GSK4027|2079896-25-4--Shanghai xingMo Biotechnology

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Description

GSK4027 is a potent and selective chemical probe for the PCAF/GCN5 bromodomain. GSK4027 has PCAF TR-FRET pIC50 = 7.4 ; PCAF BROMOscan pKi = 8.9; GCN5 BROMOscan pKi = 8.9; PCAF NanoBRET pIC50 =7.2; BRD4 BD1 TR-FRET pIC50 < 4.3. GSK4027 shows high potency for the PCAF/GCN5 bromodomain, high solubility, cellular target engagement, and ≥18000-fold selectivity over the BET family, together with ≥70-fold selectivity over the wider bromodomain families. p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development.

Chemical Structure

Chemical Name

4-bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one

SMILES Code

CN1C[C@@H](C2=CC=CC=C2)C[C@@H](NC3=C(Br)C(N(C)N=C3)=O)C1

Theoretical Analysis

XingMo Cat#:XM341
Product Name:GSK4027
Synonyms:GSK4027; GSK-4027; GSK 4027.
CAS#:2079896-25-4
Chemical Formula:C₁₇H₂₁BrN₄O
Exact Mass:376.0899
Molecular Weight:377.286
Purity:>98%

Technical Data

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 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years)

Solubility: Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly.

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

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

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

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