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首页-小分子抑制剂&激动剂-Epigenetics-Histone Acetyltransferase (HAT)-SGF29 inhibitor DC60
SGF29 inhibitor DC60

Chemical Structure : SGF29 inhibitor DC60

CAS No.: 6638-82-0

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SGF29 inhibitor DC60 (Cpd DC60)

货号: PC-21843Not For Human Use, Lab Use Only.

SGF29 inhibitor DC60 is a small molecule inhibitor of Spt-Ada-Gcn5 acetyltransferase (SAGA)-associated factor 29 (SGF29, CCDC101) with IC50 of 6.4 uM, binds to SGF29 second Tudor domain (SGF29 Tudor 2) and blocks SGF29 chromatin binding domain.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SGF29 inhibitor DC60 is a small molecule inhibitor of Spt-Ada-Gcn5 acetyltransferase (SAGA)-associated factor 29 (SGF29, CCDC101) with IC50 of 6.4 uM, binds to SGF29 second Tudor domain (SGF29 Tudor 2) and blocks SGF29 chromatin binding domain.
DC60 inhibits interaction of SGF29 Tudor 2 with its natural ligand H3K4me3 peptide with IC50 of 6.4 uM in AlphaScreen assays.
DC60 shows broad spectrum anticancer activity against of hematopoietic cancer cells (MLL-r leukemia cells, IC50=5.7-16.0 uM), solid tumor cells are substantially less sensitive.
DC60 also reduces the SGF29 protein level in leukemic cells, as well as the level of KAT2A and KAT2B protein.
DC60 suppresses leukemia progression in mice receiving MLL-AF9 leukemia.
DC60 also suppresses the expression of RPL8 and RPS2, resembling the impact caused by SGF29 depletion in leukemia.
SGF29 is a component of SAGA/ATAC acetyltransferase complexes, as a crucial factor for H3K9 acetylation, ribosomal gene expression, and leukemogenesis.

物理化学性质&存储条件

分子量 519.65
分子式 C33H33N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3,7,11-tribenzyl-3,4,7,8,11,12-hexahydro-2H,6H,10H-benzo[1,2-e:3,4-e':5,6-e'']tris([1,3]oxazine)

参考文献

1. Chan AKN, et al. Sci Adv. 2024 Feb 23;10(8):eadk3127.

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