GSK J1
Tocris Bioscience, part of Bio-Techne | Catalog # 4593
Potent JMJD3/UTX inhibitor
Key Product Details
Description
Potent JMJD3/UTX inhibitor
Product Description
GSK J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A) (IC50 values are 28 and 53 nM respectively). Also inhibits KDM5B, KDM5C and KDM5A (IC50 values are 170, 550 and 6,800 nM respectively). Exhibits no activity against a panel of other histone demethylases (IC50 >20 μM), and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30 μM.Ethyl ester derivative and Negative Control also available.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK J1 probe summary on the SGC website.Product Specifications
Molecular Weight
389.45
Formula
C22H23N5O2
Storage
Desiccate at RT
Purity
≥98% (HPLC)
Chemical Name
N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
CAS Number
1373422-53-7
PubChem ID
56963315
InChI Key
AVZCPICCWKMZDT-UHFFFAOYSA-N
SMILES
O=C(CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1)O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.94 | 100 | |
| Ethanol | 38.94 | 100 |
Preparing Stock Solutions
for GSK J1
The following data is based on the product molecular weight 389.45
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.57 mL | 12.84 mL | 25.68 mL |
| 5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.57 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Heinemann Inhibition of demethylases by GSK-J1/J4. Nature 2014 PMID: 25279926
- Kruidenier A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 2012 PMID: 22842901
Product Specific Notices for GSK J1
For research use only
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