Tubastatin-A

Product Name: Tubastatin-A
CAS No.: 1252003-15-8
Chemical Name: Tubastatin-A
Synonyms: CS-1922;Tubastatin;Tubastatin A BASE;TubastatinA inhibitor;Tubastatin A(free base);Tubastatin A, 10 mM in DMSO;Tubastatin A (TubA, AG-CR1-3900);N-hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide;N-hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)methyl)benzamide;N-Hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]benzamide
CBNumber: CB32667491
Molecular Formula: C20H21N3O2
Formula Weight: 335.4
MOL File: 1252003-15-8.mol

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Tubastatin-A Property

Density: 1.28±0.1 g/cm3(Predicted)
storage temp.: Sealed in dry,Store in freezer, under -20°C
solubility: insoluble in EtOH; insoluble in H2O; ≥10.75 mg/mL in DMSO
form: solid
pka: 8.95±0.10(Predicted)
color: Off-white to light yellow
InChI: InChI=1S/C20H21N3O2/c1-22-11-10-19-17(13-22)16-4-2-3-5-18(16)23(19)12-14-6-8-15(9-7-14)20(24)21-25/h2-9,25H,10-13H2,1H3,(H,21,24)
InChIKey: GOVYBPLHWIEHEJ-UHFFFAOYSA-N
SMILES: C(NO)(=O)C1=CC=C(CN2C3=C(C=CC=C3)C3CN(C)CCC2=3)C=C1

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 15785
Product name: Tubastatin A
Purity: ≥95%
Packaging: 5mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 15785
Product name: Tubastatin A
Purity: ≥95%
Packaging: 10mg
Price: $74
Updated: 2024/03/01

Cayman Chemical

Product number: 15785
Product name: Tubastatin A
Purity: ≥95%
Packaging: 25mg
Price: $130
Updated: 2024/03/01

Cayman Chemical

Product number: 15785
Product name: Tubastatin A
Purity: ≥95%
Packaging: 50mg
Price: $193
Updated: 2024/03/01

ChemScene

Product number: CS-5376
Product name: TubastatinA
Purity: 98.12%
Packaging: 200mg
Price: $250
Updated: 2021/12/16

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Tubastatin-A Chemical Properties,Usage,Production

Uses

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).

Definition

ChEBI: A pyridoindole that is 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indole which is substituted on the tetrahydropyridine nitrogen by a methyl group and on the indole nitrogen by a p-[N-(hydroxy)aminoca bonyl]benzyl group. It is a histone deacetylase 6 (HDAC6) inhibitor that is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).

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].

target

HDAC6

IC 50

HDAC6: 15 nM (IC₅₀); HDAC8: 854 nM (IC₅₀); HDAC1: 16400 nM (IC₅₀)

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 DOI:10.1021/ja102758v
[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. DOI:10.1158/1541-7786.MCR-13-0654
[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. DOI:10.1128/MCB.05155-11
[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 DOI:10.1371/journal.pone.0028563
[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. DOI:10.1039/c2ib00168c
[7] Lechner S, Malgapo MIP, Gr?tz 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. DOI:10.1038/s41589-022-01015-5
[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. DOI:10.1021/acs.jmedchem.8b01936
[9] Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28. DOI:10.1038/s41589-022-01015-5

Tubastatin-A Preparation Products And Raw materials

Raw materials

Preparation Products

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Tubastatin-A Suppliers

China 108 India 1 United States 12 Global 121

Tianjin Kailiqi Biotechnology Co., Ltd.

Tel: 15076683720
Fax: 022-23754520
Email: klq@cw-bio.com
Country: China
ProdList: 8011
Advantage: 55

Jinan Jiuli Biotechnology Co. , Ltd.

Tel: 15865264761
Email: 486064515@qq.com
Country: China
ProdList: 4798
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Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2922
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Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
ProdList: 4747
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Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
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Guangzhou Isun Pharmaceutical Co., Ltd

Tel: 020-39119399 18927568969
Fax: 020-39119999
Email: isunpharm@qq.com
Country: China
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Credit Asia Chemical Co., Ltd.

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Cool Pharm, Ltd

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Hubei Jusheng Technology Co.,Ltd

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Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4757
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View Lastest Price from Tubastatin-A manufacturers

Shaanxi Haibo Biotechnology Co., Ltd

Product: TUBASTATIN A 1252003-15-8
Price: US $0.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 2000ton
Release date: 2023-08-29

1252003-15-8, Tubastatin-ARelated Search:

Tubastatin A hydrochloride ACY-1215 Tacedinaline PCI 34051 Vorinostat Entinostat RGFP966

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

N-hydroxy-4-((2-methyl-2,3,4,5-tetrahydro-1H-indeno[1,2-c]pyridin-5-yl)methyl)benzamide

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

Tubastatin A BASE

Tubastatin A(free base)

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

N-hydroxy-4-(2-methyl-1,2,3,4-tetrahydro-pyrido[4,3-b]indol-5-ylmethyl)benzamide

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

CS-1922

Tubastatin

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

Tubastatin A (TubA, AG-CR1-3900)

TubastatinA inhibitor

Tubastatin A, 10 mM in DMSO

1252003-15-8

Inhibitors