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324788

Sigma-Aldrich

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
CAS Number:
Molecular Weight:
276.29

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

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DAPK Inhibitor The DAPK Inhibitor, also referenced under CAS 315694-89-4, controls the biological activity of DAPK.

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GSK-3β Inhibitor VII The GSK-3β Inhibitor VII, also referenced under CAS 99-73-0, controls the biological activity of GSK-3β. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

361548

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form

solid

form

solid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, desiccated, protect from light

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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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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