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Merck

SML0701

GSK-J4

≥98% (HPLC), jumonji H3K27 demethylase inhibitor, powder

동의어(들):

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C24H27N5O2
CAS 번호:
1373423-53-0
Molecular Weight:
417.50
UNSPSC Code:
51111800
PubChem Substance ID:
329825585
NACRES:
NA.77
MDL number:
MFCD22683852

주요 문서

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제품 이름

GSK-J4, ≥98% (HPLC)

SMILES string

O=C(OCC)CCNC1=CC(N2CCC(C=CC=C3)=C3CC2)=NC(C4=CC=CC=N4)=N1

InChI key

WBKCKEHGXNWYMO-UHFFFAOYSA-N

InChI

1S/C24H27N5O2/c1-2-31-23(30)10-14-26-21-17-22(28-24(27-21)20-9-5-6-13-25-20)29-15-11-18-7-3-4-8-19(18)12-16-29/h3-9,13,17H,2,10-12,14-16H2,1H3,(H,26,27,28)

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

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관련 카테고리

Application

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.

Biochem/physiol Actions

GSK-J4 is a potent selective jumonji H3K27 demethylase inhibitor.
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

Features and Benefits

GSK-J4 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Other Notes

GSK-J4 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK-J4 probe summary on the Chemical Probes Portal website.

저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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시험 성적서(COA)

Lot/Batch Number
0000215863
0000215864
0000215863
0000215864
0000193051

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문서 라이브러리 방문

Targeting glioma stem?like cell survival and chemoresistance through inhibition of lysine?specific histone demethylase KDM2B.
Staberg M, et al.
Molecular Oncology, 12(3), 406-420 (2018)
Natalia Pediconi et al.
Cell death & disease, 10(7), 518-518 (2019-07-10)
Modification of histones by lysine methylation plays a role in many biological processes, and it is dynamically regulated by several histone methyltransferases and demethylases. The polycomb repressive complex contains the H3K27 methyltransferase EZH2 and controls dimethylation and trimethylation of H3K27
Inhibitor of H3K27 demethylase JMJD3/UTX GSK-J4 is a potential therapeutic option for castration resistant prostate cancer.
Morozov V M, et al.
Oncotarget, 8(37), 62131-62131 (2017)
Cristian Doñas et al.
Journal of autoimmunity, 75, 105-117 (2016-08-17)
As it has been established that demethylation of lysine 27 of histone H3 by the lysine-specific demethylase JMJD3 increases immune responses and thus elicits inflammation, we hypothesize that inhibition of JMJD3 may attenuate autoimmune disorders. We found that in vivo administration
Imane Chakroun et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 29(11), 4738-4755 (2015-08-01)
Adult skeletal muscles can regenerate after injury, due to the presence of satellite cells, a quiescent population of myogenic progenitor cells. Once activated, satellite cells repair the muscle damage by undergoing myogenic differentiation. The myogenic regulatory factors (MRFs) coordinate the
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Discover Bioactive Small Molecules for Gene Regulation

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.

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