PROTAC DAPK1 Degrader-1
Based on 1 Customer Validation
PROTAC DAPK1 Degrader-1 is a death-associated protein kinase 1 (DAPK1) degrader with a DC50 of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increases MDM2 protein levels and inhibits neuronal apoptosis in ceramide-induced cells. PROTAC DAPK1 Degrader-1 can be used to study neurological disorders such as cerebral ischemia and traumatic brain injury.
(Pink: DAPK ligand (HY-179071); Blue: Cereblon ligand (HY-10984); Black: linker (HY-40171)).
For research use only. We do not sell to patients.
- Purity : 96.70%
- CAS No.: 3063030-38-3
- Formula: C30H27N9O7S
- Molecular Weight:657.66
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
DAPK1 119.6 nM (DC50) |
MDM2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | DC50 |
0.1196 μM
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DAPK1 protein degradation in human SH-SY5Y neuroblastoma cells assessed via Western blot assay.
DAPK1 protein degradation in human SH-SY5Y neuroblastoma cells assessed via Western blot assay.
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41032954 |
In Vitro
PROTAC DAPK1 Degrader-1 (CP1) (0.1-10 μM; 2-24 h) induces time- and dose-dependent degradation of DAPK1 in SH-SY5Y cells, with a DC50 of 119.6 nM[1].
PROTAC DAPK1 Degrader-1 mediates the degradation of DAPK1 in SH-SY5Y cells via the proteasomal pathway without altering the expression of DAPK1 mRNA; it exhibits no cytotoxicity against SH-SY5Y cells[1].
PROTAC DAPK1 Degrader-1 (3-10 μM) upregulates the MDM2 protein level in SH-SY5Y cells, with a significant upregulation at the concentration of 10 μM, which results from the abrogation of the inhibitory effect of DAPK1 on MDM2 stability[1].
PROTAC DAPK1 Degrader-1 inhibits ceramide-induced apoptosis in SH-SY5Y cells and exhibits neuroprotective effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y neuroblastoma cells
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Concentration:0, 0.1, 0.3, 1, 3, 10 μM
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Incubation Time:24 h
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Result:Induced DAPK1 degradation with a DC50 of 0.1196 μM.
Confirmed significant reductions in DAPK1 levels at both 3 μM and 10 μM.
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Cell Line:SH-SY5Y neuroblastoma cells
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Concentration:3 μM
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Incubation Time:0, 2, 4, 8, 16, 24 h
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Result:Induced observable DAPK1 degradation at 3 μM for 2 h.
Degraded over 50% of DAPK1 protein at 3 μM for 4 h.
Exceeded 80% DAPK1 degradation rate at 3 μM or 10 μM for 24 h.
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Cell Line:SH-SY5Y neuroblastoma cells
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Concentration:0, 0.1, 0.3, 1, 3, 10, 20 μM
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Incubation Time:12 h
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Result:Exhibited no cytotoxicity against SH-SY5Y cells.
Chemical Information
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CAS No. 3063030-38-3
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Appearance Solid
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Molecular Weight 657.66
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Formula C30H27N9O7S
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Color Light yellow to green yellow
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SMILES
O=C(C1=CC=CC(N2N=CC3=C2N=C(NC3=O)SC(C(N)=O)C)=C1)NCCNC4=CC=CC(C(N5C(C(N6)=O)CCC6=O)=O)=C4C5=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 4.17 mg/mL (6.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5205 mL | 7.6027 mL | 15.2054 mL | 38.0136 mL |
| 5 mM | 0.3041 mL | 1.5205 mL | 3.0411 mL | 7.6027 mL |
PROTAC DAPK1 Degrader-1 Related Classifications
HY-179055 Related Classifications
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