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GSK-J4

Cat. No. M5149
GSK-J4 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 130  USD130 In stock
5mg USD 80  USD80 In stock
10mg USD 120  USD120 In stock
25mg USD 250  USD250 In stock
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Quality Control & Documentation
Biological Activity

GSK-J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases.

Product Citations
Customer Product Validations & Biological Datas
Source Oncotarget (2018). Figure 4. GSK-J4
Method XTT assay
Cell Lines LNCaP and DU 145 cells
Concentrations 10 μM
Incubation Time 24 h, 48 h and 72 h
Results JMJD3 expression with GSK-J4 treatment was reduced by 61% for LNCaP and by around 20% for DU 145 and PC-3
Source Sci Transl Med (2018). Figure 4. GSK-J4 (Abmole Bioscience)
Method Seventy-two–hour Cell Titer-Glo assay
Cell Lines neuroblastoma cell lines
Concentrations 1 μM
Incubation Time 72 hours
Results The venetoclax/GSK-J4 combination suppressed the growth of several MYCN-amplified neuroblastoma cell lines, which was due to an increase in the induction of apoptosis by the combination compared to GSK-J4 or venetoclax single-agent therapy
Source Sci Transl Med (2018). Figure 3. GSK-J4 (Abmole Bioscience)
Method Cell viability assays
Cell Lines SH-SY5Y cells
Concentrations 1 μM
Incubation Time 6 days
Results Furthermore, the combination of RA and GSK-J4 induced both the differentiation marker CHD5 and several ER stress markers, including PUMA, after 6 days of treatment
Source Sci Transl Med (2018). Figure 2. GSK-J4 (Abmole Bioscience)
Method Western blot
Cell Lines neuroblastoma cell lines
Concentrations 1 μM
Incubation Time 72 hours
Results Consistent with a role for PUMA in GSK-J4–mediated efficacy, RNA-seq and Western blot analyses indicated induction of BBC3/PUMA, whereas knockdown of BBC3 by short hairpin–mediated RNA (shRNA) silencing protected cells from GSK-J4–induced apoptosis/necrosis
Source Sci Transl Med (2018). Figure 1. GSK-J4 (Abmole Bioscience)
Method cell viability assay
Cell Lines Neuroblastoma cell lines
Concentrations 1 μM
Incubation Time 72 hours
Results GSK-J4 delivered daily was sufficient to induce tumor regressions in the IMR32 model, completely block growth in the COG-N-561 PDX, and inhibit tumor growth in the FELIX PDX and CHLA20 models
Chemical Information
Molecular Weight 417.5
Formula C24H27N5O2
CAS Number 1373423-53-0
Solubility (25°C) DMSO 20 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] Kruidenier L, et al. Nature. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.

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


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