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SML0709

GSK-J1

Name: GSK-J1
Brand: SIGMA

≥98% (HPLC)

Synonym(e):

3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid; N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-Alanine

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About This Item

Empirische Formel (Hill-System):

C₂₂H₂₃N₅O₂

CAS-Nummer:

1373422-53-7

Molekulargewicht:

389.45

MDL-Nummer:

MFCD22683851

UNSPSC-Code:

12352202

PubChem Substanz-ID:

329825587

NACRES:

NA.77

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Tranylcypromin, HCl, CAS-Nr. 1986-47-6, Calbiochem

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Histone Lysine Demethylase Inhibitor VII, GSK-J1

Sigma-Aldrich

385911

Hyaluronsäure-bindendes Protein, Rindernasenknorpel, biotinyliert

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 15 mg/mL, clear

Lagertemp.

2-8°C

SMILES String

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

InChI

1S/C22H23N5O2/c28-21(29)8-12-24-19-15-20(26-22(25-19)18-7-3-4-11-23-18)27-13-9-16-5-1-2-6-17(16)10-14-27/h1-7,11,15H,8-10,12-14H2,(H,28,29)(H,24,25,26)

InChIKey

AVZCPICCWKMZDT-UHFFFAOYSA-N

Anwendung

GSK-J1 has been used in formaldehyde dehydrogenase (FDH)-coupled demethylase assay.

Biochem./physiol. Wirkung

GSK-J1 is 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. For full characterization details, 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

GSK-J1 is also termed as 3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate. It may disturb the differentiation of specific neuronal subtypes in growing rat retina.

Leistungsmerkmale und Vorteile

GSK-J1 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.

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

Suchen Sie nach Analysenzertifikate (COA), indem Sie die Lot-/Chargennummer des Produkts eingeben. Lot- und Chargennummern sind auf dem Produktetikett hinter den Wörtern ‘Lot’ oder ‘Batch’ (Lot oder Charge) zu finden.

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Congenital Hyperinsulinism in Infants with Turner Syndrome: Possible Association with Monosomy X and KDM6A Haploinsufficiency.

Christopher E Gibson et al.

Hormone research in paediatrics, 89(6), 413-422 (2018-06-15)

Previous case reports have suggested a possible association of congenital hyperinsulinism with Turner syndrome. We examined the clinical and molecular features in girls with both congenital hyperinsulinism and Turner syndrome seen at The Children's Hospital of Philadelphia (CHOP) between 1974

The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads, 1362-1362 (2017)

Small Molecule GSK-J1 Affects Differentiation of Specific Neuronal Subtypes in Developing Rat Retina.

Raeisossadati R, et al.

Molecular Neurobiology, 1-12 (2018)

Characterization of a linked Jumonji domain of the KDM5/JARID1 family of histone H3 lysine 4 demethylases.

Horton JR, et al.

The Journal of Biological Chemistry, 291(6), 2631-2646 (2016)

Small Molecule GSK-J1 Affects Differentiation of Specific Neuronal Subtypes in Developing Rat Retina.

Reza Raeisossadati et al.

Molecular neurobiology, 56(3), 1972-1983 (2018-07-08)

Histone post-translational modification has been shown to play a pivotal role in regulating gene expression and fate determination during the development of the central nervous system. Application of pharmacological blockers that control histone methylation status has been considered a promising

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GSK-J1

≥98% (HPLC)

About This Item

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Lagertemp.

SMILES String

InChI

InChIKey

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Anwendung

Biochem./physiol. Wirkung

Leistungsmerkmale und Vorteile

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WGK

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Flammpunkt (°C)

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Analysenzertifikate (COA)

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