ChemicalBook > CAS DataBase List > GSK-J4 Hydrochloride

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

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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