Purmorphamine

製品コード:S3042 別名:Shh Signaling Antagonist VI

For research use only.

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

サイズ 価格(税別)
JPY 26400
JPY 80000

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(39)

製品安全説明書

Hedgehog/Smoothened阻害剤の選択性比較

相関Hedgehog/Smoothened製品

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.
ターゲット
Smoothened [1]
(HEK293T cells)
~1.5 μM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C3H10T1/2 M{ThbWZ2dmO2aX;uJIF{e2G7 Ml6wOkBl[Xm| NFryVYdC[3Srdnn0fUBifCCVbX:gbY4hdW:3c3WgR|NJOTCWMT:yJINmdGy|IHHzd4V{e2WmIHHzJIlv\HWldHnvckBw\iClZXzsJIRq\m[ncnXueIlifGmxbjDpcpRwKG:|dHXvZoxie3RiaX7jeYJifGWmIH\vdkA3KGSjeYOgZpkh[WytYXzpcoUheGixc4DoZZRie2ViYYPzZZktKEWFNUCgQUAxNjhizszNMi=> MnHaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd2MkmyOVUoRjJ5NEK5NlU2RC:jPh?=
Shh Light2 NELqe5VHfW6ldHnvckBie3OjeR?= MnTrN|AhcHK| M4jTTWFkfGm4YYTpc44hd2ZiU3joJIlvKG2xdYPlJHNpcCCOaXfoeFIh[2WubIOgZYZ1\XJiM{CgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFEh|ryPLh?= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjRyOEC4PEc,OTZ2MEiwPFg9N2F-
C3H10T1/2 NHTRSmdHfW6ldHnvckBie3OjeR?= NIXsOGpKdmS3Y4Tpc44hd2Zib4P0[Y9o\W6nc3nzJIlvKG2xdYPlJGM{UDFyVEGvNkBk\WyuczDhd5Nme3OnZDDhd{BqdmS3Y4Tpc44hd2Zib4P0[Y9jdGG|dDDzdIVkcW[rYzDtZZJs\XJiYXzrZYxqdmVicHjvd5Bp[XSjc3WgZpkhcW2vdX7v[ox2d3Knc3PlcoNmKG2ndHjv[EwhTUN3MDC9JFEh|ryPLh?= NYrMOHJSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[0NFgxODNpPkG2OFA5ODB|PD;hQi=>
HEK293T M1jyc2Z2dmO2aX;uJIF{e2G7 M1rLWFEhcHJ? NWHnfGltUW6qaXLpeIlwdiCxZjDCU2RKWFlvY4njcI9x[W2rbnWgZolv\GmwZzD0c{BUdW9iZYjwdoV{e2WmIHnuJGhGUzJ7M2SgZ4VtdHNiYX\0[ZIhOSCqcjDifUBndHWxcnXzZ4Vv[2VibXnjdo9{[2:yeTygTWM2OCB;IEGuOUDPxE1w MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjRyOEC4PEc,OTZ2MEiwPFg9N2F-
Shh Light2 NWq3co5QTnWwY4Tpc44h[XO|YYm= NVrBdmN3OzBiaILz NYniXWZySWO2aY\heIlwdiCxZjDTbIghcW5ibX;1d4UhW2iqIFzp[4h1OiClZXzsd{Bie3Onc4Pl[EBieyCkZYThMYdidGGldH;zbYRie2ViYXP0bZZqfHliYX\0[ZIhOzBiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTDpckBxemW|ZX7j[UBw\iBzMECgcm0hOy2tZYTvMW4u[W2rbn;leIh6dC2QJz3hcYlvd2OjcILvfYxlcWi7ZILvZ4lvdmGvb4nsJIN6[2yxcHHtbY5m M1;Sc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4NEC4NFg5Lz5zNkSwPFA5QDxxYU6=
HEK293T NFnQfZRHfW6ldHnvckBie3OjeR?= M32w[lUhfU1? NGXGeW01KGi{cx?= NGjacGxKdmirYnn0bY9vKG:oIFLPSGlRYS2leXPsc5BidWmwZTDibY5lcW6pIITvJHNudyCQLYTldo1qdmGuIHP5d5RmcW6nIHTvcYFqdiCneIDy[ZN{\WRiaX6gTGVMOjl|VDDj[YxteyCjdDC1JJVOKGGodHXyJFQhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCvaXPyc5Nkd3C7 NXK1Z3VZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[0NFgxQDhpPkG2OFA5ODh6PD;hQi=>
HEK293T MmSzSpVv[3Srb36gZZN{[Xl? MX[1JJVO NWDmUWg1PCCqcoO= M2fTU2lvcGmkaYTpc44hd2ZiQl;ETXB[NWO7Y3zvdIFucW6nIHLpcoRqdmdidH:gV41wKENvdHXycYlv[WxiY4n0c5Bt[XOvaXOg[I9u[WmwIHX4dJJme3OnZDDpckBJTUt{OUPUJINmdGy|IHH0JFUhfU1iYX\0[ZIhPCCqcoOgZpkh\my3b4Lld4NmdmOnIH3pZ5Jwe2OxcIm= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjRyOEC4PEc,OTZ2MEiwPFg9N2F-
SK-N-MC NH3rUGZyUFSVIHHzd4F6 M{nhS5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NW\iRXpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
アッセイ
Methods Test Index PMID
Western blot Patch1 / Gli1 / LC3 / p62 26609469
Immunofluorescence SOX18 26588701
Growth inhibition assay Cell viability 26588701
体内試験 Purmorphamine up-regulates ALP expression in human mesenchymal stem cell-based constructs on rats. [4]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
  • 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 × 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 × PBS buffer for 10 min at room temperature (1 mL/well), treated with 1 × PBS containing 10 mM glycine and 0.2% sodium azide for 5 min (1 mL/well), washed with 1 × PBS buffer (1 mL/well), and treated with the Purmorphamine-containing media described above for 4 h at room temperature.

細胞試験:[2]
  • 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.

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。

1mg/mL

化学情報

分子量 520.62
化学式

C31H32N6O2

CAS No. 483367-10-8
Storage 3年 -20°C
2年 -80°C in solvent
Smiles C1CCC(CC1)N2C=NC3=C(N=C(N=C32)OC4=CC=CC5=CC=CC=C54)NC6=CC=C(C=C6)N7CCOCC7

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

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。

便利ツール

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: Purmorphamineを買う | Purmorphamine ic50 | Purmorphamine供給者 | Purmorphamineを購入する | Purmorphamine費用 | Purmorphamine生産者 | オーダーPurmorphamine | Purmorphamine化学構造 | Purmorphamine分子量 | Purmorphamine代理店