CAS NO: | 330461-64-8 |
生物活性 | AK-1 is a potent, specific and cell-permeableSIRT2inhibitor, with anIC50of 12.5 μM. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | AK-1 achieves significant neuroprotection in Huntington’s disease flies at 10 μM, improving the number of rhabdomeres from 5.2 to 5.6[1]. AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor, with an IC50of 12.5 μM[2]. AK-1 treatment induces proteasomal degradation of the Snail transcription factor through inactivation of the NF-κB/CSN2 pathway. Reduction in the level of Snail results in upregulation of p21, leading to G1 arrest, slow proliferation, and slow wound-healing activity. The regulation of Snail-p21 axis by AK-1 also occurs in HT-29 colon cancer cells[3]. Under hypoxic conditions, AK-1 increases the ubiquitination of HIF-1α in a VHL-dependent manner, leading to the degradation of HIF-1α via a proteasomal pathway. Downregulation of HIF-1α expression reduces its transcriptional activity and, eventually, reduces the expression of BNIP3, one of HIF-1 target genes, in AK-1-treated cells[4]. | ||||||||||||||||
分子量 | 403.45 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H21N3O5S | ||||||||||||||||
CAS 号 | 330461-64-8 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(123.93 mM) *"≥" means soluble, but saturation unknown. 配制储备液
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