GSK2801 | CAS#1619994-68-1 | BAZ2 inhibitor

MedKoo Cat#: 406639 | Name: GSK2801

Description:

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

GSK2801 is a A Selective Chemical Probe for BAZ2B/A bromodomains. BAZ2A/B belong to a family of ubiquitously expressed bromodomain containing proteins. Proteins of the BAZ family are characterized by a carboxy-terminal bromodomain adjacent to a PHD finger and a WACZ motif. In addition four other conserved motifs are typically found in the N-terminus of BAZ family members, namely the LH motif (a leucine-rich helical domain), the ZB2 motif and the BAZ 1 and BAZ 2 motifs. Little is known about the biological function of BAZ2B but it has been suggested to regulate nucleosome mobilization by the ATP-dependent chromatin remodeling factor ISWI.

Chemical Structure

GSK2801

CAS#1619994-68-1

Theoretical Analysis

MedKoo Cat#: 406639

Name: GSK2801

CAS#: 1619994-68-1

Chemical Formula: C20H21NO4S

Exact Mass: 371.1191

Molecular Weight: 371.45

Elemental Analysis: C, 64.67; H, 5.70; N, 3.77; O, 17.23; S, 8.63

Price and Availability

Size	Price	Availability
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,250.00	Ready to ship
500mg	USD 2,650.00	Ready to ship
1g	USD 3,950.00	Ready to ship

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Related CAS #

No Data

Synonym

GSK2801; GSK-2801; GSK 2801.

IUPAC/Chemical Name

1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone

InChi Key

KHWCPNJRJCNVRI-UHFFFAOYSA-N

InChi Code

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

SMILES Code

CC(C1=CC(C2=CC=CC=C2S(=O)(C)=O)=C3C=C(OCCC)C=CN13)=O

Appearance

Pale yellow 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 C for short term (days to weeks) or -20 C 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 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Certificate of Analysis

View CoA: current batch, Lot#BBC60318

QC Data

View QC data: current batch, Lot#BBC60318

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 371.45 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

1: Yellapu NK, Pei D, Nissen E, Thompson JA, Koestler DC. Comprehensive exploration of JQ1 and GSK2801 targets in breast cancer using network pharmacology and molecular modeling approaches. Comput Struct Biotechnol J. 2023 Jun 3;21:3224-3233. doi: 10.1016/j.csbj.2023.06.003. PMID: 38213901; PMCID: PMC10781883. 2: Cazzanelli G, Vedove AD, Parolin E, D'Agostino VG, Unzue A, Nevado C, Caflisch A, Lolli G. Reevaluation of bromodomain ligands targeting BAZ2A. Protein Sci. 2023 Sep;32(9):e4752. doi: 10.1002/pro.4752. PMID: 37574751; PMCID: PMC10464297. 3: Molteni E, Baldan F, Damante G, Allegri L. GSK2801 Reverses Paclitaxel Resistance in Anaplastic Thyroid Cancer Cell Lines through MYCN Downregulation. Int J Mol Sci. 2023 Mar 22;24(6):5993. doi: 10.3390/ijms24065993. PMID: 36983070; PMCID: PMC10054879. 4: Yellapu NK, Ly T, Sardiu ME, Pei D, Welch DR, Thompson JA, Koestler DC. Synergistic anti-proliferative activity of JQ1 and GSK2801 in triple-negative breast cancer. BMC Cancer. 2022 Jun 8;22(1):627. doi: 10.1186/s12885-022-09690-2. PMID: 35672711; PMCID: PMC9173973. 5: Jia Y, Li L, Lin YH, Gopal P, Shen S, Zhou K, Yu X, Sharma T, Zhang Y, Siegwart DJ, Ready JM, Zhu H. In vivo CRISPR screening identifies BAZ2 chromatin remodelers as druggable regulators of mammalian liver regeneration. Cell Stem Cell. 2022 Mar 3;29(3):372-385.e8. doi: 10.1016/j.stem.2022.01.001. Epub 2022 Jan 31. PMID: 35090595; PMCID: PMC8897233. 6: Abeywickrama-Samarakoon N, Cortay JC, Sureau C, Müller S, Alfaiate D, Guerrieri F, Chaikuad A, Schröder M, Merle P, Levrero M, Dény P. Hepatitis Delta Virus histone mimicry drives the recruitment of chromatin remodelers for viral RNA replication. Nat Commun. 2020 Jan 21;11(1):419. doi: 10.1038/s41467-020-14299-9. PMID: 31964889; PMCID: PMC6972770. 7: Chee J, Wilson C, Buzzai A, Wylie B, Forbes CA, Booth M, Principe N, Foley B, Cruickshank MN, Waithman J. Impaired T cell proliferation by ex vivo BET- inhibition impedes adoptive immunotherapy in a murine melanoma model. Epigenetics. 2020 Jan-Feb;15(1-2):134-144. doi: 10.1080/15592294.2019.1656156. Epub 2019 Aug 26. PMID: 31423932; PMCID: PMC6961692. 8: Bevill SM, Olivares-Quintero JF, Sciaky N, Golitz BT, Singh D, Beltran AS, Rashid NU, Stuhlmiller TJ, Hale A, Moorman NJ, Santos CM, Angus SP, Zawistowski JS, Johnson GL. GSK2801, a BAZ2/BRD9 Bromodomain Inhibitor, Synergizes with BET Inhibitors to Induce Apoptosis in Triple-Negative Breast Cancer. Mol Cancer Res. 2019 Jul;17(7):1503-1518. doi: 10.1158/1541-7786.MCR-18-1121. Epub 2019 Apr 18. PMID: 31000582; PMCID: PMC6610760. 9: Yang X, Wu X, Zhang J, Zhang X, Xu C, Liao S, Tu X. Recognition of hyperacetylated N-terminus of H2AZ by TbBDF2 from Trypanosoma brucei. Biochem J. 2017 Nov 9;474(22):3817-3830. doi: 10.1042/BCJ20170619. PMID: 29025975. 10: Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6. PMID: 25799074; PMCID: PMC4770311.