PROTAC YAP degrader-1

Name: PROTAC YAP degrader-1
Brand: MedChemExpress
SKU: HY-168016
Rating: 4.5 (0 reviews)

製品番号: HY-168016 純度: 99.77%: Data Sheet SDS COA 取扱説明書
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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)).

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PROTAC YAP degrader-1 構造式

CAS 番号 : 3058483-58-9

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 887	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 887	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$405	在庫あり	Estimated Time of Arrival: December 31
10 mg	$650	在庫あり	Estimated Time of Arrival: December 31
25 mg	$1300	在庫あり	Estimated Time of Arrival: December 31
50 mg	$2100	在庫あり	Estimated Time of Arrival: December 31
100 mg	$3230	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 0 publication(s) in Google Scholar

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

YAP アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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^[1]. (Pink: YAP ligand (HY-168017); Blue: E3 ligase ligand; Black: linker (HY-140480)).

IC₅₀ & Target

YAP^[1]

Cellular Effect

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]

体外実験

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.

Immunofluorescence^[1]

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).

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-last	AUC_0-∞	MRT_0-∞
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

体内実験

PROTAC YAP degrader-1 (YZ-6) (35 mg/kg; i.p.; every 3 days; 24 days) achieves 82% tumor growth inhibition in a Huh7 hepatocellular carcinoma xenograft model in NSG mice, with associated reductions in tumor YAP, CTGF, and CYR61 levels and no observed body weight loss^[1].

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.

分子量

995.19

分子式

C₅₆H₆₂N₆O₉S

CAS 番号

3058483-58-9

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0048 mL	5.0242 mL	10.0483 mL
5 mM	0.2010 mL	1.0048 mL	2.0097 mL
10 mM	0.1005 mL	0.5024 mL	1.0048 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

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濃度 _（終了）

体積 _（終了）

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

純度: 99.77%

Select Batch:

データシート (275 KB) SDS (252 KB)

COA (250 KB) HNMR (373 KB) RP-HPLC (227 KB) LCMS (96 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Zhou C, et al. Exploring Degradation of Intrinsically Disordered Protein Yes-Associated Protein Induced by Proteolysis TArgeting Chimeras. J Med Chem. 2024;67(17):15168-15198. [Content Brief]

Complete Stock Solution Preparation Table

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