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GSK-J4 (hydrochloride)

Item № 12073
CAS № 1797983-09-5
Purity ≥95%
product image
                (CAS 1797983-09-5)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $25.00 0.00
     5 mg $94.00 0.00
     10 mg $138.00 0.00
     50 mg $625.00 0.00

Pricing updated 2019-07-18. Prices are subject to change without notice.

Description

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.1,2 GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.3 Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).3

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Technical Information
Formal Name
N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine, ethyl ester, monohydrochloride
CAS Number
1797983-09-5
Molecular Formula
C24H27N5O2 • HCl
Formula Weight
454.0
Purity
≥95%
Formulation
A crystalline solid
λmax
260 nm
SMILES
O=C(OCC)CCNC1=CC(N2CCC(C=CC=C3)=C3CC2)=NC(C4=CC=CC=N4)=N1.Cl
InChI Code
InChI=1S/C24H27N5O2.ClH/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);1H
InChI Key
TYXWLTBYINKVNT-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

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References & Product Citations
Product Description References

1. Agger, K., Cloos, P.A.C., Christensen, J., et al. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development Nat.Lett. 449(7163), 731-734 (2011).

2. Hübner, M.R., and Spector, D.L. Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulation Cold Spring Harb.Symp.Quant.Biol. 75, 43-49 (2010).

3. Kruidenier, L., Chung, C.W., Cheng, Z., et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response Nature 488, 404-408 (2012).

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