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GSK-J4

Cat. No. M5149
GSK-J4 Structure
Size Price Availability Quantity
10mM/1mL 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
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 417.5
Formula C24H27N5O2
CAS Number 1373423-53-0
Purity >98%
Solubility DMSO 20 mg/mL
Storage at -20°C
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 demethylases, inhibitors

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