- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
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IWR-1-endo
別名: endo-IWR 1, IWR-1
IWR-1-endo (endo-IWR 1, IWR-1)是一種Wnt通路抑制劑，在表達(dá) Wnt3A 的 L-細(xì)胞中IC50為180 nM，誘導(dǎo)Axin2蛋白水平，并通過穩(wěn)定Axin骨架破壞復(fù)合體來促進(jìn)β-catenin磷酸化。
IWR-1-endo Chemical Structure
CAS: 1127442-82-3
產(chǎn)品質(zhì)控
批次：
純度：
99.94%
99.94
常與IWR-1-endo一起在實(shí)驗(yàn)中被使用的化合物
IWR-1-endo和CHIR99021在一定程度上支持人前列腺上皮細(xì)胞 (PrEC) 的連續(xù)細(xì)胞增殖。
IWR-1-endo和WH-4-023以及其他細(xì)胞因子用于制備3i/LAF培養(yǎng)基,培養(yǎng)豬E10原腸胚形成前外胚層(pgEpiSC)。
IWR-1-endo和SB431542是WNT和SMAD抑制劑，用于補(bǔ)充第19天的神經(jīng)誘導(dǎo)培養(yǎng)基。
IWR-1-endo和XAV-939通過抑制HIV感染的PBMCs中的β-連環(huán)蛋白信號(hào)傳導(dǎo)來消除17β-雌二醇對(duì)HIV復(fù)制的抑制。
與IWR-1-endo相比，ICG-001顯著減少U87細(xì)胞中核酸β-catenin的積累。
IWR-1-endo相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | WNT β-catenin Wnt/β-catenin | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)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 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 干細(xì)胞小分子化合物庫 GPCR小分子化合物庫 干細(xì)胞分化化合物庫 | 點(diǎn)擊展開 |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | IWR-1-endo (endo-IWR 1, IWR-1)是一種Wnt通路抑制劑，在表達(dá) Wnt3A 的 L-細(xì)胞中IC50為180 nM，誘導(dǎo)Axin2蛋白水平，并通過穩(wěn)定Axin骨架破壞復(fù)合體來促進(jìn)β-catenin磷酸化。 | ||
|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | IWR-1 和XAV939作為Wnt通路的可逆抑制劑，在體內(nèi)外具有相似的藥理作用，IWR-1通過與Axin相互作用而發(fā)揮效果,而XAV939直接與TNKS結(jié)合。[1] |
|||
|---|---|---|---|---|
| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | E-cadherin / N-cadherin / Snail / Vimentin p-Akt / Akt Survivin |
|
26450645 | |
化學(xué)信息&溶解度
| 分子量 | 409.44 | 分子式 | C25H19N3O3 |
| CAS號(hào) | 1127442-82-3 | SDF | -- |
| Smiles | C1C2C=CC1C3C2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)NC5=CC=CC6=C5N=CC=C6 | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 82 mg/mL ( (200.27 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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