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 在庫  
JPY 54715.44 あり
JPY 24477.96 あり
JPY 38876.76 あり
JPY 96471.96 あり

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 NYrmbFV1WHKxbHnm[ZJifGmxbjDhd5NigQ>? M13Gd2NwdXCxdX7kJJdieyCndnHseYF1\WRiZn;yJIFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5ib4\hdolidiClYYLjbY5wdWFiY3XscEBtcW6nIFGyO|gxNCCLQ{WwQVMvPCEQvF2= MYCxNVUyPDF2NR?=
SW620 cell MlfJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NInpelJKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiClb3zvdoVkfGGuIHPhdoNqdm:vYTDTW|YzOCClZXzsJIxqdmW|LDDJR|UxRTZwMjDuUS=> M3XIU|E2PjV6OEe5
MCF-7 cell M3XSdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVLYWFAzUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgbJVu[W5iYoLlZZN1KGOjbnPldkBOS0ZvNzDj[YxtKGyrbnXzMEBKSzVyPU[uOUBvVQ>? MXKxOVY2QDh5OR?=
SKBR3 cells NInCPZhRem:uaX\ldoF1cW:wIHHzd4F6 NUXn[ZRjPzJiaB?= M3XQPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4Sg[ZN1em:pZX6gdoVk\XC2b4Kg[IVncWOrZX70JIh2dWGwIGPLRnI{KGOnbHzzJIFnfGW{IEeyJIhzeyxiSVO1NF05NjVibl2= NUH4[3pNOjN4NEixPFA>
MCF7 cells NY\5XFIxWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1e0cVczKGh? NF\jUHhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOg[ZhxemW|c3nu[{Bme3S{b3flckBz\WOncITvdkBi\nSncjC3NkBpenNuIFnDOVA:QS56IH7N MXiyN|Y1QDF6MB?=
MDA-kb2 cells M4nTPWZ2dmO2aX;uJIF{e2G7 NEXzSJAyQCCq NIXRXVJKdmirYnn0bY9vKG:oIFjTVFkxKGmwIHj1cYFvKE2GQT3rZlIh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHfseYNw[2:{dHnjc4llKHKnY3XweI9zNWSncHXu[IVvfCCudXPp[oVz[XOnIHX4dJJme3Orb36gZYZ1\XJiMUigbJJ{KGK7IH\pdoVndHlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUGwJI5O MknyNlQ6QDR7M{[=
human SK-BR-3 cells M3nLUHBzd2yrZnXyZZRqd25iYYPzZZk> MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVLSMVMh[2WubIOsJGlEPTB;MUWuPEBvVQ>? MYKxPVg6Pjh2OB?=
HUVEC cells Moi0R5l1d3SxeHnjxsBie3OjeR?= MV63NkBp M4jZcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEiXVlXDJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OTlibl2= Mn7sNlUzPzdyNke=
human HCT116 cells M3TzRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMtKEeLNUC9NlEhdk1? MUmxPFI1OzdyMx?=
K562 cell M{XSfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlKwTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4hdGW3a3XtbYEhUzV4MjDj[YxtKGyrbnXzMEBKSzVyPUKyMlEhdk1? Mki5NVU3PTh6N{m=
HT-29 cell M2\R[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVjJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBkd2yxcnXjeIFtKGOjcnPpco9u[SCKVD2yPUBk\WyuIHzpcoV{NCCLQ{WwQVI1NjVibl2= NELXZnkyPTZ3OEi3PS=>
HCT116 cells NF33Z2ZRem:uaX\ldoF1cW:wIHHzd4F6 NEDlVotCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCudX3pcoV{[2WwY3WgZZN{[XluIFXDOVA:OC5yMzFOwG0> M2ThN|IyPjB3OUe1
NCI-H1975 cells NVLQVndsWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXTkV5RjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNuIFnDOVA:OzZibl2= NW\Rb4F2OjF5MUWxOlU>
human DLD1 cells MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHjVR3VIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBFVERzIHPlcIx{NCCJSUWwQVM4KG6P NVfvOnRvOTh{NEO3NFM>
human A431 cells NV;wfWNCS3m2b4TvfIlkyqCjc4PhfS=> M1j5UlczKGh? MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NECgcm0> MmLSNlUzPzdyNke=
human HepG2 cells M2m4d2N6fG:2b4jpZ:Kh[XO|YYm= MlzFO|IhcA>? MnvZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20NEBvVQ>? NF7KWYQzPTJ5N{C2Oy=>
human BGC823 cells M3fibWN6fG:2b4jpZ:Kh[XO|YYm= NIfQboY4OiCq NEmxO5BEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDT0N6MkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF01OCCwTR?= Mli3NlUzPzdyNke=
human SKBR3 cells NGn5bGJEgXSxdH;4bYPDqGG|c3H5 MWW3NkBp NUTwdXBQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uEUkOgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KGOnbHz0bZRmei2pbH:gZZN{[XluIFnDOVA:PDFibl2= MUexPVQxPTV{OB?=
human MDA-MB-231 cells NIWwVFREgXSxdH;4bYPDqGG|c3H5 MoriO|IhcA>? MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PTBibl2= NXHTS4FVOjV{N{ewOlc>
human A549 cells MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXnqSZdxT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxteyxiR1m1NF03PCCwTR?= NYrvUI5GOTh{NEO3NFM>
Sf9 cells NH:5dJlHfW6ldHnvckBie3OjeR?= NF\1W2RFcXOybHHj[Y1mdnRib3[gS20uSk:GSWDZJIZzd21iaIXtZY4h\nWubDDs[Y5ofGhiSGPQPVAh[WyyaHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|LXnu[oVkfGWmIGPmPUBk\WyuczDh[pRmeiBzNjDodpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3ME23OEBvVQ>? MXyyOFc2OTR2MR?=
human U87MG cells NW\zTYIzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV6N13HJINmdGy|LDDJR|UxRTh7IH7N MUmyNVcyPTF4NR?=
human A549 cells MYPDfZRwfG:6aXRCpIF{e2G7 MUS3NkBp NUPlSnV[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVk4KG6P Mn7ONlUzPzdyNke=
mouse P19 cells NV;EWHZYS3m2b4TvfIlkyqCjc4PhfS=> NGDnUm8yQCCq MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDQNVkh[2WubIOgZYZ1\XJiMUigbJJ{NCCLQ{WwQVAvOSEQvF2= MkPzNVc1PDJ3NkW=
human HL7702 cells NYrBTZRXS3m2b4TvfIlkyqCjc4PhfS=> MoLSO|IhcA>? MofIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw4PzB{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4yPDFizszN M1vsPVI2Ojd5ME[3
human A549 cells Mlf2R5l1d3SxeHnjxsBie3OjeR?= NXPsNlNMOiCmYYnz M2PNTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgNkBl[Xm|IHL5JGFt[W2jclLseYUh[XO|YYmsJGlEPTB;MD6xOUDPxE1? NYnPcXlYOjN7NEe3PVQ>
human A431 cells NH3ET3hRem:uaX\ldoF1cW:wIHHzd4F6 MnTUO|IhcA>? NIfITmRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0N|Eh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVAvOiEQvF2= MYSyNFY2PTJ|Nx?=
human HepG2 cells MUPDfZRwfG:6aXRCpIF{e2G7 M33SNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkOg{txO Mm\lNlM3PTZ3NU[=
human SW480 cells NHz0TVNEgXSxdH;4bYPDqGG|c3H5 M3LTRlczKGh? MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTW|Q5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuN|Eh|ryP MkfNNlUzPzdyNke=
human LNCAP cells MWDDfZRwfG:6aXRCpIF{e2G7 MkDjO|IhcA>? M{e1emN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxPS0GSIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE41OyEQvF2= M{fqSlI2OTB3OUK0
human LS174T cells NXTNWFBzS3m2b4TvfIlkyqCjc4PhfS=> M4fkcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxUOTd2VDDj[YxteyCkeTDNWHMh[XO|YYmsJGlEPTB;MD60OUDPxE1? MVKxO|A{PDF|NR?=
human HeLa cells NF2yUmZEgXSxdH;4bYPDqGG|c3H5 MlvTO|IhcA>? M4fK[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlc6QCEQvF2= NXL2UIY{OjV{N{ewOlc>
rat L6 cells NEi0O4pEgXSxdH;4bYPDqGG|c3H5 NFLXPHU4OiCq MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBz[XRiTE[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEGuYX3hdkBDdHWnIHHzd4F6NCCLQ{WwQVUh|ryP M4K1bVI1PThyNUOx
human MCF7 cells MWLDfZRwfG:6aXRCpIF{e2G7 M2LQ[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[nliU2LCJIF{e2G7LDDJR|UxRTlwNjFOwG0> MnOxNVk2PjB|NUO=
human MCF7 cells Mn[5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXzHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IHThfZMh[nliU2LCJIF{e2G7LDDHTVUxRTN3Lk[g{txO M2D5bVE4QDZ7MEm4
HEK293T cells NEK3d2lHfW6ldHnvckBie3OjeR?= MmjRTY5pcWKrdHnvckBw\iCWTl[tZYxxcGFvaX7keYNm\CCQRj3rZZBx[UJiYXP0bZZifGmxbjDlfJBz\XO|ZXSgbY4hUEWNMkmzWEBk\WyuczDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? MV[xPFQxQDdzMx?=
human Jurkat cells NEjVTlBHfW6ldHnvckBie3OjeR?= MmraTY5pcWKrdHnvckBw\iCWTl[tZYxxcGFvaX7keYNm\CCQRj3rZZBx[UJiYXP0bZZifGmxbjDlfJBz\XO|ZXSgbY4hTkGGRDDk[YZq[2mnboSgbJVu[W5iSoXyb4F1KGOnbHzzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= MmrqNVg1ODh5MUO=
human SKBR3 cells MnPJSpVv[3Srb36gZZN{[Xl? M1jFUFI1KGh? MUfJcohq[mm2aX;uJI9nKEi|cEmwMY1m\GmjdHXkJGhGWjJiZHXndoFl[XSrb36gbY4hcHWvYX6gV2tDWjNiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfA>? NX7XV2FlOTh6MU[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
in solvent
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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