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GSK-J1 - ≥99%, high purity , CAS No.1373422-53-7, Inhibitor of lysine demethylase 5A;Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B

Moligand™
≥99%

CAS#: 1373422-53-7
Formula: C₂₂H₂₃N₅O₂
Molecular Weight: 389.46
PubChem CID: 56963315

Item Number

G275049

Grouped product items
SKU	Size	Availability	Price
G275049-10mg	10mg	In stock	$75.90
G275049-25mg	25mg	In stock	$124.90
G275049-50mg	50mg	In stock	$222.90
G275049-100mg	100mg	In stock	$369.90

Potent and selective H3K27 histone demethylase inhibitor

View related series

lysine demethylase 5A Inhibitor lysine demethylase 5B Inhibitor lysine demethylase 5C Inhibitor lysine demethylase 6A Inhibitor lysine demethylase 6B Inhibitor

Basic Description

Synonyms	GSK-J1\|1373422-53-7\|GSK J1\|GSKJ1\|3-[[2-Pyridin-2-Yl-6-(1,2,4,5-Tetrahydro-3-Benzazepin-3-Yl)pyrimidin-4-Yl]amino]propanoic Acid\|3-((2-(Pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoic acid\|3-{[2-(pyridin-2-yl)-6-(2
Specifications & Purity	≥99%
Storage Temp	Store at -20°C,Desiccated
Shipped In	Dry ice
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of lysine demethylase 5A;Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B
Product Description	Product introduction GSK J1 is a potent and selective inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3, a Fe2+- and α-ketoglutarate-dependent oxygenase involved in a variety of physiological functions including the inflammatory response, with the half maximal inhibition concentration IC50 value of 60 nM . Application GSK-J1 has been used in formaldehyde dehydrogenase (FDH)-coupled demethylase assay.

Associated Targets

KDM5A Tchem Lysine-specific demethylase 5A 1 Activities

Discover Target: KDM5A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDM5C Tchem Lysine-specific demethylase 5C 1 Activities

Discover Target: KDM5C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDM6A Tchem Lysine-specific demethylase 6A 1 Activities

Discover Target: KDM6A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDM6B Tchem Lysine-specific demethylase 6B 0 Activities

Discover Target: KDM6B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDM5B Tchem Lysine-specific demethylase 5B 1 Activities

Discover Target: KDM5B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoic acid
INCHI	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)
InChi Key	AVZCPICCWKMZDT-UHFFFAOYSA-N
Canonical SMILES	C1CN(CCC2=CC=CC=C21)C3=NC(=NC(=C3)NCCC(=O)O)C4=CC=CC=N4
Isomeric SMILES	C1CN(CCC2=CC=CC=C21)C3=NC(=NC(=C3)NCCC(=O)O)C4=CC=CC=N4
PubChem CID	56963315
Molecular Weight	389.46

PubChem CID

56963315

CAS Registry No.

1373422-53-7

ChEMBL Ligand

CHEMBL3188597

RCSB PDB Ligand

K0I, URY

Certificates

Certificate of Analysis(COA)

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4 results found

Lot Number	Certificate Type	Date	Item
H2206417	Certificate of Analysis	May 12, 2023	G275049
H2206442	Certificate of Analysis	May 12, 2023	G275049
H2206467	Certificate of Analysis	May 12, 2023	G275049
H2206474	Certificate of Analysis	May 12, 2023	G275049

Safety and Hazards(GHS)

Pictogram(s)	GHS07
Signal	Warning
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P271:Use only outdoors or in a well-ventilated area. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell.

References

1. Sakurai M, Rose NR, Schultz L, Quinn AM, Jadhav A, Ng SS, Oppermann U, Schofield CJ, Simeonov A. (2010) A miniaturized screen for inhibitors of Jumonji histone demethylases.. Mol Biosyst, 6 (2): (357-64). [PMID:20094655]
2. Mackeen MM, Kramer HB, Chang KH, Coleman ML, Hopkinson RJ, Schofield CJ, Kessler BM. (2010) Small-molecule-based inhibition of histone demethylation in cells assessed by quantitative mass spectrometry.. J Proteome Res, 9 (8): (4082-92). [PMID:20583823]
3. Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H et al.. (2012) A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.. Nature, 488 (7411): (404-8). [PMID:22842901]
4. Heinemann B, Nielsen JM, Hudlebusch HR, Lees MJ, Larsen DV, Boesen T, Labelle M, Gerlach LO, Birk P, Helin K. (2014) Inhibition of demethylases by GSK-J1/J4.. Nature, 514 (7520): (E1-2). [PMID:25279926]

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