2. Epigenetics
  3. Histone Acetyltransferase
  4. PU141

PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.

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PU141 Chemical Structure

PU141 Chemical Structure

CAS No. : 168334-34-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 170 In-stock
Solution
10 mM * 1 mL in DMSO USD 170 In-stock
Solid
5 mg USD 155 In-stock
10 mg USD 250 In-stock
25 mg USD 505 In-stock
50 mg USD 810 In-stock
100 mg USD 1300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PU141 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity[1].

IC50 & Target

CBP/p300[1]
In Vitro

PU141 inhibits cell growth at micromolar concentrations in A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma)[1].
PU141 causes both histone hypoacetylation and growth inhibition in vitro. PU141 (25 µM) leads to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation, whereas H3K9 and H4K16 acetylation levels remaine stable after co-treatment of HDAC and HAT inhibitor. The impact on histone acetylation is similar in both SK-N-SH and HCT116 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PU141 Related Antibodies

Cell Viability Assay[1]

Cell Line: A431 (epidemoid carcinoma), A549 (alveolar basal epithelial adenocarcinoma), A2780 (ovarian carcinoma), HCT116 (epithelial colon carcinoma), HepG2 (hepatocellular carcinoma), MCF7 (breast carcinoma), SK-N-SH (neuroblastoma), SW480 (colon adenocarcinoma) and U-87MG (epithelial-like glioblastoma-astrocytoma)
Concentration: 0, 10, 20, 30, 40, 50, and 60 µM
Incubation Time:
Result: Inhibited cell growth at micromolar concentrations in all screened cell lines. The highest cellular antiproliferative activity was detected for the neuroblastoma SK-N-SH cell line.

Western Blot Analysis[1]

Cell Line: SK-N-SH neuroblastoma and HCT116 colon carcinoma cells
Concentration: 25 µM
Incubation Time: 3 hours
Result: Led to a decrease in SAHA-induced H3K14 and H4K8 hyperacetylation.
In Vivo

PU141 (25 mg/kg; administered once intraperitoneally for 24 days) exhibits a significant antitumor effects against neuroblastoma xenografts in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male NMRI:nu/nu mice bearing a xenograft model[1]
Dosage: 12.5 and 25 mg/kg
Administration: Administered once intraperitoneally (i.p.) as a detergent containing saline microemulsion; for 24 days
Result: Led to significant tumor volume reduction (19%) at 25 mg/kg.
Molecular Weight

310.29

Formula

C14H9F3N2OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(SC2=NC=CC=C21)CC3=CC=C(C=C3)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (322.28 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2228 mL 16.1140 mL 32.2279 mL
5 mM 0.6446 mL 3.2228 mL 6.4456 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 5 mg/mL (16.11 mM); Clear solution; Need ultrasonic and warming and heat to 80°C

    This protocol yields a clear solution of 5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 5 mg/mL (16.11 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2228 mL 16.1140 mL 32.2279 mL 80.5698 mL
5 mM 0.6446 mL 3.2228 mL 6.4456 mL 16.1140 mL
10 mM 0.3223 mL 1.6114 mL 3.2228 mL 8.0570 mL
15 mM 0.2149 mL 1.0743 mL 2.1485 mL 5.3713 mL
20 mM 0.1611 mL 0.8057 mL 1.6114 mL 4.0285 mL
25 mM 0.1289 mL 0.6446 mL 1.2891 mL 3.2228 mL
30 mM 0.1074 mL 0.5371 mL 1.0743 mL 2.6857 mL
40 mM 0.0806 mL 0.4028 mL 0.8057 mL 2.0142 mL
50 mM 0.0645 mL 0.3223 mL 0.6446 mL 1.6114 mL
60 mM 0.0537 mL 0.2686 mL 0.5371 mL 1.3428 mL
80 mM 0.0403 mL 0.2014 mL 0.4028 mL 1.0071 mL
100 mM 0.0322 mL 0.1611 mL 0.3223 mL 0.8057 mL
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PU141 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PU141168334-34-7PU 141PU-141Histone AcetyltransferaseHATsHATp300 HATCBP/p300 selectivityKAT3-selective inhibitorpyridoisothiazoloneanticancerInhibitorinhibitorinhibit

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