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Synonyms:
TEAD ligand-Linker Conjugate 3
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | TEAD ligand-Linker Conjugate 3 (A536) is an IAP-recruiting bifunctional degrader (IPD) in the ALP2 series, specifically targeting TEAD1, with a degradation DC50 of 110 nM for human TEAD1 and a maximum degradation efficiency (Dmax) of 51%. This compound binds effectively to cIAP1 and induces its degradation (IC50=122 nM), while also possessing good cell permeability. It is composed of ALP2 target protein ligand and PROTA Clinker, making it suitable for PROTAC synthesis. A536 demonstrates dose-dependent inhibition of cell proliferation in Hippo pathway-dependent human malignant mesothelioma cells and downregulates the transcriptional expression of the TEAD1 downstream target gene CTGF. Additionally, A536 is useful for studying mechanisms in malignancies with abnormal Hippo pathway activation, particularly in NF2-mutant mesothelioma. |
| Targets & IC50 | CIAP1:122 nM |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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