TC-DAPK 6 is a novel, potent, ATP-competitive, and highly selective death-associated protein kinase (DAPK) inhibitor with IC₅₀ of 69 and 225 nM against DAPK1 and DAPK3, respectively, with 10 μM ATP.

Physicochemical Properties

Molecular Formula	C17H12N2O2
Molecular Weight	276.29
Exact Mass	276.089
Elemental Analysis	C, 73.90; H, 4.38; N, 10.14; O, 11.58
CAS #	315694-89-4
Related CAS #	315694-89-4
PubChem CID	5676111
Appearance	Light yellow to yellow solid powder
Density	1.2±0.1 g/cm3
Boiling Point	439.6±55.0 °C at 760 mmHg
Flash Point	219.7±31.5 °C
Vapour Pressure	0.0±1.1 mmHg at 25°C
Index of Refraction	1.615
LogP	3.62
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	21
Complexity	473
Defined Atom Stereocenter Count	0
SMILES	O=C(OC(/C=C/C1=CC=CC=C1)=N/2)C2=C/C3=CC=CN=C3
InChi Key	GFGMISOSPOPSHN-QCTDOKRBSA-N
InChi Code	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+
Chemical Name	(4E)-2-[(E)-2-phenylethenyl]-4-(pyridin-3-ylmethylidene)-1,3-oxazol-5-one
Synonyms	TC-DAPK 6; TCDAPK6; TC DAPK 6; DAPK Inhibitor; T6908224; T 6908224; -6908224
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	DAPK1 (IC50 = 69 nM); DAPK3 (IC50 = 225 nM)
ln Vitro	TC-DAPK 6 is found to be the most potent Death-associated protein kinase (DAPK) inhibitor with enzyme selectivity. The IC50 values for DAPK1 and DAPK3 when measured with 10 μM ATP are 69 and 225 nM, respectively. p70S6K is also inhibited by TC-DAPK 6 (1 μM < IC50< 10 μM)[1].
References	[1]. Identification of death-associated protein kinases inhibitors using structure-based virtual screening. J Med Chem. 2009 Nov 26;52(22):7323-7.

Solubility Data

Solubility (In Vitro)

DMSO: ~18.7 mg/mL (~67.6 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2 mg/mL (7.24 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.6194 mL	18.0969 mL	36.1939 mL
	5 mM	0.7239 mL	3.6194 mL	7.2388 mL
	10 mM	0.3619 mL	1.8097 mL	3.6194 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.