The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.,. GSK-J4 is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1, an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.3 However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition. Reference: . 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). . 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). . 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).

Product information

CAS Number: 1394854-51-3

Molecular Weight: 417.50

Formula: C24H27N5O2

Chemical Name: ethyl 3-{[2-(pyridin-3-yl)-6-(2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl)pyrimidin-4-yl]amino}propanoate

Smiles: CCOC(=O)CCNC1=CC(=NC(=N1)C1=CN=CC=C1)N1CCC2=CC=CC=C2CC1

InChiKey: LQPGVGSKBNXQDU-UHFFFAOYSA-N

InChi: InChI=1S/C24H27N5O2/c1-2-31-23(30)9-13-26-21-16-22(28-24(27-21)20-8-5-12-25-17-20)29-14-10-18-6-3-4-7-19(18)11-15-29/h3-8,12,16-17H,2,9-11,13-15H2,1H3,(H,26,27,28)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.