IWR-1-endo

別名:endo-IWR 1, IWR-1

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.

IWR-1-endo化学構造

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
JPY 22000 国内在庫あり
JPY 37500 国内在庫あり
JPY 94300 国内在庫あり
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]
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製品安全説明書

現在のバッチを見る: 純度: 99.94%
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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.

XAV-939


IWR-1-endo and XAV-939 use abrogates 17β-estradiol inhibition of HIV replication by inhibiting β-catenin signaling in HIV-infected peripheral blood mononuclear cells (PBMCs).

Szotek EL, et al. Virology. 2013 Sep 1;443(2):375-83.

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

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 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.
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
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]

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

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

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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)

mg/kg g μL

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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