Tubastatin A

Name: Tubastatin A
Brand: MedChemExpress
SKU: HY-13271A
Rating: 5.0 (38 reviews)

Cat. No.: HY-13271A Purity: 99.07%: Data Sheet
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Tubastatin A is a potent and selective HDAC6 inhibitor with an IC₅₀ of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).

For research use only. We do not sell to patients.

Tubastatin A Chemical Structure

CAS No. : 1252003-15-8

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Customer Review

Based on 38 publication(s) in Google Scholar

Other Forms of Tubastatin A:

34 Publications Citing Use of MCE Tubastatin A

RT-PCR

: Tubastatin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Oct 21;13(10):888. [Abstract]; Construction of HCT116 cell line with stable HDAC6 knockdown. Tubastatin A HCl is HDAC6 selective inhibitor.

: Tubastatin A purchased from MedChemExpress. Usage Cited in: J Nutr. 2020 Jul 1;150(7):1790-1798. [Abstract]; Effects of TBSA (Tubastatin A) pretreatment on glucose-induced changes in mRNA amounts of genes in IECs of yellow catfish.

: Tubastatin A purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Feb 1:9:34. [Abstract]; HDAC6 inhibition with Tubastatin A acetylates TFEB, facilitates TFEB nuclear translocation and attenuates programmed cell death in NRK-52E cells. Immunoblotting for acetylated α-tubulin in NRK-52E cells treated with Tubastatin A.

: Tubastatin A purchased from MedChemExpress. Usage Cited in: Medical Science, University of Toronto. 2017 Nov.; Tubastatin A induces a dose-dependent increase in acetylated α-tubulin levels in NRK-52E cells.

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Metallo-β-lactamase

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Protocol
Purity & Documentation
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Description

IC₅₀ & Target^[1]

HDAC6

15 nM (IC₅₀)

HDAC8

854 nM (IC₅₀)

HDAC1

16400 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
697	IC₅₀	2006 nM Compound: Tubastatin A	Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay	[PMID: 31710483]
A549	GI₅₀	> 5 μM Compound: 3	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay Antiproliferative activity against human A549 cells after 48 hrs by SRB assay	[PMID: 28038324]
A549	GI₅₀	> 5 μM Compound: Tubastatin A	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay	[PMID: 31924504]
B16	GI₅₀	40.5 μM Compound: Tubastatin A	Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay	[PMID: 23009203]
CAL-27	IC₅₀	4.6 μM Compound: Tubastatin A	Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay	[PMID: 28581289]
HCT-116	GI₅₀	> 5 μM Compound: 3	Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay	[PMID: 28038324]
HCT-116	GI₅₀	> 5 μM Compound: Tubastatin A	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by Sulforhodamine B assay	[PMID: 31924504]
HCT-116	IC₅₀	2 μM Compound: Tubastatin A	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28953386]
HCT-116	IC₅₀	2 μM Compound: Tubastatin A	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 27541357]
HEL	IC₅₀	2.54 μM Compound: 27	Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay	[PMID: 29940115]
HEL	IC₅₀	3.75 μM Compound: 27	Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
HEL	IC₅₀	8.09 μM Compound: Tubastatin A	Antiproliferative activity against human HEL cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay Antiproliferative activity against human HEL cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay	[PMID: 33992929]
HEL 92.1.7	IC₅₀	> 2 μM Compound: Tubastatin A	Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay	[PMID: 27541357]
HEL 92.1.7	IC₅₀	> 4 μM Compound: Tubastatin A	Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay	[PMID: 28953386]
HeLa	IC₅₀	2.5 μM Compound: Tubastatin A	Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay	[PMID: 25454270]
HeLa S3	IC₅₀	0.031 μM Compound: Tubastatin	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 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	[PMID: 28337317]
HeLa S3	IC₅₀	2.7 μM Compound: Tubastatin	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 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	[PMID: 28337317]
HeLa S3	IC₅₀	2.9 μM Compound: Tubastatin	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 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	[PMID: 28337317]
HeLa S3	IC₅₀	3.9 μM Compound: Tubastatin	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 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	[PMID: 28337317]
HL-60	IC₅₀	2.54 μM Compound: 27	Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay	[PMID: 29940115]
HL-60	IC₅₀	3.75 μM Compound: 27	Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
HL-60	IC₅₀	4.09 μM Compound: Tubastatin A	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay	[PMID: 33992929]
Huh-7	CC₅₀	11 μM Compound: Tubastatin A	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 31201063]
HUVEC	IC₅₀	29.17 μM Compound: TubA	Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
HUVEC	IC₅₀	69.23 μM Compound: Tubastatin A	Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 33992929]
Jurkat	IC₅₀	14.58 μM Compound: Tubastatin A	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay	[PMID: 33992929]
Jurkat	IC₅₀	3.38 μM Compound: Tubastatin A	Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay	[PMID: 24304348]
K562	IC₅₀	2.07 μM Compound: Tubastatin A	Cytotoxicity against human K562 cells incubated for 72 hrs by Sulphorhodamine assay Cytotoxicity against human K562 cells incubated for 72 hrs by Sulphorhodamine assay	[PMID: 37146520]
K562	IC₅₀	2.54 μM Compound: 27	Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay	[PMID: 29940115]
K562	IC₅₀	3.75 μM Compound: 27	Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
KB	IC₅₀	14.81 μM Compound: Tubastatin A	Cytotoxicity against human KB cells after 72 hrs by MTS assay Cytotoxicity against human KB cells after 72 hrs by MTS assay	[PMID: 25899338]
KG-1	IC₅₀	8.82 μM Compound: Tubastatin A	Antiproliferative activity against human KG-1 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay Antiproliferative activity against human KG-1 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay	[PMID: 33992929]
LNCaP	IC₅₀	10.88 μM Compound: Tubastatin A	Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay	[PMID: 24304348]
MCF7	IC₅₀	3.7 μM Compound: Tubastatin A	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28953386]
MCF7	IC₅₀	3.7 μM Compound: Tubastatin A	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 27541357]
MDA-MB-231	IC₅₀	10.4 μM Compound: Tubastatin A	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 28953386]
MDA-MB-231	IC₅₀	10.4 μM Compound: Tubastatin A	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27541357]
NCI-H929	IC₅₀	15.42 μM Compound: Tubastatin A	Antiproliferative activity against human NCI-H929 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay Antiproliferative activity against human NCI-H929 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay	[PMID: 33992929]
PC-3	GI₅₀	> 5 μM Compound: 3	Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay	[PMID: 28038324]
PC-3	IC₅₀	8.6 μM Compound: Tubastatin A	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 28953386]
PC-3	IC₅₀	8.6 μM Compound: Tubastatin A	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 27541357]
Sf21	IC₅₀	> 10000 nM Compound: Tubastatin A	Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells by using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay Inhibition of recombinant human C-terminal FLAG/His-tagged HDAC1 (1 to 482 residues) expressed in Sf21 insect cells by using RHK-K(Ac)-AMC as substrate measured after 60 mins by fluorescence assay	[PMID: 31924504]
Sf9	IC₅₀	> 2000 nM Compound: Tubastatin A	Inhibition of human recombinant GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using MOCPAC as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis Inhibition of human recombinant GST-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using MOCPAC as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis	[PMID: 27650925]
Sf9	IC₅₀	> 30000 nM Compound: tubustatin A	Inhibition of human recombinant HDAC11 expressed in baculovirus/sf9 cells using RHKKAc as substrate Inhibition of human recombinant HDAC11 expressed in baculovirus/sf9 cells using RHKKAc as substrate	[PMID: 23905680]
Sf9	IC₅₀	> 30000 nM Compound: tubustatin A	Inhibition of human recombinant HDAC10 expressed in baculovirus/sf9 cells using RHKKAc as substrate Inhibition of human recombinant HDAC10 expressed in baculovirus/sf9 cells using RHKKAc as substrate	[PMID: 23905680]
Sf9	IC₅₀	> 30000 nM Compound: tubustatin A	Inhibition of human recombinant HDAC2 expressed in baculovirus/sf9 cells using RHKKAc as substrate Inhibition of human recombinant HDAC2 expressed in baculovirus/sf9 cells using RHKKAc as substrate	[PMID: 23905680]
Sf9	IC₅₀	0.0035 μM Compound: Tubastatin A	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 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	[PMID: 27541357]
Sf9	IC₅₀	11 nM Compound: Tubastatin A	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 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	[PMID: 27541357]
Sf9	IC₅₀	14 nM Compound: Tubastatin A	Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based assay	[PMID: 31391882]
Sf9	IC₅₀	15 nM Compound: Tubastatin A	Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate	[PMID: 23009203]
Sf9	IC₅₀	15 nM Compound: tubustatin A	Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate	[PMID: 23905680]
Sf9	IC₅₀	16400 nM Compound: Tubastatin A	Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate	[PMID: 23009203]
Sf9	IC₅₀	16400 nM Compound: tubustatin A	Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate	[PMID: 23905680]
Sf9	IC₅₀	21 nM Compound: Tubastatin A	Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method	[PMID: 31710483]
Sf9	IC₅₀	2490 nM Compound: Tubastatin A	Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based a Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Z-Lys(Ac)-AMC as substrate incubated for 90 mins followed by trypsin addition and measured after 30 mins by fluorescence based a	[PMID: 31391882]
Sf9	IC₅₀	854 nM Compound: tubustatin A	Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate	[PMID: 23905680]
SH-SY5Y	IC₅₀	1109.7 nM Compound: Tubastatin A	Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis	[PMID: 27650925]
SH-SY5Y	IC₅₀	122.1 nM Compound: Tubastatin A	Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis	[PMID: 27650925]
SH-SY5Y	IC₅₀	3.15 μM Compound: Tubastatin A	Cytotoxicity against human SH-SY5Y cells assessed as cell viability measured after 36 hrs by CCK8 assay Cytotoxicity against human SH-SY5Y cells assessed as cell viability measured after 36 hrs by CCK8 assay	[PMID: 36645952]
SH-SY5Y	IC₅₀	94.3 nM Compound: Tubastatin A	Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis	[PMID: 27650925]
THP-1	IC₅₀	> 10 μg/mL Compound: Tubastatin A	Cytotoxicity against human THP1 cells after 48 hrs by Alamar blue assay Cytotoxicity against human THP1 cells after 48 hrs by Alamar blue assay	[PMID: 25240614]
THP-1	IC₅₀	1.9 μg/mL Compound: Tubastatin A	Antileishmanial activity against amastigote stage of Leishmania donovani infected in human THP1 cells after 48 hrs by Alamar blue assay Antileishmanial activity against amastigote stage of Leishmania donovani infected in human THP1 cells after 48 hrs by Alamar blue assay	[PMID: 25240614]
U-937	EC₅₀	83 μM Compound: Tubastatin	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 44 hrs by MTT assay Cytotoxicity against human U937 cells assessed as decrease in cell viability after 44 hrs by MTT assay	[PMID: 29150330]
Vero	IC₅₀	> 20 μM Compound: Tubastatin A	Cytotoxicity against African green monkey Vero cells assessed as growth inhibition after 72 hrs by MTS assay Cytotoxicity against African green monkey Vero cells assessed as growth inhibition after 72 hrs by MTS assay	[PMID: 24304348]

In Vitro

Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM^[1]. At 100 ng/mL Tubastatin A increases Foxp³⁺ T-regulatory cells (Tregs) suppression of T cell proliferation in vitro^[2]. Tubastatin A treatment in CC12 cells would lead to myotube formation impairment when alpha-tubulin is hyperacetylated early in the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyeperacetylated in myotubes^[3]. A recent study indicates that Tubastatin A treatment increases cell elasticity as revealed by atomic force microscopy (AFM) tests without exerting drastic changes to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Daily treatment of Tubastatin A at 0.5 mg/kg inhibits HDAC6 to promote Tregs suppressive activity in mouse models of inflammation and autoimmunity, including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

335.40

Formula

C₂₀H₂₁N₃O₂

CAS No.

1252003-15-8

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NO)C1=CC=C(CN2C3=C(CN(C)CC3)C4=C2C=CC=C4)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (37.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9815 mL	14.9076 mL	29.8151 mL
5 mM	0.5963 mL	2.9815 mL	5.9630 mL
10 mM	0.2982 mL	1.4908 mL	2.9815 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.73 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.73 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.73 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 25 mg/mL (74.54 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.07%

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Data Sheet (285 KB) SDS (393 KB)

COA (253 KB) HNMR (281 KB) RP-HPLC (249 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Kyle V. Butler et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A J. Am. Chem. Soc., 2010, 132 (31), pp 10842-10846 [Content Brief]

[2]. Kozyreva VK, et al. NEDD9 regulates actin dynamics through cortactin deacetylation in an AURKA/HDAC6-dependent manner. Mol Cancer Res. 2014 May;12(5):681-93. [Content Brief]

[3]. de Zoeten EF, et al. Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol. 2011 May;31(10):2066-78. [Content Brief]

[4]. Brijmohan, Angela, et al. Role of HDAC6 in Transcription Factor EB Mediated Clearance of Misfolded Proteins in Chronic Kidney Disease. University of Toronto.Nov-2017.

[5]. Di Fulvio S, et al. Dysferlin interacts with histone deacetylase 6 and increases alpha-tubulin acetylation. PLoS One. 2011;6(12):e28563 [Content Brief]

[6]. Ketene AN, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells. Integr Biol (Camb). 2012 May;4(5):540-9. [Content Brief]

[7]. Lechner S, Malgapo MIP, Grätz C, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target [published online ahead of print, 2022 Apr 28]. Nat Chem Biol. 2022;10.1038/s41589-022-01015-5. [Content Brief]

[8]. Géraldy M, Morgen M, Sehr P, et al. Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. J Med Chem. 2019;62(9):4426-4443. [Content Brief]

[9]. Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28. [Content Brief]

Cell Assay ^[1]	Primary cortical neuron cultures are obtained from the cerebral cortex of fetal Sprague-Dawley rats (embryonic day 17) as described previously. All experiments are initiated 24 hours after plating. Under these conditions, the cells are not susceptible to glutamate-mediated excitotoxicity. For cytotoxicity studies, cells are rinsed with warm PBS and then placed in minimum essential medium containing 5.5 g/L glucose, 10% fetal calf serum, 2 mM L-glutamine, and 100 μM cystine. Oxidative stress is induced by the addition of the glutamate analogue homocysteate (HCA; 5 mM) to the media. HCA is diluted from 100-fold concentrated solutions that are adjusted to pH 7.5. In combination with HCA, neurons are treated with Tubastatin A at the indicated concentrations. Viability is assessed after 24 hours by MTT assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	The effects of HDAC6 targeting in dextran sodium sulfate (DSS) and adoptive transfer models of colitis are evaluated, using 10 mice per group. Freshly prepared 4% (wt/vol) DSS (MP Biomedicals) is added daily for 5 days to the pH-balanced tap water of WT B6 mice. Mice are treated daily for 7 days with tubacin or niltubacin (0.5 mg/kg of body weight/day, i.p.), and colitis is assessed by daily monitoring of body weight, stool consistency, and fecal blood. Stool consistency is scored as 0 (hard), 2 (soft), or 4 (diarrhea), and fecal blood (Hemoccult) is scored as 0 (absent), 2 (occult), or 4 (gross). To assess prevention of colitis in a T cell-dependent model, CD⁴⁺ CD45RBhi T cells (1×10⁶) isolated from WT mice using magnetic beads (>95% cell purity, flow cytometry) are injected i.p. into B6/Rag1^−/− mice plus CD⁴⁺ CD²⁵⁺ Tregs (1.25×10⁵) isolated using magnetic beads from HDAC6^−/− or WT mice (>90% Treg purity, flow cytometry) and mice are monitored biweekly for clinical evidence of colitis. To assess therapy of established T cell-dependent colitis, B6/Rag1^−/− mice are injected i.p. with CD⁴⁺ CD45RBhi cells (1×10⁶). Once colitis has developed, mice also receive CD⁴⁺ CD²⁵⁺ Tregs (5×10⁵ cells) isolated as described above from HDAC6^−/− or WT mice or treatment with HDAC6i (tubastatin A) or HSP90i (17-AAG). Mice are monitored for continued weight loss and stool consistency. At the cessation of the study, paraffin sections of colons stained with Alcian Blue or hematoxylin and eosin are graded histologically or evaluated by immunoperoxidase staining for Foxp³⁺ Treg infiltration. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Kyle V. Butler et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A J. Am. Chem. Soc., 2010, 132 (31), pp 10842-10846 [Content Brief] [2]. Kozyreva VK, et al. NEDD9 regulates actin dynamics through cortactin deacetylation in an AURKA/HDAC6-dependent manner. Mol Cancer Res. 2014 May;12(5):681-93. [Content Brief] [3]. de Zoeten EF, et al. Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol. 2011 May;31(10):2066-78. [Content Brief] [4]. Brijmohan, Angela, et al. Role of HDAC6 in Transcription Factor EB Mediated Clearance of Misfolded Proteins in Chronic Kidney Disease. University of Toronto.Nov-2017. [5]. Di Fulvio S, et al. Dysferlin interacts with histone deacetylase 6 and increases alpha-tubulin acetylation. PLoS One. 2011;6(12):e28563 [Content Brief] [6]. Ketene AN, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells. Integr Biol (Camb). 2012 May;4(5):540-9. [Content Brief] [7]. Lechner S, Malgapo MIP, Grätz C, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target [published online ahead of print, 2022 Apr 28]. Nat Chem Biol. 2022;10.1038/s41589-022-01015-5. [Content Brief] [8]. Géraldy M, Morgen M, Sehr P, et al. Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. J Med Chem. 2019;62(9):4426-4443. [Content Brief] [9]. Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9815 mL	14.9076 mL	29.8151 mL	74.5379 mL
	5 mM	0.5963 mL	2.9815 mL	5.9630 mL	14.9076 mL
	10 mM	0.2982 mL	1.4908 mL	2.9815 mL	7.4538 mL
	15 mM	0.1988 mL	0.9938 mL	1.9877 mL	4.9692 mL
	20 mM	0.1491 mL	0.7454 mL	1.4908 mL	3.7269 mL
	25 mM	0.1193 mL	0.5963 mL	1.1926 mL	2.9815 mL
	30 mM	0.0994 mL	0.4969 mL	0.9938 mL	2.4846 mL

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tubastatin A1252003-15-8Beta-lactamaseHDACAutophagyApoptosisβ-lactamaseHistone deacetylasesInhibitorinhibitorinhibit

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