Home Epigenetics HDAC inhibitor Tubastatin A

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Tubastatin A HDAC inhibitor

Kat.-Nr.: S8049

Tububastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). This compound promotes autophagy and increases apoptosis.
Tubastatin A HDAC inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 335.4

Springe zu

Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.63%
99.63

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung 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
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Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 335.4 Formel

C20H21N3O2

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 1252003-15-8 SDF herunterladen Lagerung von Stammlösungen

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

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 16.7 mg/mL (49.79 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

Targets/IC50/Ki
HDAC6
(Cell-free assay)
15 nM
In vitro
Tubastatin A ist selektiv gegenüber allen Isozymen außer HDAC8 und behält eine über 1000-fache Selektivität gegenüber allen Isoformen außer HDAC8 bei, bei denen es eine etwa 57-fache Selektivität aufweist. Diese Verbindung induziert bevorzugt eine α-tubulin-Hyperacetylierung bei 2,5 μM. Eine leichte Induktion der Histon-Hyperacetylierung wird für diese Chemikalie bei 10 μM beobachtet. Es zeigt einen dosisabhängigen Schutz gegen durch Homocysteinsäure induzierten neuronalen Zelltod, beginnend bei 5 μM mit nahezu vollständigem Schutz bei 10 μM. Diese Verbindung (10 μM) induziert einen Anstieg des Spiegels an acetyliertem α-tubulin und die Wiederherstellung der Primärzilienexpression in den Cholangiokarzinom-Zelllinien (18-fach); die Wiederherstellung der Primärzilien korrelierte mit herunterregulierten Hedgehog (Hh)- und MAPK-Signalwegen sowie verringerten Zellproliferationsraten (im Durchschnitt um 50 %) und Invasion (um 40 %). Es zeigt eine signifikante Hemmung von TNF-α und IL-6 in LPS-stimulierten menschlichen THP-1-Makrophagen mit einem IC50 von 272 nM bzw. 712 nM. Dieser Inhibitor hemmt die Stickstoffmonoxid (NO)-Sekretion in murinen Raw 264.7-Makrophagen dosisabhängig mit einem IC50 von 4,2 μM.
Kinase-Assay
HDAC-Enzymtests
Tubastatin A wird in Assay-Puffer (50 mM HEPES, pH 7,4, 100 mM KCl, 0,001 % Tween-20, 0,05 % BSA und 20 μM Tris(2-carboxyethyl)phosphin) auf die 6-fache Endkonzentration gelöst und verdünnt. HDAC-Enzyme werden in Assay-Puffer auf die 1,5-fache Endkonzentration verdünnt und vor der Zugabe des Substrats für 10 Minuten mit dieser Verbindung vorinkubiert. Die Menge an FTS (HDAC1, HDAC2, HDAC3 und HDAC6) oder MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8 und HDAC9), die für jedes Enzym verwendet wird, entspricht der Michaelis-Konstante (Km), wie durch eine Titrationskurve bestimmt. FTS oder MAZ-1675 wird in Assay-Puffer auf die 6-fache Endkonzentration mit 0,3 μM Trypsin in Sequenzierqualität verdünnt. Die Substrat/Trypsin-Mischung wird zur Enzym/Verbindung-Mischung gegeben, die Platte wird für 60 Sekunden geschüttelt und dann in ein SpectraMax M5 Mikroplatten-Lesegerät gestellt. Die enzymatische Reaktion wird über 30 Minuten auf die Freisetzung von 7-Amino-4-methoxy-cumarin nach Deacetylierung der Lysin-Seitenkette im Peptid-Substrat überwacht und die lineare Rate der Reaktion wird berechnet.
In vivo
Tubastatin A reduziert das Wachstum von Cholangiokarzinomen in vivo. Diese Verbindung (10 mg/kg) induziert im syngenen orthotopen Rattenmodell für Cholangiokarzinome ein 6-fach geringeres mittleres Tumorgewicht sowie eine Verringerung der Verhältnisse von Tumorgewicht zu Lebergewicht bzw. Körpergewicht (5- bzw. 5,6-fach) und eine höhere Frequenz an cillierten Cholangiozyten im Vergleich zu den Kontrollen (29 % vs. 1,4 %). Es senkt die Anzahl der PCNA-positiven Zellen in den behandelten Tumoren im Vergleich zu den Vehikelkontrollen signifikant (34 % vs. 65 %). Diese Chemikalie zeigt bei 30 mg/kg i.p. eine signifikante Hemmung des Pfotenvolumens in einem durch Freund's complete adjuvant (FCA) induzierten Entzündungsmodell bei Tieren. Es (30 mg/kg i.p.) schwächt die klinischen Scores (~ 70 %) und die IL-6-Expression im Pfotengewebe der kollageninduzierten Arthritis bei DBA1-Mäusen signifikant ab.
Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/22262760/

Anwendungen (Applications)

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

Häufig gestellte Fragen (Frequently Asked Questions)

Frage 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?

Antwort:
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.

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

Antwort:
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.