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GSK J4 HCl

GSK J4 HCl structure

CAS No.: 1373423-53-0

Chemical Name:: GSK J4 HCl

Synonyms: GSK-J4;GSK J4;CS-1667;CS-2143;GSK J4 HCl;6-Triiodophenol;GSK J4 free base;GSKJ4HCL(free base);GSK J4 HCl USP/EP/BP;GSK J4 HCl (GSKJ4 HCl)

CBNumber:: CB62665155

Molecular Formula:: C24H27N5O2

Molecular Weight:: 417.5

MDL Number:: MFCD22683852

MOL File:: 1373423-53-0.mol

MSDS File:: SDS

Last updated:2023-06-30 15:45:59

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GSK J4 HCl Properties

Boiling point	581.2±50.0 °C(Predicted)
Density	1.216±0.06 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO: soluble20mg/mL, clear
pka	5.95±0.10(Predicted)
form	Tan semi-solid
color	white to beige
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.
InChIKey	WBKCKEHGXNWYMO-UHFFFAOYSA-N

SAFETY

Risk and Safety Statements

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H319-H315-H335
Precautionary statements	P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P
Hazard Codes	Xi
Risk Statements	36/37/38
Safety Statements	26
WGK Germany	3

GSK J4 HCl price More Price(16)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Sigma-Aldrich	SML0701	GSK-J4 ≥98% (HPLC)	1373423-53-0	5mg	$117	2024-03-01	Buy
Sigma-Aldrich	420205	Histone Lysine Demethylase Inhibitor VIII, GSK-J4	1373423-53-0	10mg	$245	2024-03-01	Buy
Sigma-Aldrich	SML0701	GSK-J4 ≥98% (HPLC)	1373423-53-0	25mg	$469	2024-03-01	Buy
Tocris	4594	GSKJ4 ≥99%(HPLC)	1373423-53-0	50	$876	2021-12-16	Buy
TRC	G797555	GSKJ4	1373423-53-0	10mg	$165	2021-12-16	Buy

Product number	Packaging	Price	Buy
SML0701	5mg	$117	Buy
420205	10mg	$245	Buy
SML0701	25mg	$469	Buy
4594	50	$876	Buy
G797555	10mg	$165	Buy

GSK J4 HCl Chemical Properties,Uses,Production

Description

GSK-J4 (1373423-53-0) is a histone demethylase JMJD3/UTX inhibitor. Inhibits demethylation of histone H3K27. Reduces LPS-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable, ethyl ester of GSK J1 (cat.# 10-1393).1 GSK-J4 rescues newborn pups from embryonic lethality in BRAF knockin mice which recapitulate major features of RASopathies.2

Uses

GSK-J4 has been used to study the effect of KDM2B (Jumonji (JmjC) domain histone 3 lysine 36 (H3K36) di-demethylase) inhibition on the survival and DNA repair potential of glioblastoma cells. It has also been used in sulforhodamine B (SRB) cell growth assay and cell viability assay.

Definition

ChEBI: 3-[[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)-4-pyrimidinyl]amino]propanoic acid ethyl ester is an organonitrogen heterocyclic compound.

Biochem/physiol Actions

GSK-J4 is cell permeable prodrug rapidly hydrolysed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. 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. The prodrug 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. For characterization details for GSK-J4 and full characterization details for GSK-J1, please visit the GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

storage

Room temperature

References

1) Kruidenier et al. (2012), Selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404 2) Inoue et al. (2014) New Braf knockin mice provide a pathogenic mechanism of developmental defects and therapeutic approach in cardio-facio-cutaneous syndrome; Hum. Mol. Genet.,?23?6553

GSK J4 HCl synthesis

Synthesis of GSK J4 HCl from 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINE and ethyl 3-((6-chloro-2-(pyridin-2-yl)pyriMidin-4-yl)aMino)propanoate

GSK J4 HCl Preparation Products And Raw materials

Raw materials

ethyl 3-((6-chloro-2-(pyridin-2-yl)pyriMidin-4-yl)aMino)propanoate 4,6-DICHLORO-2-(2-PYRIDINYL)PYRIMIDINE 2,3,4,5-TETRAHYDRO-1H-BENZO[D]AZEPINE

Preparation Products

GSK J4 HCl Suppliers

Global( 114)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9348	55
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
career henan chemical co	+86-0371-86658258 15093356674;	factory@coreychem.com	China	29826	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	1026@dideu.com	China	29220	58
Chemia Biotechnology（Shanghai） Co., Ltd	+8613816753574	info@chemia-pharm.com	CHINA	311	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10523	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58

Supplier	Advantage
ATK CHEMICAL COMPANY LIMITED	60
Hangzhou FandaChem Co.,Ltd.	55
Biochempartner	58
Hubei Jusheng Technology Co.,Ltd.	58
career henan chemical co	58
HANGZHOU CLAP TECHNOLOGY CO.,LTD	58
Dideu Industries Group Limited	58
Chemia Biotechnology（Shanghai） Co., Ltd	58
Zhejiang J&C Biological Technology Co.,Limited	58
InvivoChem	58

GSK-J4 HCl: Mechanism And Bioactivity studies
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases?JMJD3/KDM6B?and?UTX/KDM6A?with?IC50s of 8.6 and 6.6 μM, respect....
Jan 5，2023

View Lastest Price from GSK J4 HCl manufacturers

Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2019-12-24	ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate 1373423-53-0	US $1.00 / KG	1KG	Min98% HPLC	g/kg/ton	Career Henan Chemical Co

ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
1373423-53-0
US $1.00 / KG
Min98% HPLC
Career Henan Chemical Co

GSK J4 HCl Spectrum

GSK J4 HCl(1373423-53-0)¹HNMR

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GSK J4 N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine ethyl ester GSK J4 HCl N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyriMidinyl]-|-alanine ethyl ester β-Alanine, N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-, ethyl ester, hydrochloride (1:1) Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)prop Histone Lysine Demethylase Inhibitor VIII, GSK-J4 ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate CS-2143 CS-1667 H3K27 histone demethylase inhibitor J4 HCl Histone Lysine Demethylase Inhibitor VIII, GSK-J4 - CAS 1373423-53-0 - Calbiochem GSK J4 free base GSKJ4HCL(free base) β-Alanine, N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-, ethyl ester GSK J4 HCl USP/EP/BP GSK J4 HCl (GSKJ4 HCl) 6-Triiodophenol GSK-J4 1373423-53-0 C24H27N5O2HCl Inhibitor Inhibitors API