Home Cart Sign in  
Chemical Structure| 158093-65-3 Chemical Structure| 158093-65-3

Structure of PU139
CAS No.: 158093-65-3

Chemical Structure| 158093-65-3

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

PU139 is a broad-spectrum histone acetyltransferase (HAT) inhibitor that blocks Gcn5, p300/CBP-associated factor (PCAF), CBP, and p300 with IC50 values of 8.39, 9.74, 2.49, and 5.35 μM, respectively, suitable for research on cancer and gene regulation.

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of PU139

CAS No. :158093-65-3
Formula : C12H7FN2OS
M.W : 246.26
SMILES Code : O=C1N(C2=CC=C(F)C=C2)SC3=NC=CC=C31
MDL No. :N/A

Safety of PU139

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of PU139

epigenetics

Isoform Comparison

Biological Activity

Description
PU139 is a strong inhibitor of pan-histone acetyltransferase (HAT). It effectively inhibits the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP), and p300 with IC50 values of 8.39, 9.74, 2.49, and 5.35 μM, respectively [1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293 cells 2 µM 24 hours To evaluate the effect of PU139 on Smp14 promoter activity. PU139 significantly inhibited the SmCBP1- and SmGCN5-mediated transcriptional activity of the Smp14 promoter. PLoS Pathog. 2014 May 8;10(5):e1004116
HCT116 colon carcinoma cells 25 µM 3 hours Evaluate the effect of HAT inhibitors on histone acetylation levels, results showed PU139 decreased SAHA-induced H3K14 and H4K8 hyperacetylation. Oncogenesis. 2015 Feb 9;4(2):e137
SK-N-SH neuroblastoma cells 25 µM 3 hours Evaluate the effect of HAT inhibitors on histone acetylation levels, results showed PU139 decreased SAHA-induced H3K14 and H4K8 hyperacetylation. Oncogenesis. 2015 Feb 9;4(2):e137

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Schistosoma mansoni Adult worm pairs In vitro culture 20 µM Medium refreshed every 24 hours for 2-4 days To evaluate the effect of PU139 on Smp14 expression and egg development. PU139 significantly reduced Smp14 mRNA and protein levels, leading to abnormal egg morphology and defective eggshells. PLoS Pathog. 2014 May 8;10(5):e1004116
NMRI:nu/nu mice SK-N-SH neuroblastoma xenograft model Intraperitoneal injection 25 mg/kg Once per week for 24 days Evaluate the antitumor effect of PU139, results showed PU139 significantly reduced tumor volume (33%). Oncogenesis. 2015 Feb 9;4(2):e137

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.06mL

0.81mL

0.41mL

20.30mL

4.06mL

2.03mL

40.61mL

8.12mL

4.06mL

References

 

Historical Records

Categories