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Necrostatin-1 (Nec-1) Inhibidor de RIPK1

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

Cat. No.S8037

Necrostatin-1 (Nec-1) es un inhibidor específico de RIP1 (RIPK1) e inhibe la necroptosis inducida por TNF-α con un EC50 de 490 nM en células 293T. Necrostatin-1 también bloquea IDO y suprime la autophagy y la apoptosis.

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

Estructura química

Peso molecular: 259.33

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Control de calidad

Lote: Pureza: 99.97%

99.97

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

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	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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Información química, almacenamiento y estabilidad

Peso molecular	259.33	Fórmula	C₁₃H₁₃N₃OS	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	4311-88-0	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	Nec-1			Smiles	CN1C(=O)C(NC1=S)CC2=CNC3=CC=CC=C32

Solubilidad

In vitro
Lote:

DMSO : 57 mg/mL (219.79 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Características	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	Necrostatin-1 (1-100 μM) inhibe la autofosforilación de RIP1 sobreexpresada y endógena. Se ha encontrado que RIP1 es el objetivo celular primario responsable de la actividad antinecroptosis de este compuesto. Este químico suprime eficientemente la muerte celular necroptótica desencadenada por una variedad de estímulos en una variedad de tipos celulares. Previamente identificado como un inhibidor de moléculas pequeñas de la necroptosis, inhibe la necroptosis inducida por RIP kinase e inhibe la necroptosis inducida por TNF-α en células Jurkat con una EC50 de 490 nM.
Ensayo de quinasa	Ensayo de quinasa RIP1
Ensayo de quinasa	La fosforilación de RIP1 requiere su actividad quinasa. Se transfectan construcciones de expresión de RIP1 de tipo salvaje (WT) marcado con FLAG o un mutante puntual inactivo de quinasa de RIP1 (K45M) en células 293T y se realiza el ensayo de quinasa RIP1 como se describe en los Métodos en presencia de [γ-³²P]ATP durante 30 min a 30℃. Las muestras se someten a SDS-PAGE y la banda RIP1 se visualiza mediante autorradiografía. Las intensidades relativas de las bandas radiactivas se cuantifican y se muestran (proporción) en este y todos los demás autorradiogramas. Paralelamente a las reacciones de quinasa, una muestra de perlas se somete a análisis de Western blot utilizando un anticuerpo anti-RIP1 para asegurar cantidades iguales de proteínas en las reacciones de quinasa.
In vivo	Necrostatin-1 (Nec-1) es un inhibidor de molécula pequeña específico de la quinasa 1 (RIPK1) que interactúa con el receptor y que inhibe específicamente la fosforilación de este compuesto.
Referencias	[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/

Aplicaciones

Métodos	Biomarcadores	Imágenes	PMID
Immunofluorescence	RIP1 / RIP3		30462730

Soporte técnico

Instrucciones de manipulación

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