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Purmorphamine
Purmorphamine是第一個(gè)針對(duì)Smoothened蛋白開發(fā)的小分子激動(dòng)劑, 能夠直接結(jié)合并激活Smo,阻斷BODIPY-cyclopamine與Smo結(jié)合。
Adavivint (SM04690)
Adavivint (SM04690,Lorecivivint) is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ?150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular as
BMS-906024
BMS-906024 是一種口服有效,選擇性的 γ 分泌酶 (gamma secretase) 抑制劑 (GSI),GSIs 是一類小分子 Notch 抑制劑。BMS-906024 可阻止具有高口服生物利用度的所有四種 Notch 受體的激活,對(duì)于 Notch1,-2,-3 和 -4 受體,IC50s 分別為 1.6,0.7,3.4 和 2.9 nM。 BMS-906024 表現(xiàn)出針對(duì)多種人癌癥異種移植物的廣譜抗腫瘤活性。
SAG hydrochloride
Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
FLI-06
A Notch inhibitor
IMR-1
An inhibitor of Maml1 recruitment to chromatin
HA-1077 (hydrochloride)
A ROCK inhibitor
Gigantol
Gigantol是一種來(lái)自幾種藥用蘭花的聯(lián)芐基化合物。Gigantol對(duì)癌癥有潛在治療價(jià)值。Gigantol是Wnt/β-catenin通路的抑制劑。
JI051
JI051是一種Hes1-PHB2相互作用穩(wěn)定劑,能夠與癌癥相關(guān)蛋白伴侶prohibitin2(PHB2)相互作用,通過(guò)抑制Notch下游效應(yīng)基因Hes1來(lái)誘導(dǎo)細(xì)胞周期停滯。具有抗腫瘤作用。
Bruceine D
Bruceine D, isolated from Brucea javanica (L.) Merr. (Simaroubaceae), shows antineoplastic properties in various human cancers including pancreas, breast, lung, blood, bone, and liver. Bruceine D induces apoptosis in human chronic myeloid leukemia K562 ce
KY1220
KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells.
IMR-1A
IMR-1A, an acid metabolite of IMR-1, is a potent inhibitor of Notch with IC50 of 0.5 μM and Kd of 2.9 μM. IMR-1A exhibits anti-tumor activity.
BMS-983970
BMS-983970是Notch口服性抑制劑,用于抗癌研究。
Jagged-1 188-204
Jagged-1 (188-204) 是 JAG-1 蛋白的一個(gè)片段。JAG-1 是一種在培養(yǎng)的和原發(fā)性多發(fā)性骨髓瘤 (MM) 細(xì)胞中高度表達(dá)的 Notch 配體。JAG-1 誘導(dǎo)單核細(xì)胞衍生的人樹突狀細(xì)胞成熟。
DK419
DK419 是一種有效、可口服的 Wnt/β-catenin 信號(hào)通路抑制劑,IC50 值為 0.19 μM。DK419 能降低 Axin2,β-catenin,c-Myc,Cyclin D1 和 Survivin 能夠改變細(xì)胞內(nèi)耗氧率,誘導(dǎo) pAMPK 的產(chǎn)生。
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