TBK1/IKKε-IN-5是一种口服有效的 TBK1 和 IKKε 双重抑制剂,其 IC50 值分别为 1 nM 和 5.6 nM。TBK1/IKKε-IN-5 能增强 PD-1 阻断反应,与 anti-PD-L1 联用时能诱导大鼠的免疫记忆,适用于癌症特别是肿瘤免疫研究。
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产品名称 | NF-κB ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PDTC ammonium | ✔ | 98% | |||||||||||||||||
QNZ |
++++
NF-κB, IC50: 11 nM |
99%+ | |||||||||||||||||
Sodium 4-Aminosalicylate Dihydrate | ✔ | 98% | |||||||||||||||||
Sodium Salicylate | ✔ | 95% | |||||||||||||||||
Parthenolide | ✔ | p53 | 97% HPLC | ||||||||||||||||
JSH-23 |
+
NF-κB, IC50: 7.1 μM |
98% | |||||||||||||||||
Phenethyl caffeate | ✔ | 98% | |||||||||||||||||
Andrographolide | ✔ | 98+% | |||||||||||||||||
Curcumin | ✔ | HDAC,Nrf2 | 98% | ||||||||||||||||
SC75741 |
+++
NF-κB, EC50: 200 nM |
99%+ | |||||||||||||||||
CBL0137 HCl |
++
NF-κB, EC50: 0.47 μM |
p53 | 99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | TBK1/IKKε inhibition can enhance response to PD-1 blockade, which effectively predicts tumor response in vivo. QUN97653 is a novel potent and selective TBK1/IKKε dual inhibitor with IC50s of 1 nM and 5.6 nM for TBK1 and IKKε, respectively. QUN97653 effectively blocked immune suppressive cytokine elaboration by CT26 cell line spheroids and enhanced secretion of IFN-γ and IL-2 from purified CD4+ and CD8+ T cells from healthy human donors and IL-2 from Jurkat human T-cell leukemia cells. Ex vivo addition of QUN97653 to PD-1 blockade enhanced killing of CT26 MDOTS (murine-derived organotypic tumor spheroids), associated with decreased levels of CCL4, CCL3, and IL-1β and induction of cytokines involved in activated innate immune responses. In Balb/c mice bearing CT26 tumors, greater tumor control and longer survival was evident with combination of QUN97653 with anti-PD-L1 than with either QUN97653 or anti-PD-L1 alone[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.95mL 0.39mL 0.19mL |
9.74mL 1.95mL 0.97mL |
19.47mL 3.89mL 1.95mL |
CAS号 | 1893397-65-3 |
分子式 | C28H31N7O3 |
分子量 | 513.591 |
别名 | compound 1 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 6 mg/mL(11.68 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |