Geldanamycin

製品コードS2713 別名:NSC 122750

Geldanamycin化学構造

分子量(MW):560.64

Geldanamycinは一種の天然なHSP90阻害剤で、Kd値が1.2μMですが、糖質ステロイド受容体(GR)/HSP連合を特異性的に妨害します。

サイズ 価格(税別)  
JPY 28220.00
JPY 44820.00
JPY 111220.00

カスタマーフィードバック(2)

  • Phenotypic effect of Genetic or Pharmacologic Compromise of the 477 Hsp70-StiA-Hsp90 Complex. The impact of each genetic modification on radial growth, conidiation, and response to various stress conditions was assessed after inoculation of a suspension of 104 conidia on glucose minimal medium (GMM) agar plates and incubation at 37ºC for 5 days.

    Antimicrob Agents Chemother, 2015, 10.1128/AAC.00946-15. Geldanamycin purchased from Selleck.

    C2C12 myoblasts were transfected with HA-tagged A17-PABPN1 constructs. Twenty-four hours post-transfection, cells were treated with CHX (10 μg/ml) alone or together with geldanamycin (2.5 μM) for the indicated times at 37°C. Lysates were blotted to show the expression of the proteins of interest. Band density was quantified and is shown in the line graph (right panels). Data are shown as the mean ± SEM (n = 5); **, P < 0.01.

    PLoS One, 2015, 10(9):e0138936.. Geldanamycin purchased from Selleck.

製品安全説明書

HSP (e.g. HSP90)阻害剤の選択性比較

生物活性

製品説明 Geldanamycinは一種の天然なHSP90阻害剤で、Kd値が1.2μMですが、糖質ステロイド受容体(GR)/HSP連合を特異性的に妨害します。
ターゲット
p185 [4]
(SKBr3 cells)
HSP90 (N-terminal domain) [1]
(Cell-free assay)
HSP90 [1]
(Cell-free assay)
70 nM 0.78 μM(Kd) 1.2 μM(Kd)
体外試験

Geldanamycin binds in the ATP-binding site in the N-terminus domain of Hsp90s (residues 1-220). Geldanamycin inhibits the ATPase activity of Hsp90 in a dose-dependent manner. [1] Geldanamycin causes a dose-dependent G2 arrest and reversible inhibiton o f entry into the S phase in A2780 human ovarian cell line. This inhibition is accompanied by p53 increase and finally demonstrated to be p53 dependent. [2] Geldanamycin causes polyubiquitination and proteasomal degradation of the p185 receptor protein-tyrosin kinase and shows a IC50 with 70 nM. [3, 4] Geldanamycin is a typical anti-tumor reagent, shows a mean GI50 with 0.18 μM against the panel of 60 human tumor cell lines. [5]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780 cells Mln0VJJwdGmoZYLheIlwdiCjc4PhfS=> MmrNR49ueG:3bnSge4F{KGW4YXz1ZZRm\CCob4KgZY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCxdnHybYFvKGOjcnPpco9u[SClZXzsJIxqdmViQUK3PFAtKEmFNUC9N{41KM7:TR?= MUexNVUyPDF2NR?=
SW620 cell NVm2XGtuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{nyPGlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKGOxbH;y[YN1[WxiY3HyZ4lvd22jIGPXOlIxKGOnbHygcIlv\XNuIFnDOVA:Pi5{IH7N Mlm0NVU3PTh6N{m=
MCF-7 cell NVTuSYg3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX;RTVdNUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgbJVu[W5iYoLlZZN1KGOjbnPldkBOS0ZvNzDj[YxtKGyrbnXzMEBKSzVyPU[uOUBvVQ>? MVixOVY2QDh5OR?=
SKBR3 cells M176eXBzd2yrZnXyZZRqd25iYYPzZZk> M1X0RVczKGh? Mnv5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDld5Rzd2enbjDy[YNmeHSxcjDk[YZq[2mnboSgbJVu[W5iU1vCVlMh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVgvPSCwTR?= NHrjZWkzOzZ2OEG4NC=>
MCF7 cells NF;OS|ZRem:uaX\ldoF1cW:wIHHzd4F6 NV3y[YlHPzJiaB?= M{\oPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDlfJBz\XO|aX7nJIV{fHKxZ3XuJJJm[2WydH;yJIFnfGW{IEeyJIhzeyxiSVO1NF06Njhibl2= NIm1WGwzOzZ2OEG4NC=>
MDA-kb2 cells MoeySpVv[3Srb36gZZN{[Xl? MX2xPEBp NVPK[41[UW6qaXLpeIlwdiCxZjDIV3A6OCCrbjDoeY1idiCPRFGtb4IzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDncJVkd2OxcoTpZ49q\CC{ZXPldJRwei2mZYDlcoRmdnRibIXjbYZmemG|ZTDlfJBz\XO|aX;uJIFnfGW{IEG4JIhzeyCkeTDmbZJm\my7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3ME2xNEBvVQ>? NVXPSVFjOjR7OES5N|Y>
human SK-BR-3 cells NEXQd5JRem:uaX\ldoF1cW:wIHHzd4F6 NVXNSmNpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1DWi1|IHPlcIx{NCCLQ{WwQVE2Njhibl2= MWKxPVg6Pjh2OB?=
HUVEC cells NIjLdZdEgXSxdH;4bYPDqGG|c3H5 MUW3NkBp NWD4SnlzS3m2b4TvfIlkcXS7IHHnZYlve3RiSGXWSWMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zOTDuUS=> Mlm1NlUzPzdyNke=
human HCT116 cells Mn;mS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMtKEeLNUC9NlEhdk1? M2nxNFE5OjR|N{Cz
K562 cell MlvqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX7Jcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBt\XWtZX3pZUBMPTZ{IHPlcIwhdGmwZYOsJGlEPTB;MkKuNUBvVQ>? NV;p[o9YOTV4NUi4O|k>
HT-29 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXfJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBkd2yxcnXjeIFtKGOjcnPpco9u[SCKVD2yPUBk\WyuIHzpcoV{NCCLQ{WwQVI1NjVibl2= M3H5S|E2PjV6OEe5
HCT116 cells NX:zdXhDWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUjsbmRNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nlibIXtbY5me2OnbnPlJIF{e2G7LDDFR|UxRTBwMEOg{txO Mn;INlE3ODV7N{W=
NCI-H1975 cells MYPQdo9tcW[ncnH0bY9vKGG|c3H5 NVfZUI92SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNuIFnDOVA:OzZibl2= M3:zT|IyPzF3MU[1
human DLD1 cells NF3ve3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{DiRmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGRNTDFiY3XscJMtKEeLNUC9N|chdk1? NETYblQyQDJ2M{ewNy=>
human A431 cells MlHrR5l1d3SxeHnjxsBie3OjeR?= MUK3NkBp NIS0W2dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFAhdk1? NHnY[HAzPTJ5N{C2Oy=>
human HepG2 cells MXPDfZRwfG:6aXRCpIF{e2G7 M4nLS|czKGh? MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSwJI5O MVyyOVI4PzB4Nx?=
human BGC823 cells MWHDfZRwfG:6aXRCpIF{e2G7 MXW3NkBp MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCS2M5OjNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20NEBvVQ>? Mn7tNlUzPzdyNke=
human SKBR3 cells NFvFNpFEgXSxdH;4bYPDqGG|c3H5 M3rxN|czKGh? NHm5VFBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubzDhd5NigSxiSVO1NF01OSCwTR?= NYS5NmFpOTl2MEW1Nlg>
human MDA-MB-231 cells Mmr6R5l1d3SxeHnjxsBie3OjeR?= MXO3NkBp NXKyZXBHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUWwJI5O MWGyOVI4PzB4Nx?=
human A549 cells MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1q3NGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGE2PDliY3XscJMtKEeLNUC9OlQhdk1? NHr2T3EyQDJ2M{ewNy=>
Sf9 cells M1fNfmZ2dmO2aX;uJIF{e2G7 NUPWblJrTGm|cHzhZ4Vu\W62IH;mJGdONUKRRFnQXUBnem:vIHj1cYFvKG[3bHygcIVv\3SqIFjTVFkxKGGucHjhJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3cz3pcoZm[3SnZDDT[lkh[2WubIOgZYZ1\XJiMU[gbJJ{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEmFNUC9O|Qhdk1? M1fC[lI1PzVzNESx
human U87MG cells MkLqVJJwdGmoZYLheIlwdiCjc4PhfS=> NYnTRoc4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVPFdOTyClZXzsd{whUUN3ME24PUBvVQ>? MoDnNlE4OTVzNkW=
human A549 cells MVPDfZRwfG:6aXRCpIF{e2G7 MYi3NkBp MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;OUegcm0> M37CbVI2Ojd5ME[3
mouse P19 cells NGjBTo5EgXSxdH;4bYPDqGG|c3H5 MWOxPEBp Moj3R5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgVFE6KGOnbHzzJIFnfGW{IEG4JIhzeyxiSVO1NF0xNjFizszN NFn4SpAyPzR2MkW2OS=>
human HL7702 cells NVLMZ3NZS3m2b4TvfIlkyqCjc4PhfS=> NUXaOnZnPzJiaB?= MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUFc4ODJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlE1OSEQvF2= MYiyOVI4PzB4Nx?=
human A549 cells MXLDfZRwfG:6aXRCpIF{e2G7 MknQNkBl[Xm| NFXCWWpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFIh\GG7czDifUBCdGGvYYLCcJVmKGG|c3H5MEBKSzVyPUCuNVUh|ryP M2n3VVI{QTR5N{m0
human A431 cells NWXpfmYxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmWwO|IhcA>? NW\qW|VHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJIFnfGW{IEeyJIhzeyxiSVO1NF0xNjJizszN MojtNlA3PTV{M{e=
human HepG2 cells MYDDfZRwfG:6aXRCpIF{e2G7 M4G3fmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkOg{txO M1TmNFI{PjV4NUW2
human SW480 cells NFmxO|lEgXSxdH;4bYPDqGG|c3H5 NIDiRVI4OiCq NGmy[YtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXzR6MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOzFizszN NE\DT5EzPTJ5N{C2Oy=>
human LNCAP cells NEfETVBEgXSxdH;4bYPDqGG|c3H5 MVS3NkBp MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMUmNCWCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuOFMh|ryP M2fSNVI2OTB3OUK0
human LS174T cells NYGwTHNmS3m2b4TvfIlkyqCjc4PhfS=> NHvaNYJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNWzF5NGSgZ4VtdHNiYomgUXRUKGG|c3H5MEBKSzVyPUCuOFUh|ryP NIKzNZUyPzB|NEGzOS=>
human HeLa cells M1\RVmN6fG:2b4jpZ:Kh[XO|YYm= NFXURWI4OiCq Ml;nR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuO|k5KM7:TR?= NX;qepBNOjV{N{ewOlc>
rat L6 cells NH3QNW5EgXSxdH;4bYPDqGG|c3H5 MV:3NkBp NI\DUHJEgXSxdH;4bYNqfHliYXfhbY5{fCC{YYSgUFYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFHsZY1ieiCEbIXlJIF{e2G7LDDJR|UxRTVizszN MnXWNlQ2QDB3M{G=
human MCF7 cells NF;oOXNEgXSxdH;4bYPDqGG|c3H5 MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiSVO1NF06NjZizszN NUPGcJgzOTl3NkCzOVM>
human MCF7 cells NVTvXZJ{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmPVS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjDkZZl{KGK7IGPSRkBie3OjeTygS2k2OD1|NT62JO69VQ>? NWPaO4dbOTd6NkmwPVg>
HEK293T cells MnTaSpVv[3Srb36gZZN{[Xl? NUW5U3lbUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBmgHC{ZYPz[YQhcW5iSFXLNlk{XCClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MlHnNVg1ODh5MUO=
human Jurkat cells Mo\rSpVv[3Srb36gZZN{[Xl? M{XQNGlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiTl[tb4FxeGGEIHHjeIl3[XSrb36g[ZhxemW|c3XkJIlvKE[DRFSg[IVncWOrZX70JIh2dWGwIFr1dotifCClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= NGfqOFIyQDRyOEexNy=>
human SKBR3 cells M3;LWGZ2dmO2aX;uJIF{e2G7 Mo\NNlQhcA>? NIjLTIpKdmirYnn0bY9vKG:oIFjzdFkxNW2nZHnheIVlKEiHUkKg[IVoemGmYYTpc44hcW5iaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdB?= NYPhNGw{OTh6MU[xNVE>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 Geldanamycin (50 mg//kg) shows 30% inhibition on pl85-associated phosphotyrosine levels in FRE/erbB-2 mice. [6]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

Isothermal Titration Calorimetry (ITC) of Nucelotide Binding:

The titration experiments are performed using the MSC system. In each experiment, 16 aliquots of 15 μL of geldanamycin (300 μM in 1% DMSO) are injected into 1.3 mL of protein (31 μM in 20 mMTris-HCl, pH 7.5, 1 mMEDTA) at 25 °C, and the resulting data are fit after subtracting the heats of dilution. Heats of dilution are determined in separate experiments from addition of geldanamycin into buffer and buffer into protein. No evidence for binding of DMSO in the nucleotide binding site is observed. Titration data are fit using a nonlinear least-squares curve-fitting algorithm with three floating variables: stoichiometry, binding constant (Kb) 1/Kd), and change of enthalpy of interaction (ΔH°). Dissociation constants estimated for geldanamycin binding to intact yeast Hsp90 is 1.22 μM, and for binding to Hsp90 N-terminal domain is 0.78 μM. No meaningful heat is observed with binding to the C-terminal fragment.
細胞試験:

[2]

+ 展開
  • 細胞株: A2780 human ovarian cell line
  • 濃度: 0.001-10 μM
  • 反応時間: 3 hours
  • 実験の流れ:

    Exponentially growing cells are treated with Geldanamycin and at various times DNA synthesis is assessed by incorporation of bromodeoxyuridine (BrdUrd) and flow cytometric analysis. No marked difference in total cell number is noted during this time course for treated and untreated cultures. BrdUrd (10 μM) is incorporated over a 4-h incubation period at 37 °C and cells are harvested and fixed in 70% ethanol. After denaturation of the DNA with 2 N HC1, cells are incubated with an anti-BrdUrd mouse monoclonal antibody followed by a fluorescein isothiocyanate (FITC)-linked goat anti-mouse IgG. Cells are stained for 30 minutes at room temperature with propidium iodide and analysed by flow cytometry using a Coulter EPICS Profile Analyzer.


    (参考用のみ)
動物試験:

[6]

+ 展開
  • 動物モデル: FRE/erbB-2 tumors in nu/nu mice
  • 製剤: Geldanamycin is dissolved in DMSO.
  • 投薬量: 50 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 36 mg/mL (64.21 mM) warming
Water Insoluble
Ethanol Insoluble

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 560.64
化学式

C29H40N2O9

CAS No. 30562-34-6
保管
別名 NSC 122750

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

HSP (e.g. HSP90)信号経路図

HSP (e.g. HSP90) Inhibitors with Unique Features

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