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GSK-J4 hydrochloride

Cat. No. M2731
GSK-J4 hydrochloride Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 84  USD84 In stock
10mg USD 118  USD118 In stock
25mg USD 240  USD240 In stock
50mg USD 420  USD420 In stock
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Quality Control & Documentation
Biological Activity

GSK J4 hydrochloride is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family.

Customer Product Validations & Biological Datas
Source Mol Cells (2018). Figure 4. GSK J4
Method qRT- PCR
Cell Lines THP-1 cells
Concentrations 5 μM
Incubation Time 48 h
Results To further determine the mechanisms underlying transcriptional regulation of p21 via KDM6B, we conducted luciferase reporter assay using p21-luciferase reporter system in HEK 293T cells. Ectopic expression of KDM6B accelerated p21 transcription (Fig. 4B), whereas KDM6B inhibition by GSK-J4 showed reduction of p21 expression
Chemical Information
Molecular Weight 453.96
Formula C24H27N5O2.HCl
CAS Number 1797983-09-5
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Robert Kleszcz, et al. The inhibitors of KDM4 and KDM6 histone lysine demethylases enhance the anti-growth effects of erlotinib and HS-173 in head and neck cancer cells

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Keywords: GSK-J4 hydrochloride supplier, Histone demethylase, inhibitors, activators


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