324788
死亡相关蛋白激酶(DAPK)抑制剂
The DAPK Inhibitor, also referenced under CAS 315694-89-4, controls the biological activity of DAPK.
别名:
死亡相关蛋白激酶(DAPK)抑制剂, （4Z）-4-（3-吡啶基亚甲基）-2-苯乙烯基-恶唑-5-酮，死亡相关蛋白激酶抑制剂
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关于此项目
经验公式（希尔记法）:
C17H12N2O2
化学文摘社编号:
分子量:
276.29
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
死亡相关蛋白激酶(DAPK)抑制剂, The DAPK Inhibitor, also referenced under CAS 315694-89-4, controls the biological activity of DAPK.
SMILES string
N1=C(OC(=O)\C\1=C/c3cnccc3)\C=C\c2ccccc2
InChI
1S/C17H12N2O2/c20-17-15(11-14-7-4-10-18-12-14)19-16(21-17)9-8-13-5-2-1-3-6-13/h1-12H/b9-8+,15-11+
InChI key
GFGMISOSPOPSHN-QCTDOKRBSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 25 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
相关类别
Disclaimer
毒性：标准处理（A）
General description
一种恶唑酮化合物，可作为有效的、ATP竞争性和高度选择性的死亡相关蛋白激酶（DAPK）抑制剂（对于DAPK1和DAPK3，IC50分别为69和225 nM，具有10 µM ATP），同时表现出大大降低的活性或即使在高浓度为10 µM的情况下，对48种其他激酶也没有活性。
Other Notes
Okamoto, M., et al. 2009.J. Med. Chem.52, 7323.
Packaging
用惰性气体包装
Preparation Note
复溶后，等分并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存至多6个月。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
DAPK3 participates in the mRNA processing of immediate early genes in chronic lymphocytic leukaemia.
Fraser Thomas et al.
Molecular oncology, 14(6), 1268-1281 (2020-04-20)
Cross-linking of the B-cell receptor (BCR) induces transcriptional activation of immediate early genes (IEGs) including EGR1 and DUSP2 in chronic lymphocytic leukaemia (CLL). Here, we have shown that this transcriptional activation correlated with histone H3 threonine 6 and 11 phosphorylation.
Mariko Takahashi et al.
Nature immunology, 22(4), 485-496 (2021-03-27)
Evasion of host immunity is a hallmark of cancer; however, mechanisms linking oncogenic mutations and immune escape are incompletely understood. Through loss-of-function screening of 1,001 tumor suppressor genes, we identified death-associated protein kinase 3 (DAPK3) as a previously unrecognized driver
Katsuya Onishi et al.
FEBS letters, 597(5), 643-656 (2023-02-02)
Stiffness of the extracellular matrix regulates various biological responses, but the response mechanisms are poorly understood. Here, we found that the nuclear diphosphorylated myosin regulatory light chain (2P-MRLC) is a critical mechanomediator that suppresses apoptosis in response to substrate stiffness.
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