Art. -Nr.: HY-120290

PU141

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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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Reinheit: 99.96%
CAS. Nr.: 168334-34-7
Formel: C₁₄H₉F₃N₂OS
Molecular Weight:310.29

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PU141 Chemical Structure

CAS. Nr.: 168334-34-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CBP/p300^[1]

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	GI₅₀	4.12 μM Compound: 2, PU141	Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTS assay Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTS assay	10.1039/C4MD00245H
HL-60	GI₅₀	4.12 μM Compound: 68	Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CellTiter 96 Aqueous non-radioactive cell proliferation assay Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CellTiter 96 Aqueous non-radioactive cell proliferation assay	[PMID: 33045661]
LNCaP	GI₅₀	36.9 μM Compound: 2, PU141	Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay Cytotoxicity against human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay	10.1039/C4MD00245H
MCF7	GI₅₀	30.2 μM Compound: 8h	Growth inhibition of human MCF7 cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay Growth inhibition of human MCF7 cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay	[PMID: 21353783]
SK-N-SH	GI₅₀	0.48 μM Compound: 8h	Growth inhibition of human SK-N-SH cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay Growth inhibition of human SK-N-SH cells by CellTiter-96 Aqueous Non-radioactive cell proliferation assay	[PMID: 21353783]

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.

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.

Chemical Information

CAS. Nr. 168334-34-7
Appearance Solid
Molecular Weight 310.29
Formel C₁₄H₉F₃N₂OS
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2228 mL

16.1140 mL

32.2279 mL

5 mM

0.6446 mL

3.2228 mL

6.4456 mL

10 mM

0.3223 mL

1.6114 mL

3.2228 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. M Gajer,et al. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo. Oncogenesis.2015 Feb 9;4(2):e137. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PU141

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PU141 Related Classifications

HY-120290 Related Classifications