WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406992
CAS#: 2079896-25-4
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.
Hodoodo Cat#: H406992
Name: GSK4027
CAS#: 2079896-25-4
Chemical Formula: C17H21BrN4O
Exact Mass: 376.09
Molecular Weight: 377.286
Elemental Analysis: C, 54.12; H, 5.61; Br, 21.18; N, 14.85; O, 4.24
Synonym: GSK4027; GSK-4027; GSK 4027.
IUPAC/Chemical Name: 4-bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one
InChi Key: VZAFGXCWAWRULT-UONOGXRCSA-N
InChi Code: InChI=1S/C17H21BrN4O/c1-21-10-13(12-6-4-3-5-7-12)8-14(11-21)20-15-9-19-22(2)17(23)16(15)18/h3-7,9,13-14,20H,8,10-11H2,1-2H3/t13-,14+/m0/s1
SMILES Code: CN1C[C@@H](C2=CC=CC=C2)C[C@@H](NC3=C(Br)C(N(C)N=C3)=O)C1
Appearance: Solid powder
Purity: >95% (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: >2 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:
| Biological target: | |
| In vitro activity: | |
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The following data is based on the product molecular weight 377.29 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Humphreys PG, Bamborough P, Chung CW, Craggs PD, Gordon LJ, Grandi P, Hayhow
TG, Hussain J, Jones KL, Lindon M, Michon AM, Renaux JF, Suckling CJ, Tough DF,
Prinjha RK. Discovery of a Potent, Cell Penetrant and Selective
p300/CBP-Associated Factor (PCAF)/General Control Non-Derepressible 5 (GCN5)
Bromodomain Chemical Probe. J Med Chem. 2016 Dec 21. doi:
10.1021/acs.jmedchem.6b01566. [Epub ahead of print] PubMed PMID: 28002667.
