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Purmorphamine

Purmorphamine

产品编号 T1810   CAS 483367-10-8
别名: Shh Signaling Antagonist VI

Purmorphamine (Shh Signaling Antagonist VI) 是平滑受体激动剂,EC50为 1 μM。它阻止 BODIPY-cyclopamine 与 Smo 结合。它也是成骨细胞分化的诱导剂。

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Purmorphamine Chemical Structure
Purmorphamine, CAS 483367-10-8
规格 价格/CNY 货期 数量
1 mg ¥ 396 现货
5 mg ¥ 890 现货
10 mg ¥ 1,250 现货
25 mg ¥ 2,650 现货
50 mg ¥ 3,450 现货
100 mg ¥ 4,990 现货
1 mL * 10 mM (in DMSO) ¥ 977 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Purmorphamine (T1810)
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纯度: 99.48%
纯度: 98.11%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo. It also is an inducer of osteoblast differentiation.
靶点活性 Smo:1.5 μM
体外活性 在大鼠中基于人间充质干细胞中,Purmorphamine 上调ALP表达.
体内活性 在全能C3H10T1/2 细胞中(EC50=1 μM),Purmorphamine能够诱导骨生成。Purmorphamine 与Smoothened直接结合,而激活Hedgehog通路(IC50=1.5 μM)。
激酶实验 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's protocols. Two days after transfection, the HEK 293T cells are incubated with DMEM containing 0.5% bovine calf serum, 5 nM BODIPY-cyclopamine, and varying concentrations of Purmorphamine (0, 1.5, or 5 ?M) (1 mL/well) for 1 h at 37 ℃. The Smo-overexpressing cells are then washed with 1 &times PBS buffer (1 mL/well), mounted with DAPI-containing medium, and visualized using a Leica DM4500B fluorescence microscope. For binding assays using fixed cells, the Smo-overexpressing HEK 293T cells are fixed with 3% paraformaldehyde in 1 &times PBS buffer for 10 min at room temperature (1 mL/well), treated with 1 &times PBS containing 10 mM glycine and 0.2% sodium azide for 5 min (1 mL/well), washed with 1 &times PBS buffer (1 mL/well), and treated with the Purmorphamine-containing media described above for 4 h at room temperature.
细胞实验 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 5 μM 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.(Only for Reference)
别名 Shh Signaling Antagonist VI
分子量 520.62
分子式 C31H32N6O2
CAS No. 483367-10-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 52.1 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9208 mL 9.6039 mL 19.2079 mL 48.0197 mL
5 mM 0.3842 mL 1.9208 mL 3.8416 mL 9.6039 mL
10 mM 0.1921 mL 0.9604 mL 1.9208 mL 4.802 mL
20 mM 0.096 mL 0.4802 mL 0.9604 mL 2.401 mL
50 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9604 mL
100 mM 0.0192 mL 0.096 mL 0.1921 mL 0.4802 mL

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TargetMol Library Books参考文献

1. Sinha S, et al. Nat Chem Biol, 2006, 2(1), 29-30. 2. Wu X, et al. J Am Chem Soc, 2002, 124(49), 14520-14521. 3. Wu X, et al. Chem Biol, 2004, 11(9), 1229-1238. 4. Faghihi F, Biomed Pharmacother, 2012, 3322(12).

TargetMol Library Books文献引用

1. Singh K, Nawabjan S A, Zhang L, et al. Discovery of small-molecule modulators of the secretin receptor: Purmorphamine as novel anti-hypertensive agent. European Journal of Medicinal Chemistry. 2022: 114642. 2. Mendonça L S, Henriques D, Fernandes V, et al.Graft-derived neurons and bystander effects are maintained for six months after human iPSC-derived NESC transplantation in mice’s cerebella.Scientific Reports.2024, 14(1): 3236.
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相关化合物库

该产品包含在如下化合物库中:
GPCR靶点分子库 膜蛋白靶向化合物库 已知活性化合物库 抗衰老化合物库 自噬库 干细胞分化化合物库 细胞重编程化合物库 活性脂质化合物库 Wnt/Hedgehog/Notch 通路化合物库 癌细胞分化化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Purmorphamine 483367-10-8 Autophagy GPCR/G Protein Stem Cells Hedgehog/Smoothened Smo inhibit Smoothened Inhibitor Shh Signaling Antagonist VI inhibitor

 

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