Cat. No.: HY-13271AG

Tubastatin A (GMP)

Tubastatin A (GMP) is the Tubastatin A (HY-13271A) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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.

CAS No.: 1252003-15-8
Formula: C₂₀H₂₁N₃O₂
Molecular Weight:335.40

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Data Sheet (278 KB)

Tubastatin A (GMP) Chemical Structure

CAS No.: 1252003-15-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

All HDAC Isoforms :

All Beta-lactamase Isoforms :

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: 27541357]
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 Antiproliferative activity against human HCT116 cells	[PMID: 29945795]
HEK293	IC₅₀	>50 μM Compound: Tubastatin A	Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37875056]
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	>4 μM Compound: Tubastatin A	Antiproliferative activity against human HL60 cells Antiproliferative activity against human HL60 cells	[PMID: 27541357]
HL-60	IC₅₀	>4 μM Compound: Tubastatin A	Antiproliferative activity against human HL60 cells Antiproliferative activity against human HL60 cells	[PMID: 28953386]
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	>4 μM Compound: Tubastatin A	Antiproliferative activity against human Jurkat cells Antiproliferative activity against human Jurkat cells	[PMID: 27541357]
Jurkat	IC₅₀	>4 μM Compound: Tubastatin A	Antiproliferative activity against human Jurkat cells Antiproliferative activity against human Jurkat cells	[PMID: 28953386]
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]
L02	IC₅₀	>50 μM Compound: Tubastatin A	Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37875056]
LNCaP	GI₅₀	5 μM Compound: TUB A	Antiproliferative activity against human LNCaP cells assessed as growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human LNCaP cells assessed as growth inhibition incubated for 72 hrs by MTT assay	[PMID: 37633202]
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: 27541357]
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 Antiproliferative activity against human MCF7 cells	[PMID: 29945795]
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]
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 Antiproliferative activity against human MDA-MB-231 cells	[PMID: 29945795]
MM1.S	IC₅₀	9.45 μM Compound: Tubastatin A	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37875056]
N2a	EC₅₀	145 nM Compound: TubA	Inhibition of HDAC6 in mouse N2A cells assessed as increase in alpha tubulin acetylation Inhibition of HDAC6 in mouse N2A cells assessed as increase in alpha tubulin acetylation	[PMID: 32435374]
N2a	IC₅₀	4.4 nM Compound: TubA	Inhibition of HDAC6 in mouse N2A cells Inhibition of HDAC6 in mouse N2A cells	[PMID: 32435374]
N2a	IC₅₀	8100 nM Compound: TubA	Inhibition of HDAC1 in mouse N2A cells Inhibition of HDAC1 in mouse N2A cells	[PMID: 32435374]
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: 27541357]
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 Antiproliferative activity against human PC3 cells	[PMID: 29945795]
RPMI-8226	IC₅₀	9.45 μM Compound: Tubastatin A	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37875056]
RWPE-1	GI₅₀	20.2 μM Compound: TUB A	Antiproliferative activity against human RWPE-1 cells assessed as growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human RWPE-1 cells assessed as growth inhibition incubated for 72 hrs by MTT assay	[PMID: 37633202]
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 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 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 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-266	IC₅₀	9.45 μM Compound: Tubastatin A	Antiproliferative activity against human U-266 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human U-266 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37875056]
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.

Chemical Information

CAS No. 1252003-15-8
Molecular Weight 335.40
Formula C₂₀H₂₁N₃O₂
SMILES

O=C(NO)C1=CC=C(CN2C3=C(CN(C)CC3)C4=C2C=CC=C4)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. 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]

[2]. 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]

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

[4]. 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]

[5]. 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.

[6]. 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]

[7]. 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]

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

[9]. 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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Tubastatin A (GMP)

Tubastatin A

Entinostat

Panobinostat

Vorinostat

Romidepsin

Mocetinostat

Tubacin

Trichostatin A

Valproic acid

Sodium butyrate

Sodium 4-phenylbutyrate

Tubastatin A (Standard)

All HDAC Isoforms

All Beta-lactamase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Bioz

Tubastatin A (GMP)

Tubastatin A

Entinostat

Panobinostat

Vorinostat

Romidepsin

Mocetinostat

Tubacin

Trichostatin A

Valproic acid

Sodium butyrate

Sodium 4-phenylbutyrate

Tubastatin A (Standard)

All HDAC Isoforms

All Beta-lactamase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Tubastatin A (GMP) Related Classifications

HY-13271AG Related Classifications

Bioz