N-(二苯并[B,D]呋喃-3-基)-5-硝基呋喃-2-甲酰胺

简介生物活性靶点体外研究 N-(二苯并[B,D]呋喃-3-基)-5-硝基呋喃-2-甲酰胺试剂级价格

CAS号:329198-87-0
英文名:N-(dibenzo[b,d]furan-3-yl)-5-nitrofuran-2-carboxamide
中文名:N-(二苯并[B,D]呋喃-3-基)-5-硝基呋喃-2-甲酰胺
CBNumber:CB44635440
分子式:C17H10N2O5
分子量:322.27
MOL File:329198-87-0.mol

N-(二苯并[B,D]呋喃-3-基)-5-硝基呋喃-2-甲酰胺化学性质

熔点 :>225°C (dec.)
沸点 :448.3±35.0 °C(Predicted)
密度 :1.506±0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :Soluble in DMSO (up to 25 mg/ml)
形态 :solid
酸度系数(pKa) :11.35±0.43(Predicted)
颜色 :Orange
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

N-(二苯并[B,D]呋喃-3-基)-5-硝基呋喃-2-甲酰胺性质、用途与生产工艺

简介 C-178 是干扰素基因刺激物 (STING) 的共价抑制剂。它与 STING 上的 Cys91 结合以阻断其棕榈酰化并阻止 TBK1 在 HEK293T 细胞中的募集和磷酸化。 C-178 (0.01-1.25 μM) 在 HEK293 细胞中选择性地降低 STING- 而不是 RIG-I- 或 TBK1- 介导的 IFN-β 报告基因活性。当以 0.5 μM 的浓度使用时，它还可以防止由环状 di-GMP、双链 DNA 和 LPS 诱导的骨髓衍生巨噬细胞 (BMDM) 中的 Ifnb1 表达增加。
生物活性 C-178是STING的共价抑制剂，与Cys91共价结合。
靶点
Target Value
STING
()

体外研究

C-178 targets the poorly characterized N-terminal portion of mmSTING that includes the transmembrane domains. Moreover, C-178 interferes with this process by inhibiting the palmitoylation of STING. C-178 does not appreciably affect STING responses in human cells.C-178 (0-1 μM; 1 hour) alone does not appreciably affect the gene expression profile of BMDMs. In addition, it inhibits the CMA-induced phosphorylation of TBK1.C-178 (1 μM; 1 hour) decreases cdG, dsDNA, CMA and LPS-induced Ifnb1 expression in mouse bone marrow-derived macrophages.C-178 (1 μM; 0.5-4 hours) inhibits the CMA-induced p-TBK1 and sting protein expression as a time-dependent manner in mouse embryonic fibroblasts.

Western Blot Analysis

Cell Line:	Mouse bone marrow-derived macrophages (BMDMs)
Concentration:	0 μM; 0.125 μM; 0.25 μM; 0.5 μM; 1 μM
Incubation Time:	1 hour
Result:	Inhibited CMA-induced p-TBK1 expression as a does dependent manner.