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Product Information:

GSK699

GSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader . GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases .

Cat. No.: EX-A10642    Purity: >98%
Chemical
Chemical structure of GSK699


For research only, Do not use for Human!

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CAS No.2260944-68-9
Purity>98%
FormulaC45H51BrN8O7
Mol Weight895.84
ColorLight yellow to yellow
StateSolid
SolubilitySoluble in DMSO
Shelf Life>3 years if stored properly
StoragePowder -20℃ 3 years, 4℃ 2 years; In solvent -20℃ 1 month;
ShippingShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
 
 
Reference:  

[1]. Neef J, et al. Discovery and Optimization of Orally Bioavailable Heterobifunctional Degraders of KAT2A/B for the Treatment of Cancer. J Med Chem. 2026;69(4):4548-4566.

[2]. Haney MS, et al. In vivo CRISPR screening identifies SAGA complex members as key regulators of hematopoiesis. bioRxiv [Preprint]. 2025 May 19:2022.07.22.501030.

[3]. Bassi ZI, et al. Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach. ACS Chem Biol. 2018;13(10):2862-2867.

[4]. Luo H, et al. Advancing Design Strategy of PROTACs for Cancer Therapy. MedComm (2020). 2025;6(7):e70258. Published 2025 Jun 25.

CoACoA of GSK699
Smiles:O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCCCC4=CC=C(N(CCCN(C(=O)C5=CC=C(C=C5)[C@H]6C[C@@H](NC7=C(Br)C(=O)N(C)N=C7)CN(C)C6)C)C)C=C4

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