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{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
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免费溶解
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 | The receptor-interacting serine/threonine protein kinase 1 (RIPK1) is a key mediator of regulated cell death and inflammation. RIPK1 inhibition would fundamentally improve the therapy of RIPK1-dependent organ damage in stroke, myocardial infarction, kidney failure, and systemic inflammatory response syndrome[1]. RIPK1 comprises an N-terminal kinase domain, an intermediate domain, and a C-terminal death domain, and the kinase domain is the direct target of Nec-1s[2]. Necrostatin-34 is a RIPK1 kinase inhibitor, stabilizing RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain. Nec-34 showed no significant inhibition against commercially available RIPK2, RIPK3,RIPK4 and RIPK5 at 10 μM, while the RIPK1 kinase activity was effectively blocked by Nec-34 at the same concentration in both biochemical and cellular assays. Nec-34 had no effect on the recruitment and ubiquitination of RIPK1 or the recruitment of TRADD, Sharpin or IKKα/β in complex I, whereas RIPK1 kinase activation, indicated by p-S166 RIPK1, was strongly blocked by Nec-34, as by Nec1s.Necrostatin-34 (10 μM) inhibits the dimerization-induced RIPK1 activation as examined by phosphorylation of Ser166 (p-S166) of RIPK1, a biomarker for RIPK1 activation. Necrostatin-34 may block TNFα-induced complex II formation by inhibiting the activation of RIPK1 kinase. Necrostatin-34 shows IC50 values of 667 nM and 134 nM for TNFα in FADD def-Jurkat cells and L939 cells, respectively. Nec-34 was about 10-fold more potent in inhibiting necroptosis of murine cells than that of human cells[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.60mL 0.52mL 0.26mL |
13.00mL 2.60mL 1.30mL |
26.01mL 5.20mL 2.60mL |
CAS号 | 375835-43-1 |
分子式 | C18H16N4O2S2 |
分子量 | 384.475 |
别名 | Nec-34 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 120 mg/mL(312.11 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 |