GSK 2801 - ≥98%(HPLC), high purity , CAS No.1619994-68-1, Inhibitor of bromodomain adjacent to zinc finger domain 2A;Inhibitor of bromodomain adjacent to zinc finger domain 2B

Item Number
G288683
Grouped product items
SKUSizeAvailabilityPrice Qty
G288683-5mg
5mg
In stock
$86.90
G288683-10mg
10mg
In stock
$118.90
G288683-25mg
25mg
In stock
$267.90
G288683-50mg
50mg
In stock
$434.90
G288683-100mg
100mg
In stock
$783.90

Selective BAZ2A and BAZ2B inhibitor

Basic Description

Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsSelective BAZ2A and BAZ2B inhibitor (IC50values are 0.40 and 0.43μM, respectively). Selective for BAZ2A/B over TAF1L and BRD9. Cell permeable and orally available.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of bromodomain adjacent to zinc finger domain 2A;Inhibitor of bromodomain adjacent to zinc finger domain 2B

Associated Targets(Human)

BAZ2A Tchem Bromodomain adjacent to zinc finger domain protein 2A (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BAZ2B Tchem Bromodomain adjacent to zinc finger domain protein 2B (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MTNR1A Tclin Melatonin receptor 1A (2519 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EP300 Tchem Histone acetyltransferase p300 (1259 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KAT2B Tchem Histone acetyltransferase PCAF (884 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CREBBP Tchem CREB-binding protein (1602 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD2 Tchem Bromodomain-containing protein 2 (1296 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BAZ2B Tchem Bromodomain adjacent to zinc finger domain protein 2B (56204 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PBRM1 Tchem Protein polybromo-1 (712 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRDT Tchem Bromodomain testis-specific protein (576 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD3 Tchem Bromodomain-containing protein 3 (1086 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ATAD2 Tchem ATPase family AAA domain-containing protein 2 (598 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM33 Tchem E3 ubiquitin-protein ligase TRIM33 (162 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PHIP Tbio PH-interacting protein (91 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD1 Tchem Bromodomain-containing protein 1 (256 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ATAD2B Tchem ATPase family AAA domain-containing protein 2B (90 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SMARCA2 Tchem Probable global transcription activator SNF2L2 (466 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SMARCA4 Tchem Transcription activator BRG1 (263 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BPTF Tchem Nucleosome-remodeling factor subunit BPTF (194 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD7 Tchem Bromodomain-containing protein 7 (146 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CECR2 Tchem Cat eye syndrome critical region protein 2 (340 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD9 Tchem Bromodomain-containing protein 9 (684 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TAF1L Tchem Transcription initiation factor TFIID subunit 1-like (141 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BAZ2A Tchem Bromodomain adjacent to zinc finger domain protein 2A (266 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SP140 Tbio Nuclear body protein SP140 (54 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TAF1 Tchem Transcription initiation factor TFIID subunit 1 (441 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRWD1 Tbio Bromodomain and WD repeat-containing protein 1 (55 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BAZ1B Tbio Tyrosine-protein kinase BAZ1B (16 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ASH1L Tbio Histone-lysine N-methyltransferase ASH1L (468 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRWD3 Tbio Bromodomain and WD repeat-containing protein 3 (17 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM28 Tbio Transcription intermediary factor 1-beta (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GCN5 Histone acetyltransferase GCN5 (89 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 1-[1-(2-methylsulfonylphenyl)-7-propoxyindolizin-3-yl]ethanone
INCHI 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
InChi Key KHWCPNJRJCNVRI-UHFFFAOYSA-N
Canonical SMILES CCCOC1=CC2=C(C=C(N2C=C1)C(=O)C)C3=CC=CC=C3S(=O)(=O)C
Isomeric SMILES CCCOC1=CC2=C(C=C(N2C=C1)C(=O)C)C3=CC=CC=C3S(=O)(=O)C
PubChem CID 73010930
MeSH Entry Terms 1-(1-(3-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone;GSK2801
Molecular Weight 371.45

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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5 results found

Lot NumberCertificate TypeDateItem
I2201471Certificate of AnalysisJun 28, 2022 G288683
I2201480Certificate of AnalysisJun 28, 2022 G288683
I2201481Certificate of AnalysisJun 28, 2022 G288683
I2201507Certificate of AnalysisJun 28, 2022 G288683
I2201509Certificate of AnalysisJun 28, 2022 G288683

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 18.57, Max Conc. mM: 50

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H302:Harmful if swallowed

Precautionary Statements

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

Related Documents

References

1. Jones MH, Hamana N, Nezu Ji, Shimane M.  (2000)  A novel family of bromodomain genes..  Genomics,  63  (1): (40-5).  [PMID:10662543] [10.1021/op500134e]
2. Guetg C, Lienemann P, Sirri V, Grummt I, Hernandez-Verdun D, Hottiger MO, Fussenegger M, Santoro R.  (2010)  The NoRC complex mediates the heterochromatin formation and stability of silent rRNA genes and centromeric repeats..  EMBO J,  29  (13): (2135-46).  [PMID:20168299] [10.1021/op500134e]

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