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別名: NVP-LDE225, Erismodegib 中文名稱:索尼德吉
Sonidegib是一種Smoothened(Smo)拮抗劑,抑制Hedgehog (Hh)信號通路,無細胞試驗中IC50分別為1.3 nM (小鼠)和2.5 nM(人)。Phase 3。
Sonidegib Chemical Structure
CAS: 956697-53-3
相關(guān)靶點 | Hedgehog Smoothened GLI | 點擊展開 |
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相關(guān)產(chǎn)品 | Cyclopamine GANT61 SAG (Smoothened Agonist) HCl Purmorphamine SANT-1 SAG (Smoothened Agonist) BMS-833923 HPI-4 (Ciliobrevin A) Taladegib (LY2940680) PF-5274857 Jervine Ciliobrevin D MK-4101 Sonic Hedgehog Rabbit Recombinant mAb JK184 | 點擊展開 |
相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 干細胞小分子化合物庫 GPCR小分子化合物庫 干細胞分化化合物庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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UACC 257 | Function assay | 10 μM | inhibits Hedgehog-GLI pathway | 23935925 | |
LOX IMVI | Function assay | 10 μM | inhibits Hedgehog-GLI pathway | 23935925 | |
Glioblastoma initiating cells | Function assay | ~10 μM | Inhibits Motility, Invasion, and Migration | 23482671 | |
Glioblastoma initiating cells | Function assay | ~10 μM | Inhibits the Expression of Genes Involved in Maintaining Pluripotency | 23482671 | |
Glioblastoma initiating cells | Function assay | ~10 μM | downregulates the SHH signaling pathway | 23482671 | |
Glioblastoma initiating cells | Cytoxicity assay | ~10 μM | induces apoptosis | 23482671 | |
Glioblastoma initiating cells | Function assay | ~10 μM | inhibits neurosphere formation | 23482671 | |
Glioblastoma initiating cells | Cytoxicity assay | ~10 μM | Inhibits Cell Viability | 23482671 | |
OS18 | Growth inhibitory assay | ~5 μM | reduces the proliferation | 23243595 | |
OS5 | Growth inhibitory assay | ~5 μM | reduces the proliferation | 23243595 | |
HeyA8MDR | Cytoxicity assay | ~10 μM | IC50=8 μM | 22553355 | |
HeyA8 | Cytoxicity assay | ~10 μM | IC50=18 μM | 22553355 | |
SKOV3TRip2 | Cytoxicity assay | ~10 μM | IC50=12 μM | 22553355 | |
SKOV3ip1 | Cytoxicity assay | ~10 μM | IC50=24 μM | 22553355 | |
A2780cp20 | Cytoxicity assay | ~10 μM | IC50=7.5 μM | 22553355 | |
A2780ip2 | Cytoxicity assay | ~10 μM | IC50=12 μM | 22553355 | |
LOX IMVI | Function assay | 10 μM | induces G1 cell cycle arrest | 23935925 | |
UACC 257 | Function assay | 10 μM | induces G1 cell cycle arrest | 23935925 | |
LOX IMVI | Cytoxicity assay | 10 μM | decreases tumor cell viability | 23935925 | |
UACC 257 | Cytoxicity assay | 10 μM | decreases tumor cell viability | 23935925 | |
LOX IMVI | Apoptosis assay | 10 μM | induces apoptosis | 23935925 | |
UACC 257 | Apoptosis assay | 10 μM | induces apoptosis | 23935925 | |
ACHN | Growth inhibitory assay | ~5 μM | IC50=2-3?μM | 25093491 | |
769-P | Growth inhibitory assay | ~5 μM | IC50=2-3?μM | 25093491 | |
786-O | Growth inhibitory assay | ~5 μM | IC50=2-3?μM | 25093491 | |
786-O SuR | Growth inhibitory assay | ~5 μM | IC50=2-3?μM | 25093491 | |
SP53 | Function assay | 30 μM | inhibits cell adhesion and migration | 26885608 | |
SP53 | Function assay | 30 μM | inhibits the VLA4-mediated FAK signaling pathway | 26885608 | |
HS5 | Function assay | 30 μM | inhibits cell adhesion and migration | 26885608 | |
HS27a | Function assay | 30 μM | inhibits cell adhesion and migration | 26885608 | |
SP53 | Cytoxicity assay | 30 μM | induces autophagy | 26885608 | |
Jeko | Cytoxicity assay | 30 μM | induces autophagy | 26885608 | |
U2OS | Function assay | 2 hrs | Displacement of [3H]cyclopamine from wild type Smo expressed in U2OS cells after 2 hrs by scintillation counting, Ki = 0.006 μM. | 23063522 | |
NIH/3T3 | Function assay | 24 hrs | Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells measured after 24 hrs by Gli-dual luciferase reporter gene assay, IC50 = 0.006 μM. | 27810591 | |
TM3 | Function assay | 48 hrs | Inhibition of Hh signaling pathway in mouse TM3 cells assessed as downregulation of Gli1 gene expression after 48 hrs by luciferase reporter gene assay, EC50 = 0.0012 μM. | 26976215 | |
NIH3T3 | Function assay | 48 hrs | Inhibition of SHH signaling pathway in mouse NIH3T3 cells measured after 48 hrs by Gli-luciferase reporter assay, IC50 = 0.0055 μM. | 24176396 | |
NIH3T3 | Function assay | 48 hrs | Inhibition of Sonic-induced hedgehog signalling in mouse NIH3T3 cells after 48 hrs by Gli-luciferase reporter assay, IC50 = 0.0055 μM. | 26820554 | |
NIH/3T3 | Function assay | Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells expressing wild type Smo assessed as reduction in Gli mRNA expression by RT-PCR method, IC50 = 0.0044 μM. | 27810591 | ||
NIH/3T3 | Function assay | Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells harboring Smo D477H mutant assessed as reduction in Gli mRNA expression by RT-PCR method, IC50 = 0.0227 μM. | 27810591 | ||
NIH/3T3 | Function assay | Inhibition of hedgehog signaling pathway expressed in mouse NIH/3T3 cells assessed as inhibition of hedgehog-induced Gli-2 accumulation at tip of primary cilia by DAPI staining based confocal microscopic analysis | 27810591 | ||
NIH/3T3 | Function assay | Inhibition of hedgehog signaling pathway in mouse NIH/3T3 cells assessed as inhibition of hedgehog-induced Smo-EGFP ciliary translocation by DAPI staining based confocal microscopic analysis | 27810591 | ||
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 | ||
Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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 | ||
MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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 | ||
Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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 | ||
SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
點擊查看更多細胞系數(shù)據(jù) |
產(chǎn)品描述 | Sonidegib是一種Smoothened(Smo)拮抗劑,抑制Hedgehog (Hh)信號通路,無細胞試驗中IC50分別為1.3 nM (小鼠)和2.5 nM(人)。Phase 3。 | ||||
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特性 | LDE225 是具有高效性和選擇性的使平滑的拮抗劑 | ||||
靶點 |
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體外研究(In Vitro) | ||||
體外研究活性 | Sonidegib (Erismodegib, NVP-LDE225)可在0.6-0.8μM劑量上抑制1nM-25nM Hh激動劑Ag1.5 處理的TM3熒光報告細胞系。[1] | |||
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細胞實驗 | 細胞系 | TM3Hh12 細胞 | ||
濃度 | 0 μM -10 μM | |||
孵育時間 | 30 分鐘 | |||
方法 | LDE225 用DMSO連續(xù)稀釋后加入空的分析平板中。TM3Hh12 細胞 (TM3 細胞含有Hh的應(yīng)答報告基因元件pTA-8xGli-Luc) 用含有5%的馬血清,2.5%的胎牛血清(FBS)和15 mM HEPES, pH 7.3的F12 Ham’s/DMEM (1:1)培養(yǎng)基培養(yǎng)。收集細胞時用胰酶消化,然后用含有5%的馬血清和15 mM HEPES, pH 7.3的F12 Ham’s/DMEM (1:1)培養(yǎng)基重懸,接著分鋪到分析板中。然后加入LDE225在37 °C ,5% CO2的培養(yǎng)箱中大約孵育30分鐘。接著加入1 nM 和25 nM 的Ag1.5到分析平板中,37 °C ,5% CO2的條件下培養(yǎng)。48小時后,向平板中加入Bright-Glo 或者 MTS試劑,測量492納米下的熒光值或者吸收峰。通過MTS法檢測Gli-驅(qū)動熒光素酶發(fā)光或吸光度信號,對濃度取Log(10)值做由非線性回歸曲線,確定IC 50值。數(shù)據(jù)處理使用R統(tǒng)計軟件包。 |
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實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
Western blot |
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