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Chemical Structure| 1310693-92-5 Chemical Structure| 1310693-92-5
Chemical Structure| 1310693-92-5

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Tubastatin A HCl

CAS No.: 1310693-92-5

Tubastatin A Hydrochloride (Tubastatin A HCl) is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay. It is 1000-fold more selective against all other isozymes except HDAC8, which it inhibits 57-fold more selectively. Tubastatin A Hydrochloride also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).

Synonyms: TSA HCl;Tubastatin A Hydrochloride

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Cat. No.: A107990 Purity: 98%

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Product Details of [ Tubastatin A HCl ]

CAS No. :1310693-92-5
Formula : C20H22ClN3O2
M.W : 371.86
SMILES Code : O=C(NO)C1=CC=C(CN2C3=C(CN(C)CC3)C4=C2C=CC=C4)C=C1.[H]Cl
Synonyms :
TSA HCl;Tubastatin A Hydrochloride
MDL No. :MFCD20488052
InChI Key :LJTSJTWIMOGKRJ-UHFFFAOYSA-N
Pubchem ID :57336514

Safety of [ Tubastatin A HCl ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of [ Tubastatin A HCl ]

epigenetics

ALK Isoform Comparison

Name HD1 HD2 HDAC HDAC1 HDAC10 HDAC11 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 Purity
Givinostat HCl monohydrate ++++

HD1-B, IC50: 7.5 nM

HD1-A, IC50: 16 nM

+++

HD2, IC50: 10 nM

98%
MC1568 ++

HD1-B (Maize), IC50: 3.4 μM

HD1-A (Maize), IC50: 100 nM

96%
Trichostatin A ++++

HDAC, IC50: ~1.8 nM

98%
Scriptaid 99%
Valproic acid sodium 97%
AR-42 +++

HDAC, IC50: 30 nM

98%
M344 ++

HDAC, IC50: 100 nM

99%
Splitomicin +

Sir2p, IC50: 60 μM

99%
Panobinostat ++++

HDAC (Reh cells), IC50: 20 nM

HDAC (MOLT-4 cells), IC50: 5 nM

98%
Sodium 4-Phenylbutyrate 98%
Vorinostat +++

HDAC, IC50: ~10 nM

98%
Curcumin 98%
Belinostat +++

HDAC, IC50: 27 nM

98%
Fimepinostat ++++

HDAC1, IC50: 1.7 nM

++++

HDAC10, IC50: 2.8 nM

++++

HDAC11, IC50: 5.4 nM

++++

HDAC2, IC50: 5.0 nM

++++

HDAC3, IC50: 1.8 nM

+++

HDAC6, IC50: 27 nM

98%
RG-2833 ++

HDAC1, Ki: 32 nM

++

HDAC3, Ki: 5 nM

98%
Valproic acid +

HDAC1, IC50: 0.4 mM

98%
BG45 +

HDAC1, IC50: 2 μM

+

HDAC2, IC50: 2.2 μM

+

HDAC3, IC50: 289 nM

99%
Entinostat +

HDAC1, IC50: 0.51 μM

+

HDAC3, IC50: 1.7 μM

98%
Ricolinostat ++

HDAC1, IC50: 58 nM

++

HDAC2, IC50: 48 nM

++

HDAC3, IC50: 51 nM

++++

HDAC6, IC50: 4.7 nM

++

HDAC8, IC50: 100 nM

98+%
Resminostat +++

HDAC1, IC50: 42.5 nM

++

HDAC3, IC50: 50.1 nM

++

HDAC6, IC50: 71.8 nM

98+%
Domatinostat +

HDAC1, IC50: 1.20 μM

+

HDAC10, IC50: 21 μM

+

HDAC11, IC50: 9.7 μM

+

HDAC2, IC50: 1.12 μM

+

HDAC3, IC50: 0.57 μM

+

HDAC5, IC50: 11.3 μM

+

HDAC9, IC50: 50 μM

99% (HPLC)
Romidepsin +++

HDAC1, IC50: 36 nM

+++

HDAC2, IC50: 47 nM

99%
Abexinostat ++++

HDAC1, Ki: 7 nM

+++

HDAC10, IC50: 24 nM

+++

HDAC2, Ki: 19 nM

++++

HDAC3/SMRT, Ki: 8.2 nM

+++

HDAC6, Ki: 17 nM

+

HDAC8, IC50: 280 nM

98%
CUDC-101 ++++

HDAC1, IC50: 4.5 nM

+++

HDAC10, IC50: 26.1 nM

+++

HDAC2, IC50: 12.6 nM

++++

HDAC3, IC50: 9.1 nM

+++

HDAC4, IC50: 13.2 nM

+++

HDAC5, IC50: 11.4 nM

++++

HDAC6, IC50: 5.1 nM

+

HDAC7, IC50: 373 nM

++

HDAC9, IC50: 67.2 nM

98%
Parthenolide 97% HPLC
Tacedinaline +

HDAC1, IC50: 0.9 μM

+

HDAC2, IC50: 0.9 μM

+

HDAC3, IC50: 1.2 μM

98%
Mocetinostat ++

HDAC1, IC50: 0.15 μM

+

HDAC11, IC50: 0.59 μM

+

HDAC2, IC50: 0.29 μM

+

HDAC3, IC50: 1.66 μM

98%
Pracinostat ++

HDAC1, IC50: 49 nM

+++

HDAC10, IC50: 40 nM

++

HDAC11, IC50: 93 nM

++ +++

HDAC3, IC50: 43 nM

++

HDAC4, IC50: 56 nM

+++

HDAC5, IC50: 47 nM

+

HDAC6, IC50: 1.008 μM

++

HDAC7, IC50: 137 nM

++

HDAC9, IC50: 70 nM

98%
Citarinostat +++

HDAC1, IC50: 35 nM

+++

HDAC2, IC50: 45 nM

+++

HDAC3, IC50: 46 nM

++++

HDAC6, IC50: 2.6 nM

++

HDAC8, IC50: 137 nM

98+%
HPOB +

HDAC1, IC50: 2.9 μM

+

HDAC10, IC50: 3.0 μM

+

HDAC2, IC50: 4.4 μM

+

HDAC3, IC50: 1.7 μM

++

HDAC6, IC50: 56 nM

+

HDAC8, IC50: 2.8 μM

97%
WT-161 ++++

HDAC1, IC50: 8.35 nM

+++

HDAC2, IC50: 15.4 nM

++++

HDAC6, IC50: 0.4 nM

98+%
Tucidinostat ++

HDAC1, IC50: 95 nM

++

HDAC10, IC50: 78 nM

++

HDAC2, IC50: 160 nM

++

HDAC3, IC50: 67 nM

97%
Santacruzamate A ++++

HDAC2, IC50: 119 pM

98%
Droxinostat +

HDAC3, IC50: 16.9 μM

+

HDAC6, IC50: 2.47 μM

+

HDAC8, IC50: 1.46 μM

99%
(E,E)-RGFP966 ++

HDAC3, IC50: 80 nM

97%
Tasquinimod 98%
LMK-235 +++

HDAC4, IC50: 11.9 nM

++++

HDAC5, IC50: 4.2 nM

99%
CAY10603 ++++

HDAC6, IC50: 2 pM

98%
Tubastatin A +++

HDAC6, IC50: 15 nM

98%
BRD73954 +++

HDAC6, IC50: 36 nM

++

HDAC8, IC50: 120 nM

99%
Tubastatin A HCl +++

HDAC6, IC50: 15 nM

+

HDAC8, IC50: 854 nM

98%
Tubacin ++++

HDAC6, IC50: 4 nM

95%
ACY-738 ++++

HDAC6, IC50: 1.7 nM

98%
Nexturastat A ++++

HDAC6, IC50: 5 nM

98%
TMP269 ++

HDAC4, IC50: 157 nM

++

HDAC5, IC50: 97 nM

+++

HDAC7, IC50: 43 nM

+++

HDAC9, IC50: 23 nM

98+%
TMP195 ++

HDAC4, Ki: 59 nM

++

HDAC5, Ki: 60 nM

+++

HDAC7, Ki: 26 nM

+++

HDAC9, Ki: 15 nM

98%
PCI-34051 +++

HDAC8, IC50: 10 nM

98%

Biological Activity

Target
  • HDAC8

    HDAC8, IC50:854 nM

  • HDAC6

    HDAC6, IC50:15 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
MOLT-4 cells 10 or 20 μM 48 hours Tubastatin A in combination with vincristine significantly enhanced cytotoxicity, leading to G2/M phase cell cycle arrest and subsequent induction of apoptosis. PMC4504084
Neuro2A cells 5 or 16 μM 24 hours Enhanced transfection efficiency, significantly increased the number of EGFP positive cells PMC5389648
Primary cortical neurons 10 μM 24 hours Significantly enhanced transfection efficiency, close to 80% of the cells were transfected PMC5389648
Mesenchymal stem cells (MSC) 10 μM 24 hours Significantly enhanced transfection efficiency, approximately 70% of MSC expressed EGFP PMC5389648
N1-LRb cells 100 ng/mL 4 hours To evaluate the effect of Tubastatin A on leptin signaling pathways, results showed that Tubastatin A enhanced leptin-induced gene expression PMC8892841
naïve CD4+ T cells 10 μM 24 hours Tubastatin A significantly suppressed the differentiation of naïve CD4+ T cells into Th17 cells under Th17-skewing conditions and reduced the expression of IL-17A and RORγt mRNA. PMC7295069
HEK293 cells 10 μM 8 hours Inhibit HDAC6 activity, increase the acetylation level of SCIN PMC10549198
C2C12 myotubes 5 µM 24 hours To evaluate the effect of HDAC6 inhibitors on utrophin A expression in C2C12 myotubes, results showed that both TubA and tubacin significantly upregulated utrophin A levels by ∼1.75-fold. PMC9675748
iPS-CM (induced pluripotent stem cell-derived cardiomyocytes) 3 µM 24 hours Increased α-tubulin acetylation levels, decreased contraction frequency, and improved contractility PMC9780334

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Rats CCA animal model Intraperitoneal injection 10 mg/kg/d Once daily for 10 days Reduced tumor growth and induced ciliogenesis PMC3768151
Mice Diet-induced obese mouse model Intraperitoneal injection 5 mg/kg/day Once daily for 6 weeks To evaluate the effect of Tubastatin A on body weight and metabolic function in obese mice, results showed that Tubastatin A significantly reduced food intake and body weight, and improved glucose homeostasis PMC8892841
mice acute lung allograft rejection model intraperitoneal injection 10 mg/100g body weight Daily for 7 days Tubastatin A significantly prolonged the survival of lung allografts and attenuated acute rejection by downregulating Th17 cell function. PMC7295069
mice Duchenne muscular dystrophy mdx mouse model intraperitoneal injection 25 mg/kg Daily injections for two weeks To evaluate the effect of TubA on muscle function in mdx mice, results showed that TubA significantly increased muscle strength, improved microtubule, neuromuscular junction, and dystrophin-associated glycoprotein complex organization, and reduced muscle atrophy and fibrosis. PMC9675748
Mice Lmnap.H222P/H222P mice Intraperitoneal injection 30 mg/kg daily until lung allograft loss Increased α-tubulin acetylation levels, improved cardiac function, and restored proper Cx43 localization in cardiomyocytes PMC9780334

Protocol

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