域 (CTD) 上丝氨酸 2 (Ser2) 的磷酸化[1]。LTβR-IN-1 以配体非依赖性方式调节非经典通路，并选择性地抑制非经典通路，同时保留经典 NF-kB 信号通路[1]。 Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | LTβR-IN-1 | ||||||||||||
| CAS | 2189366-77-4 | ||||||||||||
| Formula | C18H16N4O2 | ||||||||||||
| Molar Mass | 320.35 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Henry KL, et al. CDK12-mediated transcriptional regulation of noncanonical NF-κB components is essential for signaling. Sci Signal. 2018 Jul 31;11(541). |