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YAP-TEAD Inhibitor 1 (Peptide 17) YAP inhibitor

Name: YAP-TEAD Inhibitor 1 (Peptide 17)
Brand: Selleck Chemicals
SKU: S8164
Availability: InStock
Rating: 5 (18 reviews)

Cat.No.S8164

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.

Chemical Structure

Molecular Weight: 2019.86

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.56%

99.56

Related Targets	TEAD MAP4K LATS MST
Related Products	CA3 (CIL56) Super-TDU TED-347

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Bel-7404 cells	Function assay				Inhibition of YAP/ GST-TEAD1 interaction in human Bel-7404 cells by GST pull-down assay, Kd=0.015 μM	25221655
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	2019.86	Formula	C₉₃H₁₄₄ClN₂₃O₂₁S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1659305-78-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCCC1NC(=O)C(CCCCN)NC(=O)C(CCCNC(N)=N)NC(=O)C(CC(C)C)NC(=O)C(CCSSCC(NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CO)NC(=O)C(C)NC(=O)C3CCCN3C1=O)C(=O)NC(CCCCN)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(CCC(O)=O)C(N)=O)NC(=O)C(C

Solubility

In vitro
Batch:

Water : 40 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Clear solution	5% H2O 1 40% PEG 300 2 5% Tween 80 3 ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (0.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified H2O stock solution to 400 μL of PEG 300, mix evenly to clarify; add 50 μL of Tween 80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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].
References	https://pubmed.ncbi.nlm.nih.gov/25221655/ https://pubmed.ncbi.nlm.nih.gov/25384421/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Is it cell permeable?

Answer:
The following paper states that the cyclic YAP petide at N terminus may improve the cell permeability: “Targeting Hippo pathway by specific interruption of YAP-TEAD interaction using cyclic YAP-like peptides”. It may have appeared in this context.

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