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
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 25 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
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
相关类别
一般描述
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。
包装
用惰性气体包装
制备说明
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。
其他说明
Okamoto, M., et al. 2009.J. Med. Chem.52, 7323.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
毒性：标准处理（A）
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°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.
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.
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
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