1. Epigenetics
    Apoptosis
  2. Epigenetic Reader Domain
    Apoptosis
  3. GSK2801

GSK2801 

Cat. No.: HY-15658 Purity: 99.93%
Handling Instructions

GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.

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

GSK2801 Chemical Structure

GSK2801 Chemical Structure

CAS No. : 1619994-68-1

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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 88 In-stock
Estimated Time of Arrival: December 31
Solid
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
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Description

GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4[1].

IC50 & Target

Kd: 136 nM (BAZ2A) and 257 nM (BAZ2B)[1]

In Vitro

GSK2801 binds TAF1L(2) with an affinity KB of 0.31μM (KD: 3.2 μM) and a binding enthalpy change ΔH of −8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity KB of 0.826 μM (KD: 1.1 μM) and ΔH of −9.8 kcal/mol[1].
GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC[2].

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

In Vivo

In order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability[1].

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

Molecular Weight

371.45

Formula

C₂₀H₂₁NO₄S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    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

  • 3.

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

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.93%

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