PROTAC YAP degrader-1
Based on 1 Customer Validation
PROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC50=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma.
(Pink: YAP ligand (HY-168017); Blue: E3 ligase ligand; Black: linker (HY-140480)).
For research use only. We do not sell to patients.
- Purity: 99.77%
- CAS No.: 3058483-58-9
- Formula: C56H62N6O9S
- Molecular Weight:995.19
-
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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Stem Cell Signaling Compound Library
HY-L017
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Transcription Factor-Targeted Library
HY-L090
-
Anti-Liver Cancer Compound Library
HY-L101
-
PROTAC Library
HY-L151
Biological Activity
YAP[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | IC50 |
2.9 μM
Compound: YZ-6
|
Antiproliferative activity against human Huh-7 cells overexpressing YAP assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Antiproliferative activity against human Huh-7 cells overexpressing YAP assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 39189384] |
| NCI-H226 | IC50 |
15.3 μM
Compound: YZ-6
|
Antiproliferative activity against NF2 deficient- human NCI-H226 cells assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
Antiproliferative activity against NF2 deficient- human NCI-H226 cells assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
|
[PMID: 39189384] |
PROTAC YAP degrader-1 (YZ-6) potently inhibits the proliferation of Huh7 hepatocellular carcinoma cells and NCI-H226 mesothelioma cells, with IC50 values of 2.9 μM and 15.3 μM at 96 h, respectively. Moreover, it exhibits improved selectivity relative to normal hepatocytes compared with Sorafenib (HY-10201)[1].
PROTAC YAP degrader-1 (2.5-20 μM; 48 h) inhibits the expression of CTGF in NCI-H226 cells[1].
PROTAC YAP degrader-1 (20 μM; 12-48 h) induces time-dependent degradation of YAP protein, achieving nearly complete degradation at 48 h in NCI-H226 and Huh7 cells[1].
PROTAC YAP degrader-1 (5-20 μM; 12 h) reduces YAP protein levels and nuclear YAP concentrations in Huh7 cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Huh7 cells
-
Concentration:5, 10, 20 μM
-
Incubation Time:12 h
-
Result:Reduced both integrated and mean YAP intensity in the nucleus in a concentration-dependent manner.
Caused significant decreases observed at all tested concentrations (5, 10, 20 μM).
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-last | AUC0-∞ | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 35 mg/kg | i.p. | 13.3 h | 3.33 h | 193 ng/mL | 1943 ng·h/mL | 2692 ng·h/mL | 19.9 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:NSG (male, 6 weeks old, subcutaneous xenograft of 5×106 Huh7 cells)[1]
-
Dosage:35 mg/kg
-
Administration:i.p.; every 3 days; 24 days
-
Result:Achieved a tumor growth inhibition (TGI) rate of 82%.
Reduced levels of YAP protein, along with reduced levels of YAP/TEAD target genes CTGF and CYR61 in harvested tumor tissues.
Caused no significant changes in mouse body weight throughout the treatment period.
Chemical Information
-
CAS No. 3058483-58-9
-
Appearance Solid
-
Molecular Weight 995.19
-
Formula C56H62N6O9S
-
Color Off-white to light yellow
-
SMILES
O=C(N[C@@H](C)C1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)NC(CCOCCOCCOC4=CC=C(C=C4OC)C5=C(C(C6=CC=CC=C6N7)=NC(C8=CC=CC=C8)=C5)CC7=O)=O)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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 (100.48 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
-
Data Sheet (275 KB)
-
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)
-
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0048 mL | 5.0242 mL | 10.0483 mL | 25.1208 mL |
| 5 mM | 0.2010 mL | 1.0048 mL | 2.0097 mL | 5.0242 mL | |
| 10 mM | 0.1005 mL | 0.5024 mL | 1.0048 mL | 2.5121 mL | |
| 15 mM | 0.0670 mL | 0.3349 mL | 0.6699 mL | 1.6747 mL | |
| 20 mM | 0.0502 mL | 0.2512 mL | 0.5024 mL | 1.2560 mL | |
| 25 mM | 0.0402 mL | 0.2010 mL | 0.4019 mL | 1.0048 mL | |
| 30 mM | 0.0335 mL | 0.1675 mL | 0.3349 mL | 0.8374 mL | |
| 40 mM | 0.0251 mL | 0.1256 mL | 0.2512 mL | 0.6280 mL | |
| 50 mM | 0.0201 mL | 0.1005 mL | 0.2010 mL | 0.5024 mL | |
| 60 mM | 0.0167 mL | 0.0837 mL | 0.1675 mL | 0.4187 mL | |
| 80 mM | 0.0126 mL | 0.0628 mL | 0.1256 mL | 0.3140 mL | |
| 100 mM | 0.0100 mL | 0.0502 mL | 0.1005 mL | 0.2512 mL |
PROTAC YAP degrader-1 Related Classifications
HY-168016 Related Classifications
Powered by Bioz