GSK-J2 | CAS#1394854-52-4 | Inactive isomer of GSK J1

MedKoo Cat#: 462467 | Name: GSK-J2

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.

Chemical Structure

GSK-J2

CAS#1394854-52-4

Theoretical Analysis

MedKoo Cat#: 462467

Name: GSK-J2

CAS#: 1394854-52-4

Chemical Formula: C22H23N5O2

Exact Mass: 389.1852

Molecular Weight: 389.46

Elemental Analysis: C, 67.85; H, 5.95; N, 17.98; O, 8.22

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 Weeks
50mg	USD 950.00	2 Weeks

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Synonym

GSK-J2; GSK J2; GSKJ2; Inactive isomer of GSK J1

IUPAC/Chemical Name

3-((2-(pyridin-3-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoic acid

InChi Key

LJIFOCRGDDQFJF-UHFFFAOYSA-N

InChi Code

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

SMILES Code

O=C(O)CCNC1=NC(C2=CC=CN=C2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GSK-J2 is an isomer of GSK-J1 that does not have any specific activity.

In vitro activity:

The results showed that the RNA levels of the pluripotent marker OCT4 were not dramatically downregulated in the GSKJ1 group, but the RNA levels of the neural markers SOX1 and PAX6 were significantly increased (Figure 7A), whereas no beneficial effect was observed in the GSK126 group. Taken together, the KDM6 inhibitor GSK-J1 could significantly improve the neuroectoderm differentiation from human pluripotent stem cells. Reference: Front Cell Dev Biol. 2021 Sep 8;9:702462. https://pubmed.ncbi.nlm.nih.gov/34568320/

In vivo activity:

To further clarify the effect of JMJD3 on regulating inflammatory response, JMJD3 is downregulated specifically in mammary mouse glands via the administration of a selective histone demethylase JMJD3 inhibitor, GSK-J1. The results show that GSK-J1 significantly inhibits the level of JMJD3 expression after LPS exposure (Fig. 1, D and E). Reference: J Biol Chem. 2022 Jun;298(6):102017. https://pubmed.ncbi.nlm.nih.gov/35526564/

	Solvent	mg/mL	mM
Solubility
	DMSO	40.5	103.91

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 389.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Meng Y, Zhang T, Zheng R, Ding S, Yang J, Liu R, Jiang Y, Jiang W. Depletion of Demethylase KDM6 Enhances Early Neuroectoderm Commitment of Human PSCs. Front Cell Dev Biol. 2021 Sep 8;9:702462. doi: 10.3389/fcell.2021.702462. PMID: 34568320; PMCID: PMC8455897. 2. Wang JJ, Wang X, Xian YE, Chen ZQ, Sun YP, Fu YW, Wu ZK, Li PX, Zhou ES, Yang ZT. The JMJD3 histone demethylase inhibitor GSK-J1 ameliorates lipopolysaccharide-induced inflammation in a mastitis model. J Biol Chem. 2022 Jun;298(6):102017. doi: 10.1016/j.jbc.2022.102017. Epub 2022 May 6. PMID: 35526564; PMCID: PMC9168612.

In vitro protocol:

In vivo protocol:

1. Wang JJ, Wang X, Xian YE, Chen ZQ, Sun YP, Fu YW, Wu ZK, Li PX, Zhou ES, Yang ZT. The JMJD3 histone demethylase inhibitor GSK-J1 ameliorates lipopolysaccharide-induced inflammation in a mastitis model. J Biol Chem. 2022 Jun;298(6):102017. doi: 10.1016/j.jbc.2022.102017. Epub 2022 May 6. PMID: 35526564; PMCID: PMC9168612.

1: Heinemann B, Nielsen JM, Hudlebusch HR, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014;514(7520):E1-E2. doi:10.1038/nature13688