HOIPIN-8 是线性泛素链组装复合物 (LUBAC) 的有效抑制剂，IC₅₀ 为 11 nM。HOIPIN-8 是 HOIPIN-1 的衍生物，与 HOIPIN-1 相比，它表现出 255 倍的 petit-LUBAC 抑制能力， 对 LUBAC 和 TNF-α 介导的 NF-κB 激活作用的抑制， 是 HOIPIN-1 抑制作用的 10 倍和 4 倍。HOIPIN-8 是一个很有前途的工具用于研究 LUBAC 的细胞功能。

HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC 50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC.

Solid

HOIPIN-8 (0-100 μM; 72 hours) has little cell toxicity on A549 cells, and exhibits an IC50 value of 100 μM.
HOIPIN-8 (0-10 μM; 24 hours) has an inhibitory effect over 10-fold enhancement over that of HOIPIN-1 on NF-κB activation, exhibits an IC50 value of 0.42?μM in HEK293T cells.
HOIPIN-8 (0-30 μM; NF-κB luciferase reporter is transfected into cells for 18 hours; then with 10?ng/ml TNF-α for 6?h) exhibits a 4-fold enhancements of the potency than HOIPIN-1, the IC50 value is 11.9 μM. It also effectively reduces IL-1β-induced expression of NF-κB target genes, such as ICAM1 and IL-6 as compared to HOIPIN-1.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[1]. Ken Katsuya, et al. Small-molecule Inhibitors of Linear Ubiquitin Chain Assembly Complex (LUBAC), HOIPINs, Suppress NF-κB Signaling. Biochem Biophys Res Commun. 2019 Feb 12;509(3):700-706.

In Vitro: DMSO : 100 mg/mL (219.12 mM; Need ultrasonic)配制储备液