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Necrostatin-1 (Nec-1) Inibitore di RIPK1

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

N. Cat.S8037

Necrostatin-1 (Nec-1) è un inibitore specifico di RIP1 (RIPK1) e inibisce la necroptosi indotta da TNF-α con un EC50 di 490 nM in cellule 293T. Necrostatin-1 blocca anche IDO e sopprime l'Autophagy e l'Apoptosis.

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

Struttura chimica

Peso molecolare: 259.33

Vai a

Controllo Qualità

Lotto: Purezza: 99.97%

99.97

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

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dellattività	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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Informazioni chimiche, conservazione e stabilità

Peso molecolare	259.33	Formula	C₁₃H₁₃N₃OS	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	4311-88-0	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	Nec-1			Smiles	CN1C(=O)C(NC1=S)CC2=CNC3=CC=CC=C32

Solubilità

In vitro
Lotto:

DMSO : 57 mg/mL (219.79 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Caratteristiche	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) inibisce l'autofosforilazione di RIP1 sovraespresso ed endogeno. Si è riscontrato che RIP1 è il bersaglio cellulare primario responsabile dell'attività antinecroptotica di questo composto. Questa sostanza chimica sopprime efficacemente la morte cellulare necroptotica innescata da una serie di stimoli in una varietà di tipi cellulari. Essa, precedentemente identificata come inibitore a piccole molecole della necroptosi, inibisce la necroptosi indotta dalla RIP kinase e inibisce la necroptosi indotta da TNF-α nelle cellule Jurkat con una EC50 di 490 nM.
Saggio chinasico	Saggio della chinasi RIP1
Saggio chinasico	La fosforilazione di RIP1 richiede la sua attività chinasica. Costrutti di espressione di RIP1 wild-type (WT) taggato FLAG o di un mutante puntiforme chinasico inattivo di RIP1 (K45M) vengono trasfettati in cellule 293T e il saggio della chinasi RIP1 viene eseguito come descritto nei Metodi in presenza di [γ-³²P]ATP per 30 min a 30℃. I campioni vengono sottoposti a SDS-PAGE e la banda RIP1 viene visualizzata mediante autoradiografia. Le intensità relative delle bande radioattive vengono quantificate e mostrate (rapporto) in questo e in tutti gli altri autoradiogrammi. Parallelamente alle reazioni chinasiche, un campione di perle viene sottoposto ad analisi Western blot utilizzando un anticorpo anti-RIP1 per garantire quantità uguali di proteine nelle reazioni chinasiche.
In vivo	Necrostatin-1 (Nec-1) è un inibitore specifico a piccole molecole della proteina chinasi 1 (RIPK1) interagente con il recettore che inibisce specificamente la fosforilazione di questo composto.
Riferimenti	[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/

Applicazioni

Metodi	Biomarcatori	Immagini	PMID
Immunofluorescence	RIP1 / RIP3		30462730

Supporto tecnico

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