TC-DAPK 6

• CAT Number: I003122
• CAS Number: 315694-89-4
• Molecular Formula: C17H12N2O2
• Molecular Weight: 276.29
• Purity: ≥95%
• Synonyms: (4E)-2-[(E)-2-phenylethenyl]-4-(pyridin-3-ylmethylidene)-1,3-oxazol-5-one
• Target: DAPK
• Solubility: Soluble to 50 mM in DMSO
• Storage: Store at -20°C
• IC50: 69 nM (DAPK1); 225 nM (DAPK3)

TC-DAPK 6 is 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 uM ATP).IC50 value: 69 nM (DAPK1); 225 nM (DAPK3)Target: DAPK1; DAPK3Death-associated protein kinase (DAPK) is a serine/threonine protein kinase implicated in diverse programmed cell death pathways. DAPK is a promising target protein for the treatment of ischemic diseases. TC-DAPK 6 is 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 uM ATP); while exhibiting much reduced or no activity against a panel of 48 other kinases even at concentrations as high as 10 uM.

Reference

[1]. Gandesiri M, Chakilam S, Ivanovska J, et al. DAPK plays an important role in panobinostat-induced autophagy and commits cells to apoptosis under autophagy deficient conditions. Apoptosis. 2012 Dec;17(12):1300-15.
[2]. Arif A, Chatterjee P, Moodt RA, Fox PL. Heterotrimeric GAIT complex drives transcript-selective translation inhibition in murine macrophages. Mol Cell Biol. 2012 Dec;32(24):5046-55.
[3]. Zhang H, Chen GG, Zhang Z, et al. Induction of autophagy in hepatocellular carcinoma cells by SB203580 requires activation of AMPK and DAPK but not p38 MAPK. Apoptosis. 2012 Apr;17(4):325-34.
[4]. Okamoto M, Takayama K, Shimizu T et al. Structure-activity relationship of novel DAPK inhibitors identified by structure-based virtual screening. Bioorg Med Chem. 2010 Apr 1;18(7):2728-34. doi: 10.1016/j.bmc.2010.02.018.
[5]. Okamoto M, Takayama K, Shimizu T et al. Identification of death-associated protein kinases inhibitors using structure-based virtual screening. J Med Chem. 2009 Nov 26;52(22):7323-7. doi: 10.1021/jm901191q.