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Chemical Structure| 1373422-53-7 Chemical Structure| 1373422-53-7

Structure of GSK-J1
CAS No.: 1373422-53-7

Chemical Structure| 1373422-53-7

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GSK-J1 is a H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM for JMJD3 (KDM6B) and UTX (KDM6A), respectively.

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Product Details of GSK-J1

CAS No. :1373422-53-7
Formula : C22H23N5O2
M.W : 389.45
SMILES Code : O=C(O)CCNC1=NC(C2=NC=CC=C2)=NC(N3CCC4=CC=CC=C4CC3)=C1
MDL No. :MFCD22683851
InChI Key :AVZCPICCWKMZDT-UHFFFAOYSA-N
Pubchem ID :56963315

Safety of GSK-J1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GSK-J1

epigenetics

Isoform Comparison

Biological Activity

Target
  • KDM6

    JMJD3, IC50:60 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse mammary epithelial cells (MECs) 0.1 μM, 1 μM, 10 μM 18 hours To evaluate the cytotoxicity of GSK-J1 on mouse mammary epithelial cells, the results showed significant cytotoxicity at 100 μM, so 0.1 μM, 1 μM, and 10 μM were chosen for subsequent experiments. PMC9168612
Cal27 cells 20 μM 48 hours GSK-J1 in combination with TCP significantly induced cell apoptosis and senescence, and inhibited cell proliferation. PMC7028736
FaDu cells 15 μM 48 hours GSK-J1 in combination with TCP significantly induced cell apoptosis and senescence, and inhibited cell proliferation. PMC7028736
MCF7 20 μM 72 hours To evaluate the effect of GSK-J1 on breast cancer cell growth, results showed that the growth inhibitory concentration of GSK-J4 on MCF7 cells was 0.9–1.0 μM. PMC4742734
MDA-MB231 20 μM 72 hours To evaluate the effect of GSK-J1 on breast cancer cell growth, results showed that the growth inhibitory concentration of GSK-J4 on MDA-MB231 cells was 2.9 μM. PMC4742734
mouse mammary epithelial cells (MECs) 0.1 μM, 1 μM, 10 μM To evaluate the effect of GSK-J1 on the expression of inflammatory factors in LPS-stimulated mouse mammary epithelial cells, the results showed that GSK-J1 significantly reduced the expression of Tnfa, Il1b, and Il6. PMC9168612

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice 4NQO-induced HNSCC model and xenograft model Intraperitoneal injection 25 mg/kg 5 days a week for 3 weeks GSK-J1 in combination with TCP significantly inhibited tumor growth and progression, reducing tumor volume and weight. PMC7028736
BALB/c mice LPS-induced mastitis model intraperitoneal injection 1 mg/kg Single dose, lasting 24 hours To evaluate the effect of GSK-J1 on the inflammatory response in the mammary tissue of LPS-induced mastitis model mice, the results showed that GSK-J1 significantly alleviated the inflammatory response in the mammary tissue, reducing inflammatory cell infiltration and the expression of inflammatory factors. PMC9168612
Rats Sleep-wake cycle model Intraperitoneal injection 0.1, 1.0, or 10 mg/kg Single injection, lasting 4 hours GSK-J1, when administered during the dark phase, reduced wakefulness, increased slow wave sleep and rapid eye movement sleep time, and decreased levels of sleep-related neurochemicals PMC6428769

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.84mL

2.57mL

1.28mL

25.68mL

5.14mL

2.57mL

References

 

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