IWR-1-endo

別名：endo-IWR 1, IWR-1

製品コード：S7086 純度：99.94%

IWR-1-endo (endo-IWR 1, IWR-1) is a Wnt pathway inhibitor with IC50 of 180 nM in L-cells expressing Wnt3A, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes.

CAS No. 1127442-82-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
25mg	JPY 37500	国内在庫あり
100mg	JPY 94300	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（130）

製品安全説明書

現在のバッチを見る：純度： 99.94%

99.94

IWR-1-endoと併用されることが多い化合物

Laduviglusib (CHIR-99021)

IWR-1-endo and CHIR99021 support continuous cell proliferation to certain degrees in human prostate epithelial cells (PrECs).

Zhang C, et al. Cell Rep. 2018 Oct 16;25(3):598-610.e5.

WH-4-023

IWR-1-endo and WH-4-023 along with other small molecules and cytokines are used for the preparation of 3i/LAF medium to culture Pig pluripotent stem cell lines E10 pregastrulation epiblasts (pgEpiSCs).

Zhi M, et al. Cell Res. 2022 Apr;32(4):383-400.

SB431542

IWR-1-endo and SB431542 are WNT and SMAD inhibitors that are used to supplement neural induction media for the 1st 9 days.

Popova G, et al. Elife. 2023 Jul 20;12:RP87696.

ICG-001

ICG-001 significantly reduces the accumulation of the nucleic β-catenin in U87 cells than IWR-1-endo.

Gao L, et al. PLoS One. 2017 Aug 24;12(8):e0181346.

IWR-1-endo関連製品

関連ターゲット	WNT β-catenin Wnt/β-catenin	もっと見る
関連製品	IWP-2 SKL2001 BML-284 (Wnt agonist 1) PRI-724 Salinomycin (from Streptomyces albus) FH535 PNU-74654 LF3 KYA1797K KY02111 iCRT3 Adavivint (SM04690) MSAB Isoquercitrin IQ-1 iCRT14 CCT251545 Isoxazole 9 (ISX-9) JW55 Methyl Vanillate M435-1279 WAY-262611 JW74	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Stem Cell Signaling Compound Library GPCR Compound Library Stem Cell Differentiation Compound Library	もっと見る

シグナル伝達経路

Wnt/beta-cateninシグナル伝達経路

Wnt/beta-catenin阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
DLD1	Function assay	1 to 20 uM	24 hrs	Inhibition of tankyrase in human DLD1 cells assessed as inhibition of TCF-dependent transcriptional activity at 1 to 20 uM after 24 hrs by dual luciferase reporter gene assay	24527792
DLD1	Cytotoxicity assay	1 to 20 uM	10 days	Cytotoxicity against human DLD1 cells assessed as growth inhibition at 1 to 20 uM measured on day 10 by crystal violet staining	24527792
HT29	Function assay	25 uM	24 hrs	Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity at 25 uM after 24 hrs by dual luciferase reporter gene assay relative to control	24950489
HT29	Function assay	25 uM	24 hrs	Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity at 25 uM after 24 hrs by dual luciferase reporter gene assay relative to control in presence of GSK-3beta inhibitor LiCl	24950489
HT29	Function assay	25 uM	24 hrs	Inhibition of Wnt/beta-catenin signaling in human HT29 cells assessed as increase in axin2 mRNA expression at 25 uM after 24 hrs by quantitative real-time PCR assay	24950489
DLD1	Function assay	10 uM		Induction of Axin2 in human DLD1 cells overexpressing IWR-IS assessed as decrease in Wnt pathway activity at 10 uM by STF reporter assay method	19125156
HT29	Function assay		24 hrs	Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control, IC50 = 24.4 μM.	24950489
L-Wnt-STF	Function assay		24 hrs	Inhibition of TNKS-1 in mouse L-Wnt-STF cells assessed as disruption of Wnt signaling after 24 hrs by luciferase reporter gene assay, IC50 = 0.131 μM.	24527792
L-Wnt-STF	Function assay		24 hrs	Inhibition of TNKS-2 in mouse L-Wnt-STF cells assessed as disruption of Wnt signaling after 24 hrs by luciferase reporter gene assay, IC50 = 0.056 μM.	24527792
SW480	Function assay		40 to 48 hrs	Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs, IC50 = 0.25 μM.	23701517
SW480	Function assay		24 hrs	Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method, EC50 = 2.5 μM.	23701517
BL21 (DE3)	Function assay		90 mins	Activity of N-terminus hexaHis-tagged human TNSK2 expressed in Escherichia coli BL21 (DE3) cells using biotinylated NAD+ as substrate after 90 mins by Western blot analysis, EC50 = 0.2 μM.	22233320
DLD1	Function assay		2 hrs	Induction of Axin2 stabilization in human DLD1 cells assessed as decreased transcription of Axin2 after 2 hrs by RT-PCR method	19125156
HEK293T	Function assay			Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay, IC50 = 0.026 μM.	22191557
HEK293	Function assay			Displacement of IWR-PB from Axin2 in HEK293 cells by Western blot method	19125156
DLD1	Function assay			Inhibition of Axin2 protein degradation in human DLD1 cells by Western blot analysis	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Thr41 phosphorylated beta-casein levels by Western blot analysis	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Ser37 phosphorylated beta-casein levels by Western blot analysis	19125156
DLD1	Function assay			Decrease in beta-casein accumulation in human DLD1 cells expressing in APC mutant	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells assessed as decrease in free beta-casein levels by Western blot analysis	19125156
DLD1	Function assay			Induction of Axin2 stabilization in human DLD1 cells assessed as inhibition of Wnt/beta-casein pathway	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Ser33 phosphorylated beta-casein levels by Western blot analysis	19125156
DLD1	Function assay			Induction of Axin2 accumulation in human DLD1 cells by Western blot analysis	19125156
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生物活性

製品説明

Targets

Wnt ^[1]
(L-cells expressing Wnt3A)

180 nM

In Vitro
In vitro	Although both IWR-1 and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects both in vitro and in vivo, IWR-1 exerts its effect via interaction with Axin, while XAV939 binds TNKS directly. ^[1]
細胞実験	細胞株	Pig EpiSCs
	濃度	2.5 μM
	反応時間	2 days
	実験の流れ	For neural induction, the 3i/LAF culture medium was replaced with neural induction medium I (2.5 μM IWR-1-endo, 5 μM SB431542, and 10 ng/mL FGF2 in BM) on day 2 after pgEpiSC passage.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	E-cadherin / N-cadherin / Snail / Vimentin p-Akt / Akt Survivin		26450645

In Vivo
In Vivo	IWR-1 is a β‐catenin inhibitor.^[3]

参考
[1] Lu J, et al. Bioorg Med Chem Lett, 2009, 19(14), 3825-3827. [2] Zhi M, et al. Cell Res. 2022 Apr;32(4):383-400. [3] Wang L, et al. Clin Transl Med. 2022 May;12(5):e743.

参考

化学情報

分子量	409.44	化学式	C₂₅H₁₉N₃O₃
CAS No.	1127442-82-3	SDF	--
Smiles	C1C2C=CC1C3C2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)NC5=CC=CC6=C5N=CC=C6
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 82 mg/mL ( (200.27 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 Corn oil	1.5mg/ml (3.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.1mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.5mg/ml (3.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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