IWP-2

IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses. IWP-2 specifically inhibits CK1δ.

CAS No. 686770-61-6

サイズ	価格(税別)	在庫状況
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
1g	JPY 448500	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（92）

製品安全説明書

現在のバッチを見る：純度： 99.60%

99.60

IWP-2と併用されることが多い化合物

IWP-4

IWP-2 and IWP-4 are WNT inhibitors that are commonly used as small molecules for human cardiomyocytes (CMs) differentiation.

Moon SH, et al. Int J Stem Cells. 2017 May 30;10(1):1-11.

LGK-974

IWP-2 and LGK-974 decrease both sphere formation and transcriptional activities of CD44 in both RWPE-1 and PZ-HPV7 knock down (KD) cells.

Yun EJ, et al. Clin Cancer Res. 2016 Feb 1;22(3):670-9.

PRI-724

IWP-2 and PRI-724 induce apoptosis, affect HNSCC cell migration, and strongly affect β-catenin-dependent gene expression in HNSCC cells.

Kleszcz R, et al. Cell Oncol (Dordr). 2019 Aug;42(4):505-520.

VPA (Valproic acid)

IWP-2 promotes enterocyte differentiation, Valproic acid inhibits Lgr5+ stem cell differentiation.

Yin X, et al. Nat Methods. 2014 Jan;11(1):106-12.

IWP-2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	IWR-1-endo 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	Incubation Time	活性情報	PMID
mouse L cells	Function assay	24 h	Inhibition of porcupine-mediated Wnt signalling in mouse L cells after 24 hrs by SpringerImages-Topflash reporter assay, EC50=30 nM	23477365
HEK293T	Function assay	22 hrs	Inhibition of porcupine in HEK293T cells transfected with Wnt3A-expressing vector assessed as suppression of Wnt/beta-catenin signaling after 22 hrs by Super-top flash reporter gene assay, IC50 = 0.157 μM.	29630366
MIAPaCa2	Antiproliferative assay	48 hrs	Antiproliferative activity against human MIAPaCa2 cells after 48 hrs by MTT assay, EC50 = 1.9 μM.	29630366
SW620	Antiproliferative assay	48 hrs	Antiproliferative activity against human SW620 cells after 48 hrs by MTT assay, EC50 = 1.9 μM.	29630366
Capan1	Antiproliferative assay	48 hrs	Antiproliferative activity against human Capan1 cells after 48 hrs by MTT assay, EC50 = 2.05 μM.	29630366
PANC1	Antiproliferative assay	48 hrs	Antiproliferative activity against human PANC1 cells after 48 hrs by MTT assay, EC50 = 2.33 μM.	29630366
HEK293	Antiproliferative assay	48 hrs	Antiproliferative activity against human HEK293 cells after 48 hrs by MTT assay, EC50 = 2.76 μM.	29630366
Panc89	Antiproliferative assay	48 hrs	Antiproliferative activity against human Panc89 cells after 48 hrs by MTT assay, EC50 = 3.86 μM.	29630366
HT-29	Antiproliferative assay	48 hrs	Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, EC50 = 4.67 μM.	29630366
A818-6	Antiproliferative assay	48 hrs	Antiproliferative activity against human A818-6 cells after 48 hrs by MTT assay, EC50 = 8.96 μM.	29630366
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
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生物活性

製品説明

IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM in a cell-free assay, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses. IWP-2 specifically inhibits CK1δ.

特性

Selective inhibitor of Porcn-mediated Wnt secretion.

Targets

Wnt ^[1] (Cell-free assay)	^M82FCK1δ ^[3] (Cell-free assay)
27 nM	40 nM

In Vitro
In vitro	IWP-2 is useful in both regenerative medicine and anticancer efforts. IWP-2 inactivates Porcn, a membrane-bound O-acyltransferase (MBOAT), and selectively inhibits palmitoylation of Wnt. IWP-2 blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation. ^[1]
細胞実験	細胞株	L-Wnt-STF cells
	濃度	5 μM
	反応時間	24 h
	実験の流れ	L-Wnt-STF cells that exhibit constitutive Wnt pathway activation were incubated with IWR (10μM) and IWP (5μM) compounds for 24 hrs prior to lysis. Cellular lysates were subjected to Western blot analysis.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	Wnt5-a/b / β-catenin / Axin2 c-myc / Cyclin D1 / Survivin MMP7		27119499

参考
[1] Chen B, et al. Nat Chem Biol, 2009, 5(2), 100-107. [2] Castellana D, et al. PLoS Biol. 2014, 12(12):e1002002. [3] Balbina García-Reyes, et al. J Med Chem . 2018 May 10;61(9):4087-4102.

参考

化学情報

分子量	466.6	化学式	C₂₂H₁₈N₄O₂S₃
CAS No.	686770-61-6	SDF	Download IWP-2 SDFをダウンロードする
Smiles	CC1=CC2=C(C=C1)N=C(S2)NC(=O)CSC3=NC4=C(C(=O)N3C5=CC=CC=C5)SCC4
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:

DMF : 12.5 mg/mL

DMSO : Insoluble ( 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

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
=	×	×

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。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):