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GSK-J4 - ≥98%, high purity , CAS No.1373423-53-0, Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B

COA COA
In stock
Item Number
G276086
Grouped product items
SKU Size
Availability
 Price Qty
G276086-5mg
5mg
6
$93.90
G276086-10mg
10mg
6
$155.90
G276086-25mg
25mg
6
$351.90
G276086-50mg
50mg
5
$456.90
G276086-100mg
100mg
5
$692.90
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Cell permeable histone demethylase JMJD3/UTX inhibitor

View related series
Apoptosis (4276) Epigenetics (1496) Histone Demethylase (97) Histone Modification (1379) lysine demethylase 5B Inhibitor (5) lysine demethylase 5C Inhibitor (4) lysine demethylase 6A Inhibitor (3) lysine demethylase 6B Inhibitor (4)

Basic Description

Synonyms MFCD22683852 | Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate | Z1543021064 | AC-32705 | J-016640 | BRD-K98203492-001-01-1 | HB1407 | ETHYL 3-{[2-(PYRIDIN-2-YL)-6-(1,2,4,5-TETRAHYDRO-3-BENZAZEPIN-3-YL)
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms 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 o
Storage Temp Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of lysine demethylase 5B;Inhibitor of lysine demethylase 5C;Inhibitor of lysine demethylase 6A;Inhibitor of lysine demethylase 6B
Note Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Product 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.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Diazines
Subclass Pyrimidines and pyrimidine derivatives
Intermediate Tree Nodes Not available
Direct Parent Pyridinylpyrimidines
Alternative Parents Benzazepines  Beta amino acids and derivatives  Dialkylarylamines  Secondary alkylarylamines  Aminopyrimidines and derivatives  Azepines  Pyridines and derivatives  Benzenoids  Imidolactams  Heteroaromatic compounds  Carboxylic acid esters  Monocarboxylic acids and derivatives  Azacyclic compounds  Carbonyl compounds  Organic oxides  Organopnictogen compounds  Hydrocarbon derivatives  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Pyridinylpyrimidine - Benzazepine - Beta amino acid or derivatives - Dialkylarylamine - Aminopyrimidine - Secondary aliphatic/aromatic amine - Azepine - Imidolactam - Benzenoid - Pyridine - Heteroaromatic compound - Amino acid or derivatives - Carboxylic acid ester - Azacycle - Secondary amine - Carboxylic acid derivative - Monocarboxylic acid or derivatives - Organic oxide - Organonitrogen compound - Organooxygen compound - Carbonyl group - Organic oxygen compound - Organic nitrogen compound - Organopnictogen compound - Amine - Hydrocarbon derivative - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as pyridinylpyrimidines. These are compounds containing a pyridinylpyrimidine skeleton, which consists of a pyridine linked (not fused) to a pyrimidine by a bond.
External Descriptors Not available

Associated Targets(Human)

KDM5C Tchem Lysine-specific demethylase 5C (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDM6A Tchem Lysine-specific demethylase 6A (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDM6B Tchem Lysine-specific demethylase 6B (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDM5B Tchem Lysine-specific demethylase 5B (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KDM6A Tchem Lysine-specific demethylase 6A (39 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KDM5A Tchem Lysine-specific demethylase 5A (893 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KDM5B Tchem Lysine-specific demethylase 5B (814 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RAW264.7 (28094 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 488202292
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/488202292
IUPAC Name ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
INCHI 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)
InChIKey WBKCKEHGXNWYMO-UHFFFAOYSA-N
Smiles CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3
Isomeric SMILES CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3
Molecular Weight 417.51
Reaxy-Rn 22471772
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=22471772&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

10 results found

Lot Number Certificate Type Date Item
E2305290 Certificate of Analysis Feb 21, 2024 G276086
E2305251 Certificate of Analysis Feb 21, 2024 G276086
E2305224 Certificate of Analysis Feb 21, 2024 G276086
E2305267 Certificate of Analysis Feb 21, 2024 G276086
E2305487 Certificate of Analysis Feb 21, 2024 G276086
E2305240 Certificate of Analysis Jan 31, 2024 G276086
E2305254 Certificate of Analysis Jan 31, 2024 G276086
E2305269 Certificate of Analysis Jan 31, 2024 G276086
E2305284 Certificate of Analysis Jan 31, 2024 G276086
E2305489 Certificate of Analysis Jan 31, 2024 G276086

Chemical and Physical Properties

Solubility Soluble in DMSO to 100 mM and in ethanol to 100mM
Sensitivity Hygroscopic
Molecular Weight 417.500 g/mol
XLogP3 4.300
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 8
Exact Mass 417.216 Da
Monoisotopic Mass 417.216 Da
Topological Polar Surface Area 80.200 Ų
Heavy Atom Count 31
Formal Charge 0
Complexity 546.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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