Tubastatin A

Modify Date: 2024-01-03 01:23:57

Tubastatin A structure	Common Name	Tubastatin A
	CAS Number	1239262-52-2	Molecular Weight	449.42
	Density	1.3±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C₂₂H₂₂F₃N₃O₄	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	N/A

Use of Tubastatin A

Tubastatin A (TSA) TFA is a potent and selective?HDAC6?inhibitor with?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 TFA also inhibits HDAC10 and metallo-β-lactamase domain-containing protein?2 (MBLAC2).

Name	Tubastatin A Trifluoroacetate
Synonym	More Synonyms

Description	Tubastatin A (TSA) TFA is a potent and selective?HDAC6?inhibitor with?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 TFA also inhibits HDAC10 and metallo-β-lactamase domain-containing protein?2 (MBLAC2).
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC Signaling Pathways >> Epigenetics >> HDAC
Target	IC50: 15 nM (HDAC6)[1]
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].
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].
References	[1]. 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. [2]. 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 [3]. Di Fulvio S, et al. Dysferlin interacts with histone deacetylase 6 and increases alpha-tubulin acetylation. PLoS One. 2011;6(12):e28563 [4]. 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. [5]. Brijmohan AS, et al. HDAC6 Inhibition Promotes Transcription Factor EB Activation and Is Protective in Experimental Kidney Disease. Front Pharmacol. 2018 Feb 1;9:34. [6]. Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28.

Density	1.3±0.1 g/cm3
Molecular Formula	C₂₂H₂₂F₃N₃O₄
Molecular Weight	449.42
Exact Mass	335.163391
PSA	94.80000
LogP	2.14
Index of Refraction	1.668

4-(2-Methyl-l,2...

CAS#:1239034-70-8

trifluoroacetic acid

CAS#:76-05-1

~31%

Tubastatin A

CAS#:1239262-52-2

Literature: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS; KOZIKOWSKI, Alan; BUTLER, Kyle, B.; KALIN, Jay, Hans Patent: WO2011/11186 A2, 2011 ; Location in patent: Page/Page column 54-55 ; WO 2011/011186 A2

N-Methyl-4-pipe...

CAS#:1445-73-4

Tubastatin A

CAS#:1239262-52-2

Literature: WO2011/11186 A2, ; WO 2011/011186 A2

Phenylhydrazine

CAS#:100-63-0

Tubastatin A

CAS#:1239262-52-2

Literature: WO2011/11186 A2, ; WO 2011/011186 A2

1H-Pyrido[4,3-b...

CAS#:5094-12-2

Tubastatin A

CAS#:1239262-52-2

Literature: WO2011/11186 A2, ; WO 2011/011186 A2

Tubastatin A

CAS#:1252003-15-8

trifluoroacetic acid

CAS#:76-05-1

Tubastatin A

CAS#:1239262-52-2

Literature: Journal of the American Chemical Society, , vol. 132, # 31 p. 10842 - 10846

Precursor 5
CAS#:76-05-1 trifluoroacetic acid CAS#:1445-73-4 N-Methyl-4-pipe... CAS#:100-63-0 Phenylhydrazine CAS#:5094-12-2 1H-Pyrido[4,3-b...
CAS#:1252003-15-8 Tubastatin A
DownStream 0

TUBASTATIN A HYDROCHLORIDE

N-hydroxy-4-({2-methyl-1H,3H,4H-pyrido[4,3-b]indol-5-yl}methyl)benzamide hydrochloride

N-Hydroxy-4-[(2-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide

Benzamide, N-hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]-

Tubastatin A Trifluoroacetic Acid Salt

TUBASTSTINA HCL

TUBASTATIN A ((2-METHYL-3,4-DIHYDRO-1H-PYRIDO[4,3-B]-INDOL- 5(2H)-YL)METHYL)BENZAMIDE)

TUBASTATIN A_HCL

Tubastatin A

TUBASTANTIN A

Tubastatin A (trifluoroacetate salt)

TRIETHYLENETHIOPHOSPHORAMIDE,WHITE SOLID

[4-({2-methyl-1H,2H,3H,4H,5H-pyrido[4,3-b]indol-5-yl}methyl)phenyl]formamido 2,2,2-trifluoroacetate

N-Hydroxy-4-[(2-methyl-1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-5 -yl)methyl]benzamide

N-hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)methyl)benzamide

DC Chemicals Limited
China
Product Name: Tubastatin A TFA
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: TUBASTATIN A
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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