| Identification | Back Directory | [Name]
GSK 2801 | [CAS]
1619994-68-1 | [Synonyms]
GSK2801
CS-1607
GSK 280
GSK-2801
GSK 2801
GSK2801, >98%
GSK-2801; GSK 280
GSK2801 GSK-2801
GSK2801;GSK-2801;GSK 2801
1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone
1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone
1-[1-(2-Methanesulfonyl-phenyl)-7-propoxy-indolizin-3-yl]-ethanone
Ethanone, 1-[1-[2-(methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]-
1-(7-(2-Methylsulfonyl-phenyl)-4-propoxy-1-aza-bicyclo[4.3.0]nona-2,4,6,8-tetraen-9-yl)-ethanone | [Molecular Formula]
C20 H21 N O4 S | [MDL Number]
MFCD26142953 | [MOL File]
1619994-68-1.mol | [Molecular Weight]
371.45 |
| Chemical Properties | Back Directory | [density ]
1.23±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
insoluble in H2O; ≥18.55 mg/mL in DMSO; ≥2.82 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [color ]
Light yellow to khaki | [InChI]
1S/C20H21NO4S/c1-4-11-25-15-9-10-21-18(14(2)22)13-17(19(21)12-15)16-7-5-6-8-20(16)26(3,23)24/h5-10,12-13H,4,11H2,1-3H3 | [InChIKey]
KHWCPNJRJCNVRI-UHFFFAOYSA-N | [SMILES]
CCCOC1=CC2=C(C3=CC=CC=C3S(=O)(C)=O)C=C(C(C)=O)N2C=C1 |
| Hazard Information | Back Directory | [Description]
BAZ2A/B are bromodomain-containing proteins whose biological function is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci. BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. GSK2801 is a selective, cell-permeable inhibitor of the BAZ2 family of bromodomain-containing proteins (IC50s = 9-350 nM in a BAZ2B AlphaScreen). It binds to BAZ2A and BAZ2B with Kd values of 0.26 and 0.14 μM, respectively, and does not interact with the bromodomains of BRD4(BD1), CREBBP, TRIM24/TIF1α, PB1(BD5), PCAF, or ATAD2. See the Structural Genomics Consortium (SGC) website for more information. | [Uses]
GSK2801 is a selective cell-permeable inhibitor of the BAZ2 (bromodomain-containing protein) interfering with nucleosome spacing during chromatin assembly. | [in vivo]
In order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability[1]. | [References]
[1]. chen p, chaikuad a, bamborough p, et al. discovery and characterization of gsk2801, a selective chemical probe for the bromodomains baz2a and baz2b. journal of medicinal chemistry, 2015. |
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| Company Name: |
Spectrum Chemical Manufacturing Corp.
|
| Telephone: |
021-021-021-67601398-809-809-809 15221380277 |
| Website: |
www.spectrumchemical.com/oa_html/index.jsp?minisite=10020&respid=22372&language=us |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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