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GSK-J4 Hydrochloride

Product Name
GSK-J4 Hydrochloride
CAS No.
1797983-09-5
Chemical Name
GSK-J4 Hydrochloride
Synonyms
1797983-09-5 (HCl);GSK-J4 Hydrochloride;TYXWLTBYINKVNT-UHFFFAOYSA-N;GSK-J4 Hydrochloride, 10 mM in DMSO;Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride;Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate hydrochloride;Histone Demethylase,diabetic,Th17,mice,cells,inflammation,Th1,H3K27me3/me2,dendritic,GSKJ4 Hydrochloride,TGF-β,inhibit,Inhibitor,GSK J4 Hydrochloride,demethylase,GSK-J4,GSK-J-4 Hydrochloride
CBNumber
CB12700565
Molecular Formula
C24H28ClN5O2
Formula Weight
453.96442
MOL File
1797983-09-5.mol
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GSK-J4 Hydrochloride Property

storage temp. 
under inert gas (nitrogen or Argon) at 2-8°C
solubility 
DMSO:60.83(Max Conc. mg/mL);134.0(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:7):0.1(Max Conc. mg/mL);0.22(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);66.08(Max Conc. mM)
Ethanol:55.0(Max Conc. mg/mL);121.15(Max Conc. mM)
Water:10.0(Max Conc. mg/mL);22.03(Max Conc. mM)
form 
A crystalline solid
color 
Light yellow to yellow
InChIKey
TYXWLTBYINKVNT-UHFFFAOYSA-N
SMILES
c1(N2CCc3ccccc3CC2)cc(NCCC(=O)OCC)nc(-c2ncccc2)n1.Cl
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H290May be corrosive to metals

H314Causes severe skin burns and eye damage

Precautionary statements

P234Keep only in original container.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P330+P331IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P363Wash contaminated clothing before reuse.

P390Absorb spillage to prevent material damage.

P405Store locked up.

P406Store in corrosive resistant/… container with a resistant inner liner.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
12073
Product name
GSK-J4 (hydrochloride)
Purity
≥95%
Packaging
5mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
12073
Product name
GSK-J4(hydrochloride)
Purity
≥98%
Packaging
25mg
Price
$179
Updated
2024/03/01
Cayman Chemical
Product number
12073
Product name
GSK-J4 (hydrochloride)
Purity
≥95%
Packaging
1mg
Price
$25
Updated
2021/12/16
Cayman Chemical
Product number
12073
Product name
GSK-J4 (hydrochloride)
Purity
≥95%
Packaging
10mg
Price
$107
Updated
2024/03/01
Cayman Chemical
Product number
12073
Product name
GSK-J4 (hydrochloride)
Purity
≥95%
Packaging
50mg
Price
$302
Updated
2024/03/01
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GSK-J4 Hydrochloride Chemical Properties,Usage,Production

Description

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer. GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 with an IC50 value greater than 50 μM in vitro. Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 μM).

Uses

GSK-J4 Hydrochloride is a histone demethylase JMJD3/UTX inhibitors which blocks demethylation of histone H3K27.

in vivo

GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice[2].
GSK-J4 Hydrochloride (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[3].

Animal Model:Eight-week-old male db/m and db/db mice on a BKS background[2]
Dosage:10 mg/kg
Administration:i.p.; thrice-weekly for 10 weeks
Result:Attenuated the development of kidney disease in diabetic mice.

IC 50

KDM6

References

[1] KARL AGGER. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development[J]. Nature, 2007, 449 7163: 731-734. DOI: 10.1038/nature06145
[2] M R HüBNER  D L S. Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulation.[J]. Cold Spring Harbor symposia on quantitative biology, 2010: 43-49. DOI: 10.1101/sqb.2010.75.020
[3] LAURENS KRUIDENIER. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response[J]. Nature, 2012, 488 7411: 404-408. DOI: 10.1038/nature11262
[4] BO YANG. Reepithelialization of Diabetic Skin and Mucosal Wounds Is Rescued by Treatment With Epigenetic Inhibitors.[J]. Diabetes, 2024: 120-134. DOI: 10.2337/db23-0258

GSK-J4 Hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK-J4 Hydrochloride Suppliers

Canada 1 China 68 India 1 United States 8 Global 78
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
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Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
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Tianjin Kailiqi Biotechnology Co., Ltd.
Tel
15076683720
Fax
022-23754520
Email
klq@cw-bio.com
Country
China
ProdList
8011
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Beijing Solarbio Science & Tecnology Co., Ltd.
Tel
010-50973130 18101056239
Email
3193328036@qq.com
Country
China
ProdList
29760
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Amadis Chemical Company Limited
Tel
571-89925085
Fax
0086-571-89925065
Email
sales@amadischem.com
Country
China
ProdList
131957
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58
Shanghai Hongye Biotechnology Co. Ltd
Tel
400-9205774
Email
sales@glpbio.cn
Country
China
ProdList
6777
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InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
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United States
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6391
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HANGZHOU CLAP TECHNOLOGY CO.,LTD
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86-571-88216897,88216896 13588875226
Fax
86-571-88216895
Email
sales@hzclap.com
Country
CHINA
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
Tel
18818260767
Fax
QQ 3610331285
Email
sales@chemegen.com
Country
China
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Shanghai hongqu biomedical technology co. LTD
Tel
88888888888
Email
hongquchem@qq.com
Country
China
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5132
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58

1797983-09-5, GSK-J4 Hydrochloride Related Search:


  • GSK-J4 Hydrochloride
  • TYXWLTBYINKVNT-UHFFFAOYSA-N
  • Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride
  • 1797983-09-5 (HCl)
  • Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate hydrochloride
  • Histone Demethylase,diabetic,Th17,mice,cells,inflammation,Th1,H3K27me3/me2,dendritic,GSKJ4 Hydrochloride,TGF-β,inhibit,Inhibitor,GSK J4 Hydrochloride,demethylase,GSK-J4,GSK-J-4 Hydrochloride
  • GSK-J4 Hydrochloride, 10 mM in DMSO
  • 1797983-09-5
  • 797983-09-5