Necrostatin-1

别名: Nec-1

Necrostatin-1 (Nec-1)是一种特异性RIP1 (RIPK1)抑制剂,抑制TNF-α诱导的细胞坏死,在293T细胞中EC50为490 nM。Necrostatin-1也可抑制 IDO、细胞自噬和凋亡。

Necrostatin-1 Chemical Structure

Necrostatin-1 Chemical Structure

CAS: 4311-88-0

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1054.09 现货
10mg RMB 814.14 现货
100mg RMB 2224.79 现货
1g RMB 7944.3 现货
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批次: 纯度: 99.97%
99.83

Necrostatin-1相关产品

RIP kinase抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
L929 Growth Inhibition Assay 2/5 μg/ml  24 h reverses the cell growth inhibition and cell death induced by TNFα alone as well as TNFα + zVAD 23941769
L929 Function Assay 2 μg/ml  24 h promots caspase-6 (p20) activity and procaspase-6 cleavage 23941769
L929 Function Assay 5 μg/ml 24 h blocks zVAD induced necroptosis and autophagy 23941769
C6 Cell Viability Assay 1 mmol/L 3 h attenuates Shikonin induced glioma cell death 23840441
U87 Cell Viability Assay 1 mmol/L 3 h attenuates Shikonin induced glioma cell death 23840441
C6 Cytotoxicity Assay 1 mmol/L 3 h blocks shikonin induced necrosis 23840441
U87 Cytotoxicity Assay 1 mmol/L 3 h blocks shikonin induced necrosis 23840441
C6 Function Assay 1 mmol/L 1.5-3 h suppresses the expression of RIP-1 caused by shikonin 23840441
U87 Function Assay 1 mmol/L 1.5-3 h suppresses the expression of RIP-1 caused by shikonin 23840441
TE671 Cell Viability Assay 40 μg/ml  24 h rescues GX15-070-induced loss of cell viability 23744296
RMS13 Cell Viability Assay 40 μg/ml  24 h rescues GX15-070-induced loss of cell viability 23744296
MEFs Cytotoxicity Assay 2/6/20 μM 18 h inhibits TNFα-induced cell death in RelA KO MEFs 23727581
MEFs Function Assay 20 μM 1/2/4 h suppresses TNFα-induced RIPK1 phosphorylation 23727581
ΔN-Karpas 299  Cytotoxicity Assay 20 μM 16 h inhibits CD30-induced cell death 23545938
MM.1S  Cytotoxicity Assay 90 µM 1 h blocks BAY 11-7082 induced rapid cell swelling 23527154
KMS-12-BM Cytotoxicity Assay 90 µM 1 h blocks BAY 11-7082 induced rapid cell swelling 23527154
HT-22  Cell Viability Assay 10 μM 12 h protects against glutamate-induced cell death 23307752
HT-22  Function Assay 25 μM 0–30 min inhibits ERK Activation induced by glutamate 23307752
NIH3T3  Function Assay 10/50 μM 1/3 h ameliorates TNFα-driven complex formation 23261677
SH-EP Apoptosis Assay 10 μM  72 h  inhibits IAP inhibitor- and Lexatumumab-induced apoptosis 22890322
HL60 Apoptosis Assay 60 μM 12 h enhances shikonin-induced apoptosis 22837689
HL60/Adr Apoptosis Assay 60 μM 12 h enhances shikonin-induced apoptosis 22837689
K562 Apoptosis Assay 60 μM 12 h enhances shikonin-induced apoptosis 22837689
K562/Adr  Apoptosis Assay 60 μM 12 h enhances shikonin-induced apoptosis 22837689
HL60 Function Assay 60 μM 12 h augments the caspase-3 activity 22837689
HL60/Adr Function Assay 60 μM 12 h augments the caspase-3 activity 22837689
K562 Function Assay 60 μM 12 h augments the caspase-3 activity 22837689
K562/Adr  Function Assay 60 μM 12 h augments the caspase-3 activity 22837689
HL60 Function Assay 60 μM 12 h increases the activity of caspases, caspase 8 and 9 22837689
HL60/Adr Function Assay 60 μM 12 h increases the activity of caspases, caspase 8 and 9 22837689
K562 Function Assay 60 μM 12 h increases the activity of caspases, caspase 8 and 9 22837689
K562/Adr  Function Assay 60 μM 12 h increases the activity of caspases, caspase 8 and 9 22837689
L929sA Apoptosis Assay 10 μM 1 h inhibits the apoptotic response to TNF 22362767
L929sA Apoptosis Assay 10 μM 1 h rescues cells expressing RIPK1ΔID from TNF-induced apoptosis 22362767
L929sA Apoptosis Assay 10 μM 1 h abrogates the interaction of caspase-8 with FADD 22362767
TPC-1 Cell Viability Assay 100 μM 24 h increases cellular survival 22136818
8505c Cell Viability Assay 100 μM 24 h increases cellular survival 22136818
SW13 Cell Viability Assay 100 μM 24 h increases cellular survival 22136818
Jurkat  Cytotoxicity Assay 50/ 100/200 μm 1/3 h reduces Naegleria fowleri-induced cytotoxicity 21535020
Jurkat  Function Assay 200 μm 30 min reduces Naegleria fowleri-induced reactive oxygen species (ROS) generation 21535020
HT-22 Cytotoxicity Assay 10 μM 12 h protects against cell death induced by 5 mmol/L glutamate  17760869
L929 Function Assay 2/5 μg/ml  24 h reversed the autophagy induced by TNFα alone as well as TNFα + zVAD 23941769
NRK-52E  Cell Viability Assay 20 μM 24 h inhibits increased Drp1 protein expression after TNF-α Stimulation and ATP Depletion 24351845
NRK-52E  Cell Viability Assay 20 μM 24 h increases cell viability after TNF-α Stimulation and ATP Depletion 24351845
NRK-52E  Cell Viability Assay 20 μM 24 h protects cells from cell death caused by ischemia injury 24351845
AGS Cell Viability Assay 60 μm 1 h prevents shikonin-induced cell death 24463199
L-540  Cell Viability Assay 60 μm 1 h reduces the Givinostat/Sorafenib-induced cell death 24561519
L-540  Function Assay 60 μm 1 h prevents the mitochondrial membrane depolarization 24561519
L-540  Function Assay 60 μm 1 h prevents the generation of ROS 24561519
SK-Hep1 Function Assay 60 μM  18 h blocks β-lapachone-mediated PAR accumulation and AIF translocation to the cytosol  24832602
SK-Hep1 Function Assay 60 μM  18 h inhibits β-Lapachone-induced leakage of HMGB-1  24832602
SK-Hep1 Function Assay 60 μM  18 h blocks β-lapachone-induced morphological change, cell death and PI uptake 24832602
Huh7 Cell Viability Assay 50 µM 24/48 h prevents cell death of rAdHCV co-infected Huh7 cells 24973240
L929 Cell Viability Assay 30 μM 1 h inhibits TNF-α-induced cleavage of Topo I 25095742
L929 Cell Viability Assay 30 μM 1 h inhibits TNF-α-induced loss of cell viability 25095742
L929-A Function Assay 50 μM  12 h inhibits the TNFα-induced loss of mitochondrial membrane permeability 25398540
L929 Function Assay 50 μM  12 h inhibits TNFα-induced Bid cleavage 25398540
L929-N  Function Assay 50 μM  12 h blocks the cleavage of Caspase-3 and PARP 25398540
L929-A  Function Assay 50 μM  12 h blocks the cleavage of Caspase-3 and PARP 25398540
L929-N  Cell Viability Assay 50 μM  24 h blocks TNFα-induced cell death 25398540
L929-A  Cell Viability Assay 50 μM  24 h blocks TNFα-induced cell death 25398540
KMS-12-PE  Cell Viability Assay 60 μM 5 h inhibits SHK-induced cell death 25530098
SGC-7901 Cell Viability Assay 30 μM 1 h suppresses oxaliplatin-mediated cell death 25767076
BxPC-3 Function Assay 20 μM 24 h decreases the early necrotic cells 26000607
MiaPaCa-2 Function Assay 20 μM 24 h decreases the early necrotic cells 26000607
NCI-H28 Cell Viability Assay 10 μM 24 h prevents DAPE-induced reduction of NCI-H28 cell viability  26004138
BMDM  Function Assay 10 μM 30 min protects cells from TAKI-induced LDH release 26381601
MEFs  Cell Viability Assay 10 μM 48 h inhibits zVAD-promoted death of CNOT3-depleted MEFs 26437789
A549 Cell Viability Assay 50 μM 24 h inhibits MMS-induced cell death 26472723
Jurkat T Necroptosis assay 30 uM 24 hrs Inhibition of necroptosis in TNF-alpha-induced human Jurkat T cells assessed as cell viability at 30 uM after 24 hrs 18467094
L929 Necroptosis assay 30 uM 24 hrs Inhibition of necroptosis in zVAD-induced mouse L929 cells assessed as cell viability at 30 uM after 24 hrs 18467094
L929 Necroptosis assay 30 uM 24 hrs Inhibition of necroptosis in TNF-alpha-induced mouse L929 cells assessed as cell viability at 30 uM after 24 hrs 18467094
Jurkat Cytoprotective assay 30 uM 1 hr Cytoprotective activity against FasL-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by FasL stimulation measured after 20 hrs by Alamar blue assay 29541357
Jurkat Cytoprotective assay 30 uM 1 hr Cytoprotective activity against CHX-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by CHX stimulation by Alamar blue assay 29541357
Jurkat Cytoprotective assay 30 uM 1 hr Cytoprotective activity against Z-VAD-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by Z-VAD stimulation by Alamar blue assay 29541357
Jurkat Cytoprotective assay 30 uM 1 hr Cytoprotective activity against FasL-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by FasL stimulation measured after 20 hrs by phase contrast microscopy 29541357
Jurkat Cytoprotective assay 30 uM 1 hr Cytoprotective activity against CHX-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by CHX stimulation by phase contrast microscopy 29541357
Jurkat Cytoprotective assay 30 uM 1 hr Cytoprotective activity against Z-VAD-induced necroptosis in human Jurkat cells assessed as increase in cell viability at 30 uM incubated for 1 hr followed by Z-VAD stimulation by phase contrast microscopy 29541357
OHC Function Assay 300 μM increases the number of apoptotic OHCs without altering the levels of CC8 after noise exposure 24874734
OHC Function Assay 300 μM diminishes noise-induced AMPK activation 24874734
OHC Function Assay 300 μM results in a reduction of noise-induced RIP1 and RIP3 immunofluorescence 24874734
OHC Function Assay 300 μM decreases noise-induced swollen nuclei  24874734
OHC Function Assay 300 μM increases noise-induced condensed nuclei 24874734
Sf9 Function assay 30 mins Inhibition of recombinant human GST-fused RIPK1 (1 to 497 residues) expressed in baculovirus infected insect Sf9 cells in presence of 32P-gamma-ATP after 30 mins by autoradiogram-based Western blot method, IC50 = 0.182 μM. 28280261
3T3 Cell death assay 24 hrs Inhibition of death receptor signaling mediated necrotic cell death in mouse 3T3 cells assessed as cell viability after 24 hrs by ATP based viability assay in presence of TNFalpha and zVAD.fmk 16408008
3T3 Cell death assay 24 hrs Inhibition of death receptor signaling mediated necrotic cell death in mouse 3T3 cells assessed as cell viability after 24 hrs by ATP based viability assay in presence of FasL and zVAD.fmk 16408008
MEF Cell death assay 16 hrs Inhibition of death receptor signaling mediated necrotic cell death in SV40 transformed mouse MEF cells assessed as cell viability after 16 hrs by ATP based viability assay in presence of TNFalpha, CHX and zVAD.fmk 16408008
L929 Cell death assay 24 hrs Inhibition of death receptor signaling mediated necrotic cell death in mouse L929 cells assessed as cell viability after 24 hrs by ATP based viability assay in presence of TNFalpha 16408008
U937 Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human U937 cells assessed as cell viability after 48 hrs by ATP based viability assay in presence of TNFalpha and zVAD-fmk 16408008
3T3 Cell death assay 24 hrs Inhibition of death receptor signaling mediated necroptotic cell death in mouse 3T3 cells assessed as cell viability after 24 hrs by ATP based viability assay in presence of TNFalpha and zVAD-fmk 16408008
Jurkat Cell death assay 24 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD assessed as decreased levels of PE-conjugated LC3-II (autophagy marker) after 24 hrs by Western blot method in presence of TNFalpha 16408008
L929 Cell death assay 24 hrs Inhibition of death receptor signaling mediated necroptotic cell death in mouse L929 cells assessed as decreased levels of PE-conjugated autophagy marker LC3-II after 24 hrs by Western blot method in presence of TNFalpha 16408008
3T3 Cell death assay 24 hrs Inhibition of death receptor signaling mediated necroptotic cell death in mouse 3T3 cells assessed as decreased levels of PE-conjugated autophagy marker LC3-II after 24 hrs by Western blot method in presence of TNFalpha and zVAD-fmk 16408008
3T3 Cell death assay 24 hrs Inhibition of death receptor signaling mediated necroptotic cell death in mouse 3T3 cells assessed as decreased levels of PE-conjugated autophagy marker LC3-II after 24 hrs by Western blot method in presence of FasL and zVAD-fmk 16408008
3T3 Cell death assay 24 hrs Inhibition of death receptor signaling mediated necroptotic cell death in mouse 3T3 cells assessed as decreased levels of PE-conjugated autophagy marker LC3-II after 24 hrs by Western blot method in presence of rapamycin 16408008
Jurkat Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing FKBP12-based dimerization domain assessed as cell viability after 48 hrs by FACS in presence of AP1510, zVAD-fmk 16408008
Jurkat Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP kinase assessed as cell viability after 48 hrs by FACS in presence of AP1510, zVAD-fmk 16408008
Jurkat Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP K45M mutant assessed as cell viability after 48 hrs by FACS in presence of AP1510, zVAD-fmk 16408008
Jurkat Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP kinase domain assessed as cell viability after 48 hrs by FACS in presence of AP1510, zVAD-fmk 16408008
Jurkat Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing FKBP12-based dimerization domain assessed as cell viability after 48 hrs by FACS in presence of AP1510 16408008
Jurkat Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP kinase assessed as cell viability after 48 hrs by FACS in presence of AP1510 16408008
Jurkat Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP K45M mutant assessed as cell viability after 48 hrs by FACS in presence of AP1510 16408008
Jurkat Cell death assay 48 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cells deficient in FADD and expressing RIP kinase domain assessed as cell viability after 48 hrs by FACS in presence of AP1510 16408008
Jurkat T Necroptosis assay Inhibition of TNF-alpha-induced necroptosis in FADD-deficient human Jurkat T cells, EC50 = 0.05 μM. 18467094
Jurkat Function assay Inhibition of endogenous RIP1 autophosphorylation in human Jurkat cells, EC50 = 0.182 μM. 18408713
Jurkat T Necroptosis assay Effective concentration required for inhibition of necroptosis in FADD deficient Jurkat T cells treated with TNF-alpha, EC50 = 0.49 μM. 16153840
Jurkat Necroptosis assay Inhibition of cellular necroptosis in TNFalpha treated FADD deficient human Jurkat cells, EC50 = 0.49 μM. 18408713
IEC18 Cell death assay Inhibition of death receptor signaling mediated necrotic cell death in rat IEC18 cells assessed as cell viability in presence of TNFalpha and zVAD.fmk 16408008
HL60 Cell death assay Inhibition of death receptor signaling mediated necrotic cell death in human HL60 cells assessed as cell viability in presence of TNFalpha and zVAD.fmk 16408008
Jurkat Necrosis assay Inhibition of necrosis in human Jurkat cells assessed as nuclear condensation by bright field microscopy in presence of FasL, CHX and zVAD-fmk 16408008
Jurkat Necrosis assay Inhibition of necrosis in human Jurkat cells assessed as organelle swelling by bright field microscopy in presence of FasL, CHX and zVAD-fmk 16408008
Jurkat Necrosis assay Inhibition of necrosis in human Jurkat cells assessed as early loss of plasma membrane integrity by bright field microscopy in presence of FasL, CHX and zVAD-fmk 16408008
Jurkat Necrosis assay Inhibition of necrosis in human Jurkat cells assessed as appearance of translucent cytosol in presence of FasL, CHX and zVAD-fmk 16408008
Jurkat Necrosis assay Inhibition of necrosis in human Jurkat cells deficient in FADD assessed as inhibition of nuclear condensation by bright field microscopy in presence of TNFalpha 16408008
Jurkat Necrosis assay Inhibition of necrosis in human Jurkat cells deficient in FADD assessed as inhibition of organelle swelling by bright field microscopy in presence of TNFalpha 16408008
Jurkat Necrosis assay Inhibition of necrosis in human Jurkat cells deficient in FADD assessed as inhibition of early loss of plasma membrane integrity by bright field microscopy in presence of TNFalpha 16408008
Jurkat Necrosis assay Inhibition of necrosis in human Jurkat cells deficient in FADD assessed as inhibition of appearance of translucent cytosol in presence of TNFalpha 16408008
Sf9 Function assay Inhibition of human RIP1 K45M mutant autophosphorylation expressed in Sf9 cells 18408713
点击查看更多细胞系数据

生物活性

产品描述 Necrostatin-1 (Nec-1)是一种特异性RIP1 (RIPK1)抑制剂,抑制TNF-α诱导的细胞坏死,在293T细胞中EC50为490 nM。Necrostatin-1也可抑制 IDO、细胞自噬和凋亡。
特性 Necrostatin-1是抑制细胞坏死的有力工具。
靶点
RIP1 [1]
(293T cells)
490 nM(EC50)
体外研究(In Vitro)
体外研究活性

Necrostatin-1 (1-100 μM) 抑制过表达和内源性的RIP1发生自磷酸化。RIP1是初级细胞靶点,负责Necrostatin-1的抗细胞坏死活性。[1]

Necrostatin-1有效抑制多种类型细胞触发的坏死性细胞死亡。Necrostatin-1作为细胞坏死的小分子抑制剂, 作用于jurkat细胞,抑制RIP激酶的诱导细胞坏死,抑制TNF-α诱导的细胞坏死,EC50为490 nM。[2]

激酶实验 RIP1 激酶检测
RIP1 的磷酸化需要其激酶活性。FLAG标记的野生型(WT)或RIP1(K45M) 突变体失活激酶的表达结构转染到293T细胞中,在有[γ-32P]ATP存在时,RIP1激酶实验在30°C下进行30分钟。样品进行SDS-PAGE,通过放射自显影可观察到RIP1带。对放射性带的相对强度进行量化,并显示比率。在激酶反应的同时,珠样本使用anti-RIP1抗体进行Western Blot分析,确保与激酶反应中等量的蛋白。
细胞实验 细胞系 Jurkat, BALB/c 3T3, SV40-转化的MEF, L929
浓度 0.01-100 μM
孵育时间 --
方法

细胞接种在96孔板中(白色板进行发光检测;黑色板进行荧光检测;空白板进行MTT实验)贴壁细胞按每孔5000-10000个细胞的密度接种,悬浮细胞按每孔20,000-50,000个细胞的密度接种,孔中含100 μl合适的无酚红培养基。温育后,使用如下方法之一测定细胞存活率。ATP 实验中,使用购买的发光试剂盒,并使用Wallac Victor II酶标仪分析发光值。Sytox实验中,细胞与 1 μM Sytox Green试剂在37°C下温育30分钟,然后进行荧光读数。随后,增加5 μl 20% Triton X-100溶液到每孔中,产生最大溶解,细胞37°C下温育1小时,然后进行二次读数。Triton处理前和后,计算值的比率。MTT实验,使用CellTiter 96 AQueous 非放射性细胞增殖检测试剂盒。PI排除实验中, 加入2 μg/ml PI 到培养基中,立即使用FACSCalibur分析样品。PI-膜联蛋白V 实验中,使用ApoAlert Annexin V-EGFP 凋亡试剂盒。进行DioC6染色, 细胞与40 nM DiOC6 在37°C下温育30分钟, 洗涤一次,使用FACSCalibur分析。ROS分析中, 细胞与5 μM Dihydroethidium在37°C下温育30分钟, 洗涤一次,使用FACSCalibur分析。

实验图片 检测方法 检测指标 实验图片 PMID
Immunofluorescence RIP1 / RIP3 30462730

化学信息&溶解度

分子量 259.33 分子式

C13H13N3OS

CAS号 4311-88-0 SDF Download Necrostatin-1 SDF
Smiles CN1C(=O)C(NC1=S)CC2=CNC3=CC=CC=C32
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 57 mg/mL ( 219.79 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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