2. Epigenetics
  3. Epigenetic Reader Domain
  4. GSK8814

GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1.

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GSK8814 Chemical Structure

GSK8814 Chemical Structure

CAS No. : 1997369-78-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 506 In-stock
Solution
10 mM * 1 mL in DMSO USD 506 In-stock
Solid
5 mg USD 460 In-stock
10 mg USD 780 In-stock
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Based on 1 publication(s) in Google Scholar

GSK8814 Related Antibodies

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Description

GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1[1].

IC50 & Target

ATAD2

8.9 (pKi)

ATAD2

8 nM (Ki)

BRD4 BD1

4.6 (pIC50)

Molecular Weight

527.61

Formula

C28H35F2N5O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC2=C(N[C@H]3[C@H](OCC4CCC(F)(F)CC4)CNC[C@@H]3OC)N=CC(C5=CC(C)=CN=C5)=C2C=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (189.53 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 1.8953 mL 9.4767 mL 18.9534 mL
5 mM 0.3791 mL 1.8953 mL 3.7907 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. 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)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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

Purity: 99.60% ee.: 98.99%

COA (255 KB) HNMR (218 KB) CNMR (397 KB) RP-HPLC (264 KB) NP-HPLC (230 KB) LCMS (268 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. 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 1.8953 mL 9.4767 mL 18.9534 mL 47.3835 mL
5 mM 0.3791 mL 1.8953 mL 3.7907 mL 9.4767 mL
10 mM 0.1895 mL 0.9477 mL 1.8953 mL 4.7383 mL
15 mM 0.1264 mL 0.6318 mL 1.2636 mL 3.1589 mL
20 mM 0.0948 mL 0.4738 mL 0.9477 mL 2.3692 mL
25 mM 0.0758 mL 0.3791 mL 0.7581 mL 1.8953 mL
30 mM 0.0632 mL 0.3159 mL 0.6318 mL 1.5794 mL
40 mM 0.0474 mL 0.2369 mL 0.4738 mL 1.1846 mL
50 mM 0.0379 mL 0.1895 mL 0.3791 mL 0.9477 mL
60 mM 0.0316 mL 0.1579 mL 0.3159 mL 0.7897 mL
80 mM 0.0237 mL 0.1185 mL 0.2369 mL 0.5923 mL
100 mM 0.0190 mL 0.0948 mL 0.1895 mL 0.4738 mL
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GSK8814 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:

GSK88141997369-78-4GSK 8814GSK-8814Epigenetic Reader DomainprobeselectivecanceranalogInhibitorinhibitorinhibit

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