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Chemical Structure| 1252003-15-8 Chemical Structure| 1252003-15-8

Structure of Tubastatin A
CAS No.: 1252003-15-8

Chemical Structure| 1252003-15-8

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Tubastatin A is an effective and selective HDAC6 inhibitor with an IC50 of 15 nM. It is 57 times more selective for HDAC6 over HDAC8 and over 1000 times more selective than other isoenzymes. Tubastatin A also inhibits HDAC10 and MBLAC2.

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Product Details of Tubastatin A

CAS No. :1252003-15-8
Formula : C20H21N3O2
M.W : 335.40
SMILES Code : O=C(NO)C1=CC=C(CN2C3=C(CN(C)CC3)C4=C2C=CC=C4)C=C1
MDL No. :MFCD18071463
InChI Key :GOVYBPLHWIEHEJ-UHFFFAOYSA-N
Pubchem ID :49850262

Safety of Tubastatin A

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Tubastatin A

epigenetics

Isoform Comparison

Biological Activity

Target
  • HDAC6

    HDAC6, IC50:15 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
RN46A-B14 cells 2.5 μM 1 h To test the effect of Tubastatin A on hormone-induced GR translocation, results showed that Tubastatin A significantly inhibited DEX-induced GR translocation. Biol Psychiatry. 2015 Feb 15;77(4):345-55.
TKPTS cells 100nM 24 h To study the effect of HDAC6 inhibition on AMWAP expression, results showed that Tubastatin A slightly increased AMWAP expression in TKPTS cells. Kidney Int. 2016 Feb;89(2):317-26.
RAW264.7 cells 100nM 24 h To study the effect of HDAC6 inhibition on AMWAP expression, results showed that Tubastatin A did not increase AMWAP expression in RAW264.7 cells. Kidney Int. 2016 Feb;89(2):317-26.
CD8+ T cells 10 μM 24 h Screening for compounds that promote IFN-γ expression in CD8+ T cells, Tubastatin A significantly promoted IFN-γ expression with low cellular toxicity. Immunity. 2019 Sep 17;51(3):491-507.e7.
Naïve CD4+ T cells 10 μM 24 h Tubastatin A significantly suppressed the differentiation of Naïve CD4+ T cells under Th17-skewing conditions and reduced the expression of IL-17A and RORγt mRNA. Theranostics. 2020 May 21;10(15):6790-6805.
iBMDMs 10 μM 1 h Inhibited NLRP3 inflammasome activation, reduced caspase-1 processing and IL-1β release Science. 2020 Sep 18;369(6510):eaas8995.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice B16-OVA melanoma model Intratumoral injection 60 μg/mouse Daily until the end of the experiment To evaluate the inhibitory effect of Tubastatin A and acetate combination therapy on tumor growth, the results showed that the combination therapy significantly inhibited tumor growth. Immunity. 2019 Sep 17;51(3):491-507.e7.
Mice MCAO model Intraperitoneal injection 0.5 mg/kg Every two days By inhibiting HDAC6, the study investigated its impact on functional recovery after stroke. The results showed that HDAC6 inhibition significantly reduced the dendritic length and branch number of newly generated neurons. J Biomed Sci. 2019 Apr 18;26(1):27
Mice Acute lung allograft rejection model Intraperitoneal injection 30 mg/kg Once daily until lung allograft loss Tubastatin A significantly attenuated the pathological lesions of acute lung allograft rejection, prolonged the survival of lung allografts, and attenuated acute rejection by suppressing Th17 cell accumulation. Theranostics. 2020 May 21;10(15):6790-6805.
Mice LPS-induced endotoxic shock model Intraperitoneal injection 70 mg/kg Single dose, lasting 12 hours Tubastatin A significantly reduced LPS-induced IL-1β and IL-18 secretion and alleviated acute lung injury Science. 2020 Sep 18;369(6510):eaas8995.
Mice Photothrombotic ischemia model Intraperitoneal injection 10 mg/kg Once daily for 3 days To study the protective effect of HDAC6 inhibition on ischemic brain injury Cell Death Dis. 2022 May 18;13(5):466

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.98mL

0.60mL

0.30mL

14.91mL

2.98mL

1.49mL

29.82mL

5.96mL

2.98mL

References

 

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