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Purmorphamine

別名：Shh Signaling Antagonist VI

Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.

Purmorphamine化学構造

CAS No. 483367-10-8

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代表番号: 045-509-1970|電子メール：[email protected]
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Purmorphamine関連製品

シグナル伝達経路

Hedgehog/Smoothened Signaling Pathways

Hedgehog/Smoothenedシグナル伝達経路

Hedgehog/Smoothened阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
HEK293T Function assay 5 uM 4 hrs Inhibition of BODIPY-cyclopamine binding to Smo N-terminal cysteine domain expressed in HEK293T cells at 5 uM after 4 hrs by fluorescence microscopy 16408088
HEK293T Function assay 5 uM 4 hrs Inhibition of BODIPY-cyclopamine binding to Smo C-terminal cytoplasmic domain expressed in HEK293T cells at 5 uM after 4 hrs by fluorescence microscopy 16408088
Shh Light2 Function assay 30 hrs Activation of Shh in mouse Shh Light2 cells after 30 hrs by luciferase reporter gene assay, EC50 = 1 μM. 16408088
C3H10T1/2 Function assay 6 days Activity at Smo in mouse C3H10T1/2 cells assessed as induction of cell differentiation into osteoblast incubated for 6 days by alkaline phosphatase assay, EC50 = 0.8 μM. 27429255
HEK293T Function assay 1 hr Inhibition of BODIPY-cyclopamine binding to Smo expressed in HEK293T cells after 1 hr by fluorescence microscopy, IC50 = 1.5 μM. 16408088
Shh Light2 Function assay 30 hrs Activation of Shh in mouse Shh Light2 cells assessed as beta-galactosidase activity after 30 hrs by luciferase reporter gene assay in presence of 100 nM 3-keto-N-aminoethyl-N'-aminocaproyldihydrocinnamoyl cyclopamine 16408088
C3H10T1/2 Function assay Induction of osteogenesis in mouse C3H10T1/2 cells assessed as induction of osteoblast specific marker alkaline phosphatase by immunofluorescence method, EC50 = 1 μM. 16408003
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
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生物活性

製品説明 Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
Targets
Smoothened [1]
(HEK293T cells)
~1.5 μM
In Vitro
In vitro

Purmorphamine activates the Hedgehog pathway by directly binds and activates Smoothened with IC50 of ~ 1.5 μM in compete with cyclopamine, a Smo antagonist. [1]

Purmorphamine is a potent inducer of osteogenesis in multipotent C3H10T1/2 cells. The EC50 (based on ALP expression) for Purmorphamine is 1 μM in C3H10T1/2 cells. Purmorphamine (1 μM) and BMP-4 (100 ng/mL) together increase ALP activity more than 90-fold in 3T3-L1 cells. [2]

In contrast to BMP-4, Purmorphamine induces osteogenesis by activating Hedgehog signaling in multipotent mesenchymal progenitor cells. [3]
Kinase Assay Binding assay
Smo binding assays are conducted with BODIPY-cyclopamine and Smo-overexpressing cells as previously described4,5, using CMV promoter-based, SV40 origin-containing expression constructs for Smo-Myc3, the deletion mutant SmoCRD (deletion of amino acids 68 to 182), and SmoCT (deletion of amino acids 556 to 793). HEK 293T cells are grown on poly-D-lysine-treated glass coverslips in 12-well plates until 70% confluency and then transfected with the appropriate expression construct (0.5 g/well) using FuGene 6 according the manufacturer
細胞実験 細胞株 C3H10T1/2 cell
濃度 0.5-10 μM
反応時間 4 days
実験の流れ

C3H10T1/2 cells are expanded in T175 flasks; cells at 13th passage are detached by trypsin/EDTA and diluted in the growth media. The resulting cell suspension is then plated into black clear bottom 384-well plates with 2500 cells/well in 100 µL growth medium using a Multi-dropTM liquid delivery system. After overnight incubation, cells attached to the bottom of the wells. A stock solution of each Purmorphamine in DMSO (500 nL) is delivered into corresponding well using a Mini TrakTM multiposition dispenser system to make a final concentration of 5μM of Purmorphamine. Cells are then incubated at 37 ℃ with 5% CO2 in air atmosphere. After 4 days, the medium is removed and 10 μL of passive lysis buffer is added into each well. After 5 min, 10 μL of alkaline phosphatase substrate solution is added to each well. After incubating 15 min at room temperature, the plates are read on an Acquest high-throughput plate reader following the manufacturer's protocol.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot Patch1 / Gli1 / LC3 / p62 26609469
Immunofluorescence SOX18 26588701
Growth inhibition assay Cell viability 26588701
In Vivo
In Vivo

Purmorphamine up-regulates ALP expression in human mesenchymal stem cell-based constructs on rats. [4]
動物実験 動物モデル Male C57BL/6J mouse pups
投与量 10 mg/kg
投与経路 i.p.

化学情報

分子量 520.62 化学式

C31H32N6O2
CAS No. 483367-10-8 SDF Download Purmorphamine SDFをダウンロードする
Smiles C1CCC(CC1)N2C=NC3=C(N=C(N=C32)OC4=CC=CC5=CC=CC=C54)NC6=CC=C(C=C6)N7CCOCC7
保管

In vitro
Batch:

DMSO : 4 mg/mL ( (7.68 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 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。

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