1. Epigenetics
  2. Epigenetic Reader Domain

GSK2801 

Cat. No.: HY-15658 Purity: 99.73%
Handling Instructions

GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains.

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

GSK2801 Chemical Structure

GSK2801 Chemical Structure

CAS No. : 1619994-68-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 400 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains. IC50 value: 136 nM/257 nM(Kd, BAZ2A/BAZ2B) [1] Target: BAZ2A/2B inhibitor GSK2801 binds to BAZ2 bromodomains with dissociation constants (KD) of 136 and 257 nM for BAZ2B and BAZ2A, respectively. Crystal structures demonstrated a canonical acetyl-lysine competitive binding mode. Cellular activity was demonstrated using fluorescent recovery after photobleaching (FRAP) monitoring displacement of GFP-BAZ2A from acetylated chromatin. A pharmacokinetic study in mice showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability. Thus, GSK2801 represents a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology.

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (134.61 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6922 mL 13.4608 mL 26.9215 mL
5 mM 0.5384 mL 2.6922 mL 5.3843 mL
10 mM 0.2692 mL 1.3461 mL 2.6922 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.73 mM); Suspended solution; Need ultrasonic and warming

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (6.73 mM); Clear solution; Need warming

References
Molecular Weight

371.45

Formula

C₂₀H₂₁NO₄S

CAS No.

1619994-68-1

SMILES

O=C(C)C1=CC(C2=C(S(=O)(C)=O)C=CC=C2)=C3N1C=CC(OCCC)=C3

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

Room temperature in continental US; may vary elsewhere

Purity: 99.73%

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Product Name:
GSK2801
Cat. No.:
HY-15658
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GSK2801

Cat. No.: HY-15658