| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
DAPK1 (IC50 = 69 nM); DAPK3 (IC50 = 225 nM)
TC-DAPK 6 targets death-associated protein kinase 1 (DAPK1), a serine/threonine kinase involved in regulating apoptosis, autophagy, and cellular stress responses. It also inhibits DAPK3 with an IC50 of 225 nM. TC-DAPK 6 acts as an ATP-competitive inhibitor, binding to the ATP-binding site of the kinase and preventing substrate phosphorylation. |
|---|---|
| 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].
In vitro, TC-DAPK 6 is a potent DAPK1 inhibitor with an IC50 of 69 nM and inhibits DAPK3 with an IC50 of 225 nM. It also inhibits p70S6K with IC50 values of 1 μM–10 μM. The compound is highly selective for DAPK over other kinases, making it a valuable tool for studying DAPK-mediated signaling pathways. |
| ln Vivo |
In vivo, TC-DAPK 6 is used as a research tool to study the role of DAPK in apoptosis, autophagy, and cellular stress responses. By inhibiting DAPK1, the compound modulates cell death pathways and stress responses. It has potential applications in cancer research and the study of neurodegenerative diseases where DAPK signaling is dysregulated.
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| Enzyme Assay |
In vitro enzyme assays for TC-DAPK 6 measure its inhibition of DAPK1 and DAPK3 activity. The kinase is incubated with its substrate and ATP in the presence of varying concentrations of the compound. Kinase activity is measured by quantifying substrate phosphorylation using radioactive or fluorescence-based methods. IC50 values of 69 nM for DAPK1 and 225 nM for DAPK3 are determined.
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| Cell Assay |
In vitro cell-based assays for TC-DAPK 6 assess its effects on DAPK-mediated cellular processes. Cells are treated with serial dilutions of the compound, and DAPK activity is measured by assessing the phosphorylation of DAPK substrates. Apoptosis, autophagy, and cellular stress responses are evaluated to determine the functional consequences of DAPK inhibition.
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| Animal Protocol |
In vivo animal models for TC-DAPK 6 include models of cancer and neurodegenerative diseases where DAPK plays a role. The compound is administered via various routes, and its effects on tumor growth, cell death, and disease progression are evaluated. Pharmacodynamic studies measure DAPK inhibition and downstream signaling in target tissues.
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| ADME/Pharmacokinetics |
TC-DAPK 6 has a molecular formula of C17H12N2O2 and a molecular weight of 276.29 g/mol. It is soluble in DMSO at 16.8 mg/mL (60.81 mM). The compound is stored as a powder at -20°C for up to 3 years. It has a purity of ≥98%. The compound is for research use only and is not approved for clinical use.
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| Toxicity/Toxicokinetics |
The toxicity profile of TC-DAPK 6 is characterized in preclinical safety studies. As a kinase inhibitor, the compound may have off-target effects at high concentrations. The compound is for research use only and is not approved for human use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
TC-DAPK 6 is a novel, potent, ATP-competitive, and highly selective DAPK inhibitor. It inhibits DAPK1 and DAPK3 with IC50 values of 69 nM and 225 nM, respectively. The compound is an oxazolone-based compound and is also known as a DAPK inhibitor. It is used primarily for research purposes in the study of apoptosis, autophagy, and cellular stress responses.
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| Molecular Formula |
C17H12N2O2
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|---|---|
| Molecular Weight |
276.29
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| Exact Mass |
276.089
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| Elemental Analysis |
C, 73.90; H, 4.38; N, 10.14; O, 11.58
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| CAS # |
315694-89-4
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| Related CAS # |
315694-89-4
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| PubChem CID |
5676111
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
439.6±55.0 °C at 760 mmHg
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| Flash Point |
219.7±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.615
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| LogP |
3.62
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
473
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(OC(/C=C/C1=CC=CC=C1)=N/2)C2=C/C3=CC=CN=C3
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| InChi Key |
GFGMISOSPOPSHN-QCTDOKRBSA-N
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| 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+
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| Chemical Name |
(4E)-2-[(E)-2-phenylethenyl]-4-(pyridin-3-ylmethylidene)-1,3-oxazol-5-one
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| Synonyms |
TC-DAPK 6; TCDAPK6; TC DAPK 6; DAPK Inhibitor; T6908224; T 6908224; -6908224
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~18.7 mg/mL (~67.6 mM)
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|---|---|
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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