Home Epigenetics HDAC remmer Tubastatin A

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Tubastatin A HDAC remmer

Cat.Nr.S8049

Tububastatin A is een potente en selectieve HDAC6-remmer met een IC50 van 15 nM in een celvrije test. Het is selectief tegen alle andere isozymen (1000-voudig) behalve HDAC8 (57-voudig). Deze verbinding bevordert autophagy en verhoogt apoptosis.
Tubastatin A HDAC remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 335.4

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Kwaliteitscontrole

Batch: Zuiverheid: 99.63%
99.63

Celkweek, behandeling & werkconcentratie

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving PMID
Sf9 Function assay 2 hrs Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay, IC50 = 0.0035 μM. 27541357
Sf9 Function assay Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate by fluorescence assay, IC50 = 0.011 μM. 27541357
Sf9 Function assay 30 mins Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 0.013 μM. 29549837
Sf9 Function assay 90 mins Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using RHKK(Ac) as substrate after 90 mins by fluorimetric method, IC50 = 0.0137 μM. 28038324
Sf9 Function assay 2 hrs Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 0.015 μM. 23009203
Sf9 Function assay Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.015 μM. 23905680
Sf9 Function assay 90 mins Inhibition of human recombinant N-terminal GST-tagged full length HDAC6 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay, IC50 = 0.0304 μM. 30092367
HeLaS3 Function assay 15 mins Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 0.031 μM. 28337317
insect cells Function assay 4 hrs Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using BATCP as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0349 μM. 27650925
SHSY5Y Function assay 8 hrs Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0943 μM. 27650925
SHSY5Y Function assay 8 hrs Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.1221 μM. 27650925
Sf9 Function assay 4 hrs Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 4 hrs fluorescence assay, IC50 = 0.718 μM. 29549837
Sf9 Function assay Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate, IC50 = 0.854 μM. 23905680
Sf9 Function assay 1 hr Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 1 hr fluorescence assay, IC50 = 0.967 μM. 29549837
SHSY5Y Function assay 8 hrs Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 1.1097 μM. 27650925
Sf9 Function assay 30 mins Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 1.54 μM. 29549837
Sf9 Function assay 90 mins Inhibition of human recombinant C-terminal His/FLAG-tagged full length HDAC1 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay, IC50 = 1.91 μM. 30092367
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2 μM. 27541357
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells, IC50 = 2 μM. 29945795
Sf9 Function assay 30 mins Inhibition of full length human recombinant C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (95 to 489 residues) expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 2.26 μM. 29549837
HeLa Function assay 6 hrs Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay, IC50 = 2.5 μM. 25454270
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
HeLaS3 Function assay 15 mins Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 2.7 μM. 28337317
HeLaS3 Function assay 15 mins Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 2.9 μM. 28337317
Jurkat Cytotoxicity assay 72 hrs Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 3.38 μM. 24304348
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 3.7 μM. 27541357
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, IC50 = 3.7 μM. 29945795
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
HeLaS3 Function assay 15 mins Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 3.9 μM. 28337317
CAL27 Antiproliferative assay 72 hrs Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay, IC50 = 4.6 μM. 28581289
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 8.6 μM. 27541357
PC3 Antiproliferative assay Antiproliferative activity against human PC3 cells, IC50 = 8.6 μM. 29945795
Sf9 Function assay 30 mins Inhibition of full length human recombinant C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 9.97 μM. 29549837
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. 27541357
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells, IC50 = 10.4 μM. 29945795
Cal27CisR Antiproliferative assay 72 hrs Antiproliferative activity against human Cal27CisR cells measured after 72 hrs by MTT assay, IC50 = 10.8 μM. 28581289
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 10.88 μM. 24304348
Cal27CisR Function assay 18 hrs Inhibition of HDAC in human Cal27CisR cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 12.1 μM. 28581289
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by MTS assay, IC50 = 14.81 μM. 25899338
THLE2 Cytotoxicity assay 72 hrs Cytotoxicity against human THLE2 cells after 72 hrs by vialight cell proliferation assay, LC50 = 15.1 μM. 29549837
CAL27 Function assay 18 hrs Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 16.1 μM. 28581289
Sf9 Function assay 2 hrs Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 16.4 μM. 23009203
Sf9 Function assay Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 16.4 μM. 23905680
B16 Growth inhibition assay 48 hrs Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay, GI50 = 40.5 μM. 23009203
KB Function assay 14 uM 24 hrs Inhibition of HDAC1 in human KB cells assessed as increase in histone H4 acetylation at 14 uM after 24 hrs by Western blotting analysis 25899338
KMS-12-BM Function assay 15 uM up to 48 hrs Inhibition of HDAC6 in human KMS-12-BM cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method 27541357
MOLM14 Function assay 15 uM up to 48 hrs Inhibition of HDAC6 in human MOLM14 cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method 27541357
U937 Function assay 2 uM 18 hrs Inhibition of HDAC6 in human U937 cells assessed as increase in alpha-tubulin acetylation at Lys-40 residue at 2 uM after 18 hrs by Western blot method 28337317
LNCAP Function assay 24 hrs Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation measured after 24 hrs relative to control 27717544
human Function assay 24 hrs Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced AR protein level measured after 24 hrs relative to control 27717544
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
HEL Cell cycle assay 1 to 5 uM 48 hrs Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 5 uM after 48 hrs propidium iodide staining based flow cytometry 29940115
HeLa Function assay 2 uM 12 hrs Inhibition of HDAC6 in human HeLa cells assessed as increase in acetyl-tubulin level at 2 uM after 12 hrs by Western blot analysis 29533873
HEK293 Function assay 10 uM 24 hrs Inhibition of HDAC1 in HEK293 cells assessed as increase in histone H3 acetylation at 10 uM after 24 hrs by Western blot method 28523102
MV4-11 Function assay 200 nM 24 hrs Inhibition of HDAC6 in human MV4-11 cells assessed as accumulation of acetylated alpha-tubulin at 200 nM after 24 hrs by Western blot analysis 29738953
HCT116 Cell cycle assay 5 uM 48 hrs Cell cycle arrest in human HCT116 cells assessed as accumulation at sub-G1 phase at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric method 28038324
PC12 Neuroprotective assay 10 uM 24 hrs Neuroprotective activity against H2O2-induced toxicity in rat PC12 cells assessed as cell viability at 10 uM pretreated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by MTT assay relative to control 30385227
PC12 Neuroprotective assay 5 uM 24 hrs Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay 30385227
PC12 Neuroprotective assay 10 uM 24 hrs Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay 30385227
PC12 Cytoprotective assay 24 hrs Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based fluorescence analysis 30385227
PC12 Cytoprotective assay 24 hrs Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based inverted fluorescence microscopic analysis 30385227
PC12 Neuroprotective assay 5 to 10 uM 24 hrs Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 to 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs coincubated with ebselen by MTT assay 30385227
PC12 Antioxidant assay 5 uM 24 hrs Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by DCFH-DA dye-based fluorescence analysis 30385227
PC12 Antioxidant assay 5 uM 24 hrs Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs coincubated with ebselen by DCFH-DA dye-based fluore 30385227
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht 335.4 Formule

C20H21N3O2

 Opslag (Vanaf de ontvangstdatum)
CAS-nr. 1252003-15-8 SDF downloaden Opslag van stamoplossingen

Synoniemen N/A Smiles CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO

Oplosbaarheid

In vitro
Batch:

DMSO : 16.7 mg/mL (49.79 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa Concentratie Volume Moleculair gewicht
Verdunningscalculator Moleculair gewicht calculator

In vivo
Batch:

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC50/Ki
HDAC6
(Cell-free assay)
15 nM
In vitro
Tubastatin A is selectief voor alle isozymen behalve HDAC8 en behoudt een meer dan 1000-voudige selectiviteit tegen alle isovormen met uitzondering van HDAC8, waar het ongeveer 57-voudige selectiviteit heeft. Deze verbinding induceert bij voorkeur α-tubuline hyperacetylatie bij 2,5 μM. Lichte inductie van histonhyperacetylatie wordt waargenomen voor deze chemische stof bij 10 μM. Het vertoont dosisafhankelijke bescherming tegen door homocysteïnezuur geïnduceerde neuronale celdood, beginnend bij 5 μM met bijna volledige bescherming bij 10 μM. Deze verbinding (10 μM) induceert een toename van geacetyleerde-α-tubulineniveaus en het herstel van primaire cilia-expressie in de cholangiocarcinoom-cellijnen (18-voudig); en het herstel van primaire cilia correleerde met neerwaarts gereguleerde Hedgehog (Hh) en MAPK signaalwegen, evenals verminderde celproliferatiesnelheden (gemiddeld met 50%) en invasie (met 40%). Het vertoont significante remming van TNF-α en IL-6 in LPS gestimuleerde humane THP-1 macrofagen met een IC50 van 272 nM en 712 nM. Deze remmer remt de secretie van stikstofmonoxide (NO) in murine Raw 264.7 macrofagen dosisafhankelijk met een IC50 van 4,2 μM.
Kinase Assay
HDAC enzymatische assays
Tubastatin A wordt opgelost en verdund in assaybuffer (50 mM HEPES, pH 7,4, 100 mM KCl, 0,001% Tween-20, 0,05% BSA en 20 μM tris(2-carboxyethyl)fosfine) tot 6-voudig van de eindconcentratie. HDAC-enzymen worden verdund tot 1,5-voudig van de eindconcentratie in assaybuffer en 10 minuten gepre-incubeerd met deze verbinding vóór de toevoeging van het substraat. De hoeveelheid FTS (HDAC1, HDAC2, HDAC3 en HDAC6) of MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8 en HDAC9) gebruikt voor elk enzym is gelijk aan de Michaelisconstante (Km), zoals bepaald door een titratiecurve. FTS of MAZ-1675 wordt verdund in assaybuffer tot 6-voudig de eindconcentratie met 0,3 μM sequensing-grade trypsine. Het substraat/trypsine-mengsel wordt toegevoegd aan het enzym/verbinding-mengsel en de plaat wordt 60 seconden geschud en vervolgens in een SpectraMax M5 microtiterplaatlezer geplaatst. De enzymatische reactie wordt gedurende 30 minuten gevolgd op de afgifte van 7-amino-4-methoxy-coumarine, na de deacetylation van de lysine-zijketen in het peptidesubstraat, en de lineaire snelheid van de reactie wordt berekend.
In vivo
Tubastatin A vermindert de groei van cholangiocarcinoom in vivo. Deze verbinding (10 mg/kg) induceert een 6-voudig lager gemiddeld tumorgewicht in een syngene rat orthotopisch model van cholangiocarcinoom, en vermindering van de verhoudingen van tumorgewicht tot levergewicht en lichaamsgewicht (respectievelijk 5- en 5,6-voudig), evenals een hogere frequentie van gecilieerde cholangiocyten vergeleken met controles (29% vs 1,4%). Het vermindert significant het aantal PCNA-positieve cellen in de behandelde tumoren vergeleken met voertuigcontroles (34% vs 65%). Deze chemische stof vertoont significante remming van het pootvolume bij 30 mg/kg i.p. in een door Freund's complete adjuvans (FCA) geïnduceerd diermodel van ontsteking. Het (30 mg/kg i.p.) vermindert significant klinische scores (~ 70%), en IL-6 expressie in pootweefsels van collageen-geïnduceerde artritis DBA1 muizen.
Referenties
  • [4] https://pubmed.ncbi.nlm.nih.gov/22262760/

Toepassingen

Methoden Biomarkers Afbeeldingen PMID
Western blot EGFR / p-AKT / AKT / p-ERK / ERK
S8049-WB1
29665050
Immunofluorescence α-tubulin / Acetylated tubulin HDAC6
S8049-IF1
23798680

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Veelgestelde vragen

Vraag 1:
We are planning to order some, but I found out there are two versions of it. One has HCl and one does not. Which one do you recommend for live cell use? Will the HCl containing version significantly change the pH?

Antwoord:
S8049 and S2627 have the same molecular structure. The only difference is S2627 containing HCl and has higher solubility in DMSO (74 mg/mL vs. S8049 9 mg/mL). Since they are the same molecule, its biological function should be similar. I would recommend to use S2627 for cell culture study.

Vraag 2:
What vehicle do you recommend to dissolve it for in vivo experiments?

Antwoord:
It can be dissolved in 2% DMSO/30% PEG 300/PBS at 2.5 mg/mL as a clear solution, and is also a clear solution in 2% DMSO/ corn oil at 2.5 mg/mL. This compound in 2% DMSO/0.5% Tween 80/PBS is a homogeneous suspension at 2.5 mg/mL at first. After stay for a while, the precipitation goes out at the bottom of the tube.