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Necrostatin-1 (Nec-1) Inhibiteur de RIPK1

Name: Necrostatin-1 (Nec-1)
Brand: Selleck Chemicals
SKU: S8037
Rating: 5 (317 reviews)

N° Cat.S8037

Necrostatin-1 (Nec-1) est un inhibiteur spécifique de RIP1 (RIPK1) et inhibe la nécroptose induite par le TNF-α avec une EC50 de 490 nM dans les cellules 293T. Necrostatin-1 bloque également IDO et supprime l'autophagy et l'apoptosis.

Necrostatin-1 (Nec-1) RIP kinase inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 259.33

Aller à

Contrôle qualité

Lot : Pureté : 99.97%

99.97

Cibles apparentées	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Autre RIP kinase Inhibiteurs	Necrostatin 2 racemate (Nec-1s) GSK872 Mito-TEMPO GSK'963 RIPA-56 GSK2982772 Resibufogenin GSK583 HS-1371 GSK2983559 (compound 3)

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Formulation	Description de lactivité	PMID
HT-22	Cytotoxicity Assay	10 μM	12 h		protects against cell death induced by 5 mmol/L glutamate	17760869
Jurkat	Function Assay	200 μm	30 min		reduces Naegleria fowleri-induced reactive oxygen species (ROS) generation	21535020
Jurkat	Cytotoxicity Assay	50/ 100/200 μm	1/3 h		reduces Naegleria fowleri-induced cytotoxicity	21535020
SW13	Cell Viability Assay	100 μM	24 h	DMSO	increases cellular survival	22136818
8505c	Cell Viability Assay	100 μM	24 h	DMSO	increases cellular survival	22136818
TPC-1	Cell Viability Assay	100 μM	24 h	DMSO	increases cellular survival	22136818
L929sA	Apoptosis Assay	10 μM	1 h		abrogates the interaction of caspase-8 with FADD	22362767
L929sA	Apoptosis Assay	10 μM	1 h		rescues cells expressing RIPK1ΔID from TNF-induced apoptosis	22362767
L929sA	Apoptosis Assay	10 μM	1 h		inhibits the apoptotic response to TNF	22362767
K562/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
HL60/Adr	Function Assay	60 μM	12 h		increases the activity of caspases, caspase 8 and 9	22837689
HL60	Function Assay	60 μM	12 h		increases the activity of caspases, caspase 8 and 9	22837689
K562/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
HL60/Adr	Function Assay	60 μM	12 h		augments the caspase-3 activity	22837689
HL60	Function Assay	60 μM	12 h		augments the caspase-3 activity	22837689
K562/Adr	Apoptosis Assay	60 μM	12 h		enhances shikonin-induced apoptosis	22837689
K562	Apoptosis Assay	60 μM	12 h		enhances shikonin-induced apoptosis	22837689
HL60/Adr	Apoptosis Assay	60 μM	12 h		enhances shikonin-induced apoptosis	22837689
HL60	Apoptosis Assay	60 μM	12 h		enhances shikonin-induced apoptosis	22837689
SH-EP	Apoptosis Assay	10 μM	72 h		inhibits IAP inhibitor- and Lexatumumab-induced apoptosis	22890322
NIH3T3	Function Assay	10/50 μM	1/3 h		ameliorates TNFα-driven complex formation	23261677
HT-22	Function Assay	25 μM	0–30 min	DMSO	inhibits ERK Activation induced by glutamate	23307752
HT-22	Cell Viability Assay	10 μM	12 h	DMSO	protects against glutamate-induced cell death	23307752
KMS-12-BM	Cytotoxicity Assay	90 µM	1 h		blocks BAY 11-7082 induced rapid cell swelling	23527154
MM.1S	Cytotoxicity Assay	90 µM	1 h		blocks BAY 11-7082 induced rapid cell swelling	23527154
ΔN-Karpas 299	Cytotoxicity Assay	20 μM	16 h		inhibits CD30-induced cell death	23545938
MEFs	Function Assay	20 μM	1/2/4 h		suppresses TNFα-induced RIPK1 phosphorylation	23727581
MEFs	Cytotoxicity Assay	2/6/20 μM	18 h		inhibits TNFα-induced cell death in RelA KO MEFs	23727581
RMS13	Cell Viability Assay	40 μg/ml	24 h		rescues GX15-070-induced loss of cell viability	23744296
TE671	Cell Viability Assay	40 μg/ml	24 h		rescues GX15-070-induced loss of cell viability	23744296
U87	Function Assay	1 mmol/L	1.5-3 h		suppresses the expression of RIP-1 caused by shikonin	23840441
C6	Function Assay	1 mmol/L	1.5-3 h		suppresses the expression of RIP-1 caused by shikonin	23840441
U87	Cytotoxicity Assay	1 mmol/L	3 h		blocks shikonin induced necrosis	23840441
C6	Cytotoxicity Assay	1 mmol/L	3 h		blocks shikonin induced necrosis	23840441
U87	Cell Viability Assay	1 mmol/L	3 h		attenuates Shikonin induced glioma cell death	23840441
C6	Cell Viability Assay	1 mmol/L	3 h		attenuates Shikonin induced glioma cell death	23840441
L929	Function Assay	5 μg/ml	24 h		blocks zVAD induced necroptosis and autophagy	23941769
L929	Function Assay	2 μg/ml	24 h		promots caspase-6 (p20) activity and procaspase-6 cleavage	23941769
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	2/5 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
OHC	Function Assay	300 μM		DMSO	increases the number of apoptotic OHCs without altering the levels of CC8 after noise exposure	24874734
OHC	Function Assay	300 μM		DMSO	diminishes noise-induced AMPK activation	24874734
OHC	Function Assay	300 μM		DMSO	results in a reduction of noise-induced RIP1 and RIP3 immunofluorescence	24874734
OHC	Function Assay	300 μM		DMSO	decreases noise-induced swollen nuclei	24874734
OHC	Function Assay	300 μM		DMSO	increases noise-induced condensed nuclei	24874734
Huh7	Cell Viability Assay	50 µM	24/48 h	DMSO	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	DMSO	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				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
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
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
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
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
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
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
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
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
Sf9	Function assay				Inhibition of human RIP1 K45M mutant autophosphorylation expressed in Sf9 cells	18408713
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
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Informations chimiques, stockage et stabilité

Poids moléculaire	259.33	Formule	C₁₃H₁₃N₃OS	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	4311-88-0	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	Nec-1			Smiles	CN1C(=O)C(NC1=S)CC2=CNC3=CC=CC=C32

Solubilité

In vitro
Lot:

DMSO : 57 mg/mL (219.79 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	2.850mg/ml (10.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 57 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 10%PEG 300 2 85 %ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.200mg/ml (4.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clarified DMSO stock solution to 100 μL of PEG300, mix evenly to clarify it; add 850 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Fonctionnalités	A powerful tool for characterizing the role of necroptosis with characterized primary target.
Targets/IC₅₀/Ki	IDO RIP1 (293T cells) 490 nM(EC50)
In vitro	La Necrostatin-1 (1-100 μM) inhibe l'autophosphorylation de RIP1 surexprimée et endogène. Il est constaté que RIP1 est la cible cellulaire primaire responsable de l'activité antinécroptose de ce composé. Ce produit chimique supprime efficacement la mort cellulaire nécroptotique déclenchée par une série de stimuli dans une variété de types cellulaires. Il, précédemment identifié comme un inhibiteur de petite molécule de nécroptose, inhibe la nécroptose induite par RIP kinase et inhibe la nécroptose induite par TNF-α dans les cellules Jurkat avec une EC50 de 490 nM.
Kinase Assay	Essai kinase RIP1
Kinase Assay	La phosphorylation de RIP1 nécessite son activité kinase. Des constructions d'expression de RIP1 de type sauvage (WT) marqué FLAG ou d'un mutant ponctuel inactif de la kinase de RIP1 (K45M) sont transfectées dans des cellules 293T et l'essai kinase RIP1 est réalisé comme décrit dans les méthodes en présence de [γ-³²P]ATP pendant 30 min à 30℃. Les échantillons sont soumis à un SDS-PAGE et la bande RIP1 est visualisée par autoradiographie. Les intensités relatives des bandes radioactives sont quantifiées et sont montrées (rapport) dans cette autoradiographie et toutes les autres. Parallèlement aux réactions de kinase, un échantillon de billes est soumis à une analyse par Western blot en utilisant un anticorps anti-RIP1 pour assurer des quantités de protéines égales dans les réactions de kinase.
In vivo	La Necrostatin-1 (Nec-1) est un inhibiteur spécifique de petite molécule de la protéine kinase 1 interagissant avec le récepteur (RIPK1) qui inhibe spécifiquement la phosphorylation de ce composé.
Références	[1] http://www.ncbi.nlm.nih.gov/pubmed/?term=18408713 [2] http://www.ncbi.nlm.nih.gov/pubmed/?term=16408008 [3] https://pubmed.ncbi.nlm.nih.gov/30542285/

Applications

Méthodes	Biomarqueurs	Images	PMID
Immunofluorescence	RIP1 / RIP3		30462730

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

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