PU139

Name: PU139
Brand: MedChemExpress
SKU: HY-124696
Rating: 5.0 (3 reviews)

Cat. No.: HY-124696 Purity: 99.51%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC₅₀s of 8.39, 9.74, 2.49 and 5.35 μM, respectively.

For research use only. We do not sell to patients.

PU139 Chemical Structure

CAS No. : 158093-65-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
250 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE PU139

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

GCN5

8.39 μM (IC₅₀)

CREBBP

2.49 μM (IC₅₀)

PCAF

9.74 μM (IC₅₀)

p300

5.35 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	GI₅₀	3.42 μM Compound: 1, PU139	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	3.42 μM Compound: 67	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	36.2 μM Compound: 1, PU139	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	37.2 μM Compound: 4d	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]
Sf9	IC₅₀	10 μM Compound: PU139	Inhibition of recombinant human N-terminal His-GST-tagged p300 (965 to 1810 residues) expressed in baculovirus infected Sf9 insect cells preincubated for 10 mins in presence of biotinylated-histone H3/H4 followed by acetyl-CoA addition and measured after Inhibition of recombinant human N-terminal His-GST-tagged p300 (965 to 1810 residues) expressed in baculovirus infected Sf9 insect cells preincubated for 10 mins in presence of biotinylated-histone H3/H4 followed by acetyl-CoA addition and measured after	[PMID: 31910017]
SK-N-SH	GI₅₀	10.3 μM Compound: 4d	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

PU139 inhibits cell growth with GI₅₀s of <60 μM (A431, A549, A2780, HepG2, SW480, U-87 MG, HCT116 and SK-N-SH and MCF7 cells)^[1].
PU139 (0-100 μM; 24-72 hours) triggers caspase-independent cell death in the neuroblastoma cell line SK-N-SH^[1].

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

In Vivo

PU139 (25 mg/kg; i.p.) synergizes with Doxorubicin used as a prototypic chemotherapeutic drug in growth inhibition^[1].

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

Animal Model:	Male NMRI:nu/nu mice (Neuroblastoma xenografts)^[1]
Dosage:	25 mg/kg
Administration:	Intraperitoneally (PU139) with Dxorubicin at 8 mg/kg i.v.; Administered on days 14 and 21 as a single dose of each compound or, for combination therapy; both drugs were administered successively within 1 h.
Result:	Optimum growth inhibition following a single PU139 therapy was moderate, but significant as compared with the untreated group and confirmed the previous findings.

Molecular Weight

246.26

Formula

C₁₂H₇FN₂OS

CAS No.

158093-65-3

Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1N(C2=CC=C(F)C=C2)SC3=NC=CC=C31

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (40.61 mM; ultrasonic and warming and heat to 60°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	4.0607 mL	20.3037 mL	40.6075 mL
5 mM	0.8121 mL	4.0607 mL	8.1215 mL
10 mM	0.4061 mL	2.0304 mL	4.0607 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 (sealed storage, away from moisture). 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 1 mg/mL (4.06 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: 1 mg/mL (4.06 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

This protocol yields a clear solution of 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 99.51%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (248 KB) HNMR (132 KB) RP-HPLC (304 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

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

[2]. Carneiro VC, et al. Epigenetic changes modulate schistosome egg formation and are a novel target for reducing transmission of schistosomiasis. PLoS Pathog. 2014;10(5):e1004116. Published 2014 May 8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.0607 mL	20.3037 mL	40.6075 mL	101.5187 mL
	5 mM	0.8121 mL	4.0607 mL	8.1215 mL	20.3037 mL
	10 mM	0.4061 mL	2.0304 mL	4.0607 mL	10.1519 mL
	15 mM	0.2707 mL	1.3536 mL	2.7072 mL	6.7679 mL
	20 mM	0.2030 mL	1.0152 mL	2.0304 mL	5.0759 mL
	25 mM	0.1624 mL	0.8121 mL	1.6243 mL	4.0607 mL
	30 mM	0.1354 mL	0.6768 mL	1.3536 mL	3.3840 mL
	40 mM	0.1015 mL	0.5076 mL	1.0152 mL	2.5380 mL

PU139 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:

PU139158093-65-3PU 139PU-139Histone AcetyltransferaseHATsHATneuroblastomacellgrowthanticancerhistoneInhibitorinhibitorinhibit

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PU139

Customer Review

PU139 Related Antibodies

3 Publications Citing Use of MCE PU139

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Acetyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

PU139 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PU139 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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