2. Epigenetics
  3. Histone Acetyltransferase
  4. PU139

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

PU139 Chemical Structure

CAS No. : 158093-65-3

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1 mg USD 71 In-stock
5 mg USD 150 In-stock
10 mg USD 260 In-stock
25 mg USD 560 In-stock
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Based on 1 publication(s) in Google Scholar

PU139 Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

GCN5

8.39 μM (IC50)

CREBBP

2.49 μM (IC50)

PCAF

9.74 μM (IC50)

p300

5.35 μM (IC50)

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.

PU139 Related Antibodies
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.
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
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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.14%

COA (247 KB) HNMR (223 KB) LCMS (103 KB)

Handling Instructions (2659 KB)
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 (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.

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
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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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