PROTAC HPK1 Degrader-1
Based on 1 Customer Validation
PROTAC HPK1 Degrader-1 (compound B1) is a PROTAC degrader that recruits cereblon to induce HPK1 degradation, with a DC50 of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits HPK1 kinase activity, with an IC50 of 140.5 nM. PROTAC HPK1 Degrader-1 suppresses the phosphorylation of SLP76 protein, with an IC50 of 496.1 nM. PROTAC HPK1 Degrader-1 can be used to investigate non-kinase-dependent signaling of HPK1 in the TCR pathway and cancer-related research.
(Pink: MAP4K Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker (HY-W067489)).
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 3034182-97-0
- Formula: C43H43N7O8
- Molecular Weight:785.84
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Immunology/Inflammation Compound Library
HY-L007
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MAPK Compound Library
HY-L010
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Anti-Cancer Compound Library
HY-L025
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Oxygen Sensing Compound Library
HY-L045
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PROTAC Library
HY-L151
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Extracellular Vesicles (EVs) Compound Library
HY-L168
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Multi-Target Compound Library
HY-L176
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MCE Bioactive Compound Library
HY-L001V
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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HPK1 1.8 nM (DC50) |
HPK1 140.5 nM (IC50) |
SLP-76 496.1 nM (IC50) |
PROTAC HPK1 Degrader-1 (compound B1) inhibits purified HPK1 kinase activity with an IC50 of 140.5 nM[1].
PROTAC HPK1 Degrader-1 (compound B1) (0.68-500 nM; 24 h) induces dose-dependent HPK1 degradation in Jurkat cells with a DC50 of 1.8 nM, time-dependent degradation with maximum effect at 24 h, and acts via a ubiquitin-proteasome system-dependent mechanism requiring CRBN and HPK1 binding[1].
PROTAC HPK1 Degrader-1 (compound B1) (0.5-2 μM; 24 h) inhibits SLP76 phosphorylation in Jurkat cells with an IC50 of 496.1 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat cells
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Concentration:0.68, 2.07, 6.17, 18.5, 55, 166, 500 nM
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Incubation Time:24 h
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Result:Dose-dependently degraded HPK1 with a DC50 of 1.8 nM.
Complete degradation was observed at 100 nM.
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Cell Line:Jurkat cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Inhibited SLP76 phosphorylation in a dose-dependent manner, with an IC50 value of 496.1 nM as measured by ELISA.
Showed reduced p-SLP76 levels with increasing concentrations of the reagent via Western blot analysis.
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Cell Line:Jurkat cells
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Concentration:50 nM
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Incubation Time:0, 8, 12, 24, 48 h
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Result:HPK1 degradation became evident at 12 h, was nearly complete at 24 h and partially recovered at 48 h.
Chemical Information
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CAS No. 3034182-97-0
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Appearance Solid
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Molecular Weight 785.84
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Formula C43H43N7O8
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Color Light yellow to yellow
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SMILES
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCC(N4CCN(C5=CC=C(C6=CN=C(NC=C7C8=CC=C(OC)C(OC)=C8)C7=C6)C=C5)CC4)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (127.25 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, stored under nitrogen). 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, stored under nitrogen). 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 (273 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, stored under nitrogen). 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 |
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| DMSO | 1 mM | 1.2725 mL | 6.3626 mL | 12.7252 mL | 31.8131 mL |
| 5 mM | 0.2545 mL | 1.2725 mL | 2.5450 mL | 6.3626 mL | |
| 10 mM | 0.1273 mL | 0.6363 mL | 1.2725 mL | 3.1813 mL | |
| 15 mM | 0.0848 mL | 0.4242 mL | 0.8483 mL | 2.1209 mL | |
| 20 mM | 0.0636 mL | 0.3181 mL | 0.6363 mL | 1.5907 mL | |
| 25 mM | 0.0509 mL | 0.2545 mL | 0.5090 mL | 1.2725 mL | |
| 30 mM | 0.0424 mL | 0.2121 mL | 0.4242 mL | 1.0604 mL | |
| 40 mM | 0.0318 mL | 0.1591 mL | 0.3181 mL | 0.7953 mL | |
| 50 mM | 0.0255 mL | 0.1273 mL | 0.2545 mL | 0.6363 mL | |
| 60 mM | 0.0212 mL | 0.1060 mL | 0.2121 mL | 0.5302 mL | |
| 80 mM | 0.0159 mL | 0.0795 mL | 0.1591 mL | 0.3977 mL | |
| 100 mM | 0.0127 mL | 0.0636 mL | 0.1273 mL | 0.3181 mL |
PROTAC HPK1 Degrader-1 Related Classifications
HY-163372 Related Classifications
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