324788
DAPK Inhibitor
The DAPK Inhibitor, also referenced under CAS 315694-89-4, controls the biological activity of DAPK.
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Synonym(s):
DAPK Inhibitor, (4 Z)-4-(3-Pyridylmethylene)-2-styryl-oxazol-5-one, Death-Associated Protein Kinase Inhibitor, (4Z)-4-(3-Pyridylmethylene)-2-styryl-oxazol-5-one, Death-Associated Protein Kinase Inhibitor
Empirical Formula (Hill Notation):
C17H12N2O2
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Quality Level
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
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
General description
An oxazalone compound that acts as a potent, ATP-competitive, and highly selective death-associated protein kinase (DAPK) inhibitor (IC50 = 69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 µM ATP), while exhibiting much reduced or no activity against a panel of 48 other kinases even at concentrations as high as 10 µM.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Okamoto, M., et al. 2009. J. Med. Chem.52, 7323.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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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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