2. Epigenetics
  3. Epigenetic Reader Domain Histone Acetyltransferase
  4. GSK 4027

GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

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GSK 4027 Chemical Structure

GSK 4027 Chemical Structure

CAS No. : 2079896-25-4

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Based on 1 publication(s) in Google Scholar

Other Forms of GSK 4027:

GSK 4027 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK 4027

View All Histone Acetyltransferase Isoform Specific Products:

View All Isoforms
CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

IC50 & Target

GCN5/PCAF

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
60 nM
Compound: (R,R)-32; GSK4027
Displacement of Halo-tagged histone H3.3 from NanoLuc-tagged full length human PCAF bromodomain expressed in HEK293 cells after 18 hrs by NanoBRET assay
Displacement of Halo-tagged histone H3.3 from NanoLuc-tagged full length human PCAF bromodomain expressed in HEK293 cells after 18 hrs by NanoBRET assay
[PMID: 28002667]
In Vitro

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. GSK 4027 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 5.1±0.08, respectively. The selectivity of GSK 4027 against the wider bromodomain family is assessed in the BROMOscan panel with pKi of 8.9 and 8.9 for PCAF and GCN5, respectively. GSK 4027 shows equipotent activity against PCAF and GCN5 with Ki of 1.4 nM for both bromodomains. As expected due to the encouraging measured artificial membrane permeability (500 nm/s), treatment of HEK293 cells with GSK 4027 displace full length PCAF from histone H3.3 with little drop-off from the biochemical assay and a pIC50 7.2 (IC50 60 nM)[1].

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

GSK 4027 Related Antibodies
Molecular Weight

377.28

Formula

C17H21BrN4O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

BrC1=C(N[C@@H]2C[C@H](C3=CC=CC=C3)CN(C)C2)C=NN(C)C1=O
Shipping

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

DMSO : 50 mg/mL (132.53 mM; Need ultrasonic; 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 2.6506 mL 13.2528 mL 26.5055 mL
5 mM 0.5301 mL 2.6506 mL 5.3011 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6506 mL 13.2528 mL 26.5055 mL 66.2638 mL
5 mM 0.5301 mL 2.6506 mL 5.3011 mL 13.2528 mL
10 mM 0.2651 mL 1.3253 mL 2.6506 mL 6.6264 mL
15 mM 0.1767 mL 0.8835 mL 1.7670 mL 4.4176 mL
20 mM 0.1325 mL 0.6626 mL 1.3253 mL 3.3132 mL
25 mM 0.1060 mL 0.5301 mL 1.0602 mL 2.6506 mL
30 mM 0.0884 mL 0.4418 mL 0.8835 mL 2.2088 mL
40 mM 0.0663 mL 0.3313 mL 0.6626 mL 1.6566 mL
50 mM 0.0530 mL 0.2651 mL 0.5301 mL 1.3253 mL
60 mM 0.0442 mL 0.2209 mL 0.4418 mL 1.1044 mL
80 mM 0.0331 mL 0.1657 mL 0.3313 mL 0.8283 mL
100 mM 0.0265 mL 0.1325 mL 0.2651 mL 0.6626 mL
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GSK 4027 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:

GSK 40272079896-25-4GSK4027GSK-4027Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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