YAP-TEAD Inhibitor 1 (Peptide 17)

Catalog No.S8164 Batch:S816402

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Technical Data

Formula

C93H144ClN23O21S2

Molecular Weight 2019.86 CAS No. 1659305-78-8
Solubility (25°C)* In vitro DMSO 100 mg/mL (49.5 mM)
Water 100 mg/mL (49.5 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description YAP-TEAD Inhibitor 1 (Peptide 17) is a YAP-TEAD protein-protein interaction inhibitor which has potential usage in treatment of YAP-involved cancers with IC50 of 25 nM.
Targets
YAP/TEAD interaction [1]
(Cell-free assay)
25 nM
In vitro The engineered peptide significantly improves the potency in disrupting YAP-TEAD interaction in vitro[1]. This 17mer peptide demonstrates a single-digit micromolar affinity to TEAD1[2].

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , J Exp Clin Cancer Res. 2018, 37(1):228]

Selleck's YAP-TEAD Inhibitor 1 (Peptide 17) has been cited by 15 publications

NOX4-derived ROS Regulates Aerobic Glycolysis of Breast Cancer through YAP Pathway [ J Cancer, 2023, 14(13):2562-2573] PubMed: 37670970
NOX4-derived ROS Regulates Aerobic Glycolysis of Breast Cancer through YAP Pathway [ J Cancer, 2023, 14(13):2562-2573] PubMed: 37670970
Downregulation of circ-ZNF609 Promotes Heart Repair by Modulating RNA N6-Methyladenosine-Modified Yap Expression [ Research (Wash D C), 2022, 2022:9825916] PubMed: 35474903
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106 [ J Med Chem, 2022, 65(13):9206-9229] PubMed: 35763499
Aurintricarboxylic acid is a canonical disruptor of the TAZ-TEAD transcriptional complex [ PLoS One, 2022, 17(4):e0266143] PubMed: 35417479
Targeting the Hippo/YAP/TAZ signalling pathway: Novel opportunities for therapeutic interventions into skin cancers [ Exp Dermatol, 2022, 31(10):1477-1499] PubMed: 35913427
mTORC1 Promotes ARID1A Degradation and Oncogenic Chromatin Remodeling in Hepatocellular Carcinoma [ Cancer Res, 2021, 81(22):5652-5665] PubMed: 34429326
YAP signaling in preovulatory granulosa cells is critical for the functioning of the EGF network during ovulation [ Mol Cell Endocrinol, 2021, 541:111524] PubMed: 34856345
YAP/TAZ transcriptional co-activators create therapeutic vulnerability to verteporfin in EGFR mutant glioblastoma [ Clin Cancer Res, 2020, clincanres.0018.2020] PubMed: 33172899
Small Molecule Dysregulation of TEAD Lipidation Induces a Dominant-Negative Inhibition of Hippo Pathway Signaling [ Cell Rep, 2020, 31(12):107809] PubMed: 32579935

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.