Description
GSK-J5 hydrochloride is a cell-permeable ester derivative of GSK J2 (HY-15648A), inactive. GSK-J5 hydrochloride is also an isomer of GSK-J4 (HY-15648B) and often used as a negative group.
Product information
CAS Number: 1797983-32-4
Molecular Weight: 453.96
Formula: C24H28ClN5O2
Chemical Name: ethyl 3-{[2-(pyridin-3-yl)-6-(2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl)pyrimidin-4-yl]amino}propanoate hydrochloride
Smiles: Cl.CCOC(=O)CCNC1=CC(=NC(=N1)C1=CN=CC=C1)N1CCC2=CC=CC=C2CC1
InChiKey: QQHQMHJAOKADED-UHFFFAOYSA-N
InChi: InChI=1S/C24H27N5O2.ClH/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);1H
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
How to use
In Vitro:
GSK-J5 (25 μM) has no effects at inhibiting the LPS-induced response of human primary macrophages derived from healthy volunteers. While GSK-J4 significantly reduced the expression of 16 of 34 LPS-driven cytokines as assessed by PCR array, such as TNF-α. GSK-J5 (30 μM; 6 hours) is the inactive isomer of GSK-J4, has no effect on TNF-α protein production. But neither GSK-J4 nor GSK-J5 directly affects the levels of LPS-induced JMJD3 or of LPS-independent UTX and EZH2. GSK-J5 (30 μM; 1 hour) can not prevent the LPS-induced loss of H3K27me3 associated with the TNFA TSS or block the recruitment of RNA polymerase II to this locus but GSK-J5 can. Finally, GSK-J4, but not GSK-J5, blocks the production of TNF-α by macrophages derived from patients with rheumatoid arthritis.
Products are for research use only. Not for human use.
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