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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. PMC4297530
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. PMC4848209
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. PMC4848209
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. PMC6903704
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. PMC7295069
iBMDMs 10 μM 1 h Inhibited NLRP3 inflammasome activation, reduced caspase-1 processing and IL-1β release PMC7814939

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. PMC6903704
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. PMC6471870
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. PMC7295069
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 PMC7814939
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 PMC9117661

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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