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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-ABD957
ABD957

Chemical Structure : ABD957

CAS No.: 3007772-60-0

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ABD957 (ABD-957, ABD 957)

货号: PC-72214Not For Human Use, Lab Use Only.

ABD957 (ABD-957) is a potent, selective covalent inhibitor of the ABHD17 family of depalmitoylases, impairs N-Ras depalmitoylation in human AML cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ABD957 (ABD-957) is a potent, selective covalent inhibitor of the ABHD17 family of depalmitoylases, impairs N-Ras depalmitoylation in human AML cells.
ABD957 inhibits human ABHD17B (recombinantly expressed) with IC50 of 0.21 uM in lysates of HEK293T cells, does not inhibit LYPLA1, LYPLA2, or ABHD10.
ABD957 inhibits all three ABHD17s and partially impairs N-Ras depalmitoylation, ERK phosphorylation, and the growth of NRAS mutant cancer cells.
ABD957 stabilizes N-Ras palmitoylation less completely than Palm M, but is much more selective across the proteome.
ABD957 also impacted the subcellular distribution of N-Ras, leading to the accumulation of this protein at the plasma membrane.
ABD957 synergizes with MEK inhibition to block NRAS mutant cancer cell growth.

物理化学性质&存储条件

分子量 627.684
分子式 C27H36F3N7O5S
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

3,8-Diazabicyclo[3.2.1]octane-3-acetic acid, 8-[2-[[(3S)-4-[[3-[(dimethylamino)sulfonyl]-1H-pyrazol-1-yl]carbonyl]-3-methyl-1-piperazinyl]methyl]-5-(trifluoromethyl)phenyl]-

参考文献

1. Jarrett R Remsberg, et al. Nat Chem Biol. 2021 Aug;17(8):856-864.

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