|5-(1H-吲哚-3-基甲基)-3-甲基-2-硫酮-4-咪唑烷酮|CsnPharm

CAS No.: 4311-88-0

Necrostatin-1 Catalog No. CSN11637

Synonyms: Nec-1

Necrostatin-1 is an inhibitor of RIP1 and can decrease TNF-α-induced necroptosis with EC50 of 490 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 RIP Kinase 1

EC50:490nM
描述Necroptosis is a non-apoptotic form of cell death that can be regulated by receptor-interacting protein kinases (RIPKs). Necrostatin 1 is a potent necroptosis inhibitor with an EC50 value of 494 nM. Necrostatin 1 at the dose of 30 μM efficiently inhibited the simultaneous loss of mitochondrial membrane potential and plasma membrane integrity in Jurkat cells treated with necrotic death stimuli. The treatment of 30 μM necrostatin 1 for 24 hours blocked the necroptotic LC3-II induction as well as the formation of autophagic vesicles in U937 cells. Necrostatin 1 at 1, 10, and 100 μM efficiently inhibited the autophosphorylation of overexpressed RPI1 in vitro at a dose-dependent fashion. The kinase activity of endogenous RIP1 was suppressed by necrostatin 1 at 3 and 30 μM. Necrostatin 1 also blocked the activity of recombinant RIP1 in vitro at 30 and 100 μM. In mice that were administrated with 4 mmol/l necrostatin 1 immediately before controlled cortical impact (CCI), the brain lesion size was significantly reduced by 30 – 40 % compared with mice pretreated with vehicle at 14 days. The recovery of motor function was also significantly improved in necrostatin 1-pretreated mice compared with mice received inactive analog or vehicle. However, mice administered with 4 mmol/l necrostatin 1 at 5 mins after CCI had wire grip performance similar to vehicle-treated mice. In the examination of cognitive function, mice administered with 4 mmol/l necrostatin-1 before CCI showed significantly improved latency to the hidden platform compared with vehicle- or inactive analog-treated mice. Compared with vehicle-administrated mice, mice treated with necrostatin-1 before CCI also showed reduced numbers of PI-positive cells at 6 h after CCI in the injured cortex and dentate gyrus brain regions. The brain neutrophil counts in the injured cortical brain regions were decreased by nearly 50% in necrostatin1-treated mice.
作用机制Necrostatin 1 is a small molecular that specifically and potently inhibits cell death caused by the stimulation of death-domain receptors in the presence of caspase inhibition. The inhibition of Necrostatin 1 on RIP1 activity was through the T-loop segment.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
8505c	100 μM	Cell Viability Assay	24 h	increases cellular survival	22136818
A549	50 μM	Cell Viability Assay	24 h	inhibits MMS-induced cell death	26472723
AGS	60 μm	Cell Viability Assay	1 h	prevents shikonin-induced cell death	24463199

更多
动物研究
剂量
Mice: 0.6 mg/kg - 1.65 mg/kg^[3] (i.v.), 6 mg/kg^[4] (i.v.)

给药途径
i.v.

动物研究
剂量	Mice: 0.6 mg/kg - 1.65 mg/kg^[3] (i.v.), 6 mg/kg^[4] (i.v.)
给药途径	i.v.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8561 mL
- 19.2807 mL
- 38.5614 mL
- 5 mM
- 0.7712 mL
- 3.8561 mL
- 7.7123 mL
- 10 mM
- 0.3856 mL
- 1.9281 mL
- 3.8561 mL

技术信息

CAS号

4311-88-0

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H13N3OS

运输

蓝冰

分子量

259.33

别名

Nec-1

溶解度

DMSO	50.0 mg/mL (192.8 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+45% PEG 300+water

10 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

8505c	100 μM	Cell Viability Assay	24 h	increases cellular survival	22136818
A549	50 μM	Cell Viability Assay	24 h	inhibits MMS-induced cell death	26472723
AGS	60 μm	Cell Viability Assay	1 h	prevents shikonin-induced cell death	24463199
BMDM	10 μM	Function Assay	30 min	protects cells from TAKI-induced LDH release	26381601
BxPC-3	20 μM	Function Assay	24 h	decreases the early necrotic cells	26000607
C6	1 mmol/L	Cell Viability Assay	3 h	attenuates Shikonin induced glioma cell death	23840441
C6	1 mmol/L	Cytotoxicity Assay	3 h	blocks shikonin induced necrosis	23840441
C6	1 mmol/L	Function Assay	1.5-3 h	suppresses the expression of RIP-1 caused by shikonin	23840441
HL60	60 μM	Apoptosis Assay	12 h	enhances shikonin-induced apoptosis	22837689
HL60	60 μM	Function Assay	12 h	augments the caspase-3 activity	22837689
HL60	60 μM	Function Assay	12 h	increases the activity of caspases, caspase 8 and 9	22837689
HL60/Adr	60 μM	Apoptosis Assay	12 h	enhances shikonin-induced apoptosis	22837689
HL60/Adr	60 μM	Function Assay	12 h	augments the caspase-3 activity	22837689
HL60/Adr	60 μM	Function Assay	12 h	increases the activity of caspases, caspase 8 and 9	22837689
HT-22	10 μM	Cell Viability Assay	12 h	protects against glutamate-induced cell death	23307752
HT-22	25 μM	Function Assay	0–30 min	inhibits ERK Activation induced by glutamate	23307752
HT-22	10 μM	Cytotoxicity Assay	12 h	protects against cell death induced by 5 mmol/L glutamate	17760869
Huh7	50 µM	Cell Viability Assay	24/48 h	prevents cell death of rAdHCV co-infected Huh7 cells	24973240
Jurkat	50/ 100/200 μm	Cytotoxicity Assay	1/3 h	reduces Naegleria fowleri-induced cytotoxicity	21535020
Jurkat	200 μm	Function Assay	30 min	reduces Naegleria fowleri-induced reactive oxygen species (ROS) generation	21535020
K562	60 μM	Apoptosis Assay	12 h	enhances shikonin-induced apoptosis	22837689
K562	60 μM	Function Assay	12 h	augments the caspase-3 activity	22837689
K562	60 μM	Function Assay	12 h	increases the activity of caspases, caspase 8 and 9	22837689
K562/Adr	60 μM	Apoptosis Assay	12 h	enhances shikonin-induced apoptosis	22837689
K562/Adr	60 μM	Function Assay	12 h	augments the caspase-3 activity	22837689
K562/Adr	60 μM	Function Assay	12 h	increases the activity of caspases, caspase 8 and 9	22837689
KMS-12-BM	90 µM	Cytotoxicity Assay	1 h	blocks BAY 11-7082 induced rapid cell swelling	23527154
KMS-12-PE	60 μM	Cell Viability Assay	5 h	inhibits SHK-induced cell death	25530098
L-540	60 μm	Function Assay	1 h	prevents the generation of ROS	24561519
L-540	60 μm	Function Assay	1 h	prevents the mitochondrial membrane depolarization	24561519
L-540	60 μm	Cell Viability Assay	1 h	reduces the Givinostat/Sorafenib-induced cell death	24561519
L929	50 μM	Function Assay	12 h	inhibits TNFα-induced Bid cleavage	25398540
L929	30 μM	Cell Viability Assay	1 h	inhibits TNF-α-induced loss of cell viability	25095742
L929	30 μM	Cell Viability Assay	1 h	inhibits TNF-α-induced cleavage of Topo I	25095742
L929	2/5 μg/ml	Function Assay	24 h	reversed the autophagy induced by TNFα alone as well as TNFα + zVAD	23941769
L929	2/5 μg/ml	Growth Inhibition Assay	24 h	reverses the cell growth inhibition and cell death induced by TNFα alone as well as TNFα + zVAD	23941769
L929	2 μg/ml	Function Assay	24 h	promots caspase-6 (p20) activity and procaspase-6 cleavage	23941769
L929	5 μg/ml	Function Assay	24 h	blocks zVAD induced necroptosis and autophagy	23941769
L929-A	50 μM	Cell Viability Assay	24 h	blocks TNFα-induced cell death	25398540
L929-A	50 μM	Function Assay	12 h	blocks the cleavage of Caspase-3 and PARP	25398540
L929-A	50 μM	Function Assay	12 h	inhibits the TNFα-induced loss of mitochondrial membrane permeability	25398540
L929-N	50 μM	Cell Viability Assay	24 h	blocks TNFα-induced cell death	25398540
L929-N	50 μM	Function Assay	12 h	blocks the cleavage of Caspase-3 and PARP	25398540
L929sA	10 μM	Apoptosis Assay	1 h	inhibits the apoptotic response to TNF	22362767
L929sA	10 μM	Apoptosis Assay	1 h	rescues cells expressing RIPK1ΔID from TNF-induced apoptosis	22362767
L929sA	10 μM	Apoptosis Assay	1 h	abrogates the interaction of caspase-8 with FADD	22362767
MEFs	10 μM	Cell Viability Assay	48 h	inhibits zVAD-promoted death of CNOT3-depleted MEFs	26437789
MEFs	2/6/20 μM	Cytotoxicity Assay	18 h	inhibits TNFα-induced cell death in RelA KO MEFs	23727581
MEFs	20 μM	Function Assay	1/2/4 h	suppresses TNFα-induced RIPK1 phosphorylation	23727581
MiaPaCa-2	20 μM	Function Assay	24 h	decreases the early necrotic cells	26000607
MM.1S	90 µM	Cytotoxicity Assay	1 h	blocks BAY 11-7082 induced rapid cell swelling	23527154
NCI-H28	10 μM	Cell Viability Assay	24 h	prevents DAPE-induced reduction of NCI-H28 cell viability	26004138
NIH3T3	10/50 μM	Function Assay	1/3 h	ameliorates TNFα-driven complex formation	23261677
NRK-52E	20 μM	Cell Viability Assay	24 h	protects cells from cell death caused by ischemia injury	24351845
NRK-52E	20 μM	Cell Viability Assay	24 h	increases cell viability after TNF-α Stimulation and ATP Depletion	24351845
NRK-52E	20 μM	Cell Viability Assay	24 h	inhibits increased Drp1 protein expression after TNF-α Stimulation and ATP Depletion	24351845
OHC	300 μM	Function Assay	-	increases noise-induced condensed nuclei	24874734
OHC	300 μM	Function Assay	-	decreases noise-induced swollen nuclei	24874734
OHC	300 μM	Function Assay	-	results in a reduction of noise-induced RIP1 and RIP3 immunofluorescence	24874734
OHC	300 μM	Function Assay	-	diminishes noise-induced AMPK activation	24874734
OHC	300 μM	Function Assay	-	increases the number of apoptotic OHCs without altering the levels of CC8 after noise exposure	24874734
RMS13	40 μg/ml	Cell Viability Assay	24 h	rescues GX15-070-induced loss of cell viability	23744296
SGC-7901	30 μM	Cell Viability Assay	1 h	suppresses oxaliplatin-mediated cell death	25767076
SH-EP	10 μM	Apoptosis Assay	72 h	inhibits IAP inhibitor- and Lexatumumab-induced apoptosis	22890322
SK-Hep1	60 μM	Function Assay	18 h	blocks β-lapachone-induced morphological change, cell death and PI uptake	24832602
SK-Hep1	60 μM	Function Assay	18 h	inhibits β-Lapachone-induced leakage of HMGB-1	24832602
SK-Hep1	60 μM	Function Assay	18 h	blocks β-lapachone-mediated PAR accumulation and AIF translocation to the cytosol	24832602
SW13	100 μM	Cell Viability Assay	24 h	increases cellular survival	22136818
TE671	40 μg/ml	Cell Viability Assay	24 h	rescues GX15-070-induced loss of cell viability	23744296
TPC-1	100 μM	Cell Viability Assay	24 h	increases cellular survival	22136818
U87	1 mmol/L	Cell Viability Assay	3 h	attenuates Shikonin induced glioma cell death	23840441
U87	1 mmol/L	Cytotoxicity Assay	3 h	blocks shikonin induced necrosis	23840441
U87	1 mmol/L	Function Assay	1.5-3 h	suppresses the expression of RIP-1 caused by shikonin	23840441
ΔN-Karpas 299	20 μM	Cytotoxicity Assay	16 h	inhibits CD30-induced cell death	23545938

Necrostatin-1 Catalog No. CSN11637

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