Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate
GSK-J4
CAS: 1373423-53-0
Molecular Formula: C24H27N5O2
Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate - Names and Identifiers
Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate - Physico-chemical Properties
| Molecular Formula | C24H27N5O2 |
| Molar Mass | 417.5 |
| Density | 1.216±0.06 g/cm3(Predicted) |
| Boling Point | 581.2±50.0 °C(Predicted) |
| Solubility | DMSO: ≥ 36 mg/mL |
| Appearance | Tan semi-solid |
| Color | white to beige |
| pKa | 5.95±0.10(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| In vitro study | GSK-J4 has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α). GSK-J4 (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels. GSK-J4 (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells. GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1. GSK-J4 inhibits H3K4 demethylation at Xist , Nodal , and HoxC13 in female embryonic stem cells. |
| In vivo study | GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice. GSK-J4 (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis. Animal Model: Eight-week-old male db/m and db/db mice Dosage: 10 mg/kg Administration: i.p.; thrice-weekly for 10 weeks Result: Attenuated the development of kidney disease in diabetic mice. |
Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.395 ml | 11.976 ml | 23.952 ml |
| 5 mM | 0.479 ml | 2.395 ml | 4.79 ml |
| 10 mM | 0.24 ml | 1.198 ml | 2.395 ml |
| 5 mM | 0.048 ml | 0.24 ml | 0.479 ml |
Last Update：2024-01-02 23:10:35
Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate - Reference Information
| biological activity | GSK-J4 is an effective H3K27me3/me2 demethylase JMJD3/KDM6B and UTX/KDM6A double inhibitor, IC50 is 8.6 μM and 6.6 μM respectively. GSK-J4 inhibited LPS-induced TNF-α production by human primary macrophages with an IC50 value of 9 μM. GSK-J4 are GSK-J1 cell permeability prodrugs. GSK-J4 induces endoplasmic reticulum stress-related apoptosis (apoptosis). |
| target | IC50: 8.6 µM (JMJD3/KDM6B), 6.6 µM (UTX/KDM6A) |
| in vitro study | GSK-J4 has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α). GSK-J4 (5 μM; 48 hours) cause a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels. GSK-J4 (10, 25 nm) ACTS upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells. GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1. GSK-J4 inhibits H3K4 demethylation at Xist , Nodal , and HoxC13 in female embryonic stem cells. |
| in vivo study | GSK-J4 Hydrochloride (10 mg/kg; I. p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice. GSK-J4 (0.5 mg/kg, I. p.) significantly reduces the severity and the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis. Animal Model: Eight-week-old male db/m and db/db mice Dosage: 10 mg/kg Administration: I. p.; Thrice-weekly for 10 weeks result: attenuated the development of kidney disease in diabetic mice. |
| Animal Model: | Eight-week-old male db/m and db/db mice |
| Dosage: | 10 mg/kg |
| Administration: | I .p.; thrice-weekly for 10 weeks |
| Result: | Attenuated the development of kidney disease in diabetic mice. |
Last Update：2024-04-09 21:54:55
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CAS: 1373423-53-0
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Product Name: GSK-J4 Visit Supplier Webpage Request for quotation
CAS: 1373423-53-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1373423-53-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate