Geldanamycin

製品コードS2713 別名:NSC 122750

Geldanamycin化学構造

分子量(MW):560.64

Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.

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(3)

  • 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.

  • RT-qPCR analysis of eNOS mRNA and representative Western blot images of eNOS expression, respectively, in irradiated BAECs pretreated of geldanamycin (GA; 500 nM). At 12 h after 10 Gy irradiation, BAECs were harvested. The results suggest that both HSP90 is involved in the upregulation of eNOS in irradiated BAECs.

    Radiat Res, 2018, 189(5):519-528. 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 is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
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 NYDFPG1qWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYfRfVR7S2:vcH;1coQhf2G|IHX2ZYx2[XSnZDDmc5Ih[W62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDveoFzcWGwIHPhdoNqdm:vYTDj[YxtKGyrbnWgRVI4QDBuIFnDOVA:Oy52IN88US=> NFK3PIUyOTVzNEG0OS=>
SW620 cell MlzIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUHJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCqdX3hckBkd2yxcnXjeIFtKGOjcnPpco9u[SCVV{[yNEBk\WyuIHzpcoV{NCCLQ{WwQVYvOiCwTR?= NH;lNmIyPTZ3OEi3PS=>
MCF-7 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2fCfGlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKGK{ZXHzeEBk[W6lZYKgUWNHNTdiY3XscEBtcW6nczygTWM2OD14LkWgcm0> MlexNVU3PTh6N{m=
SKBR3 cells MXjQdo9tcW[ncnH0bY9vKGG|c3H5 MmfoO|IhcA>? NF7JWYNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIV{fHKxZ3XuJJJm[2WydH;yJIRm\mmlaXXueEBpfW2jbjDTT2JTOyClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:QC53IH7N Mn74NlM3PDhzOEC=
MCF7 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 NXvjRpJsPzJiaB?= NYPSWJh2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIV5eHKnc4Ppcoch\XO2cn;n[Y4hemWlZYD0c5Ih[W[2ZYKgO|IhcHK|LDDJR|UxRTlwODDuUS=> M3S0VFI{PjR6MUiw
MDA-kb2 cells NW\2T|JYTnWwY4Tpc44h[XO|YYm= NVu3RYFvOThiaB?= M2i3[2lvcGmkaYTpc44hd2ZiSGPQPVAhcW5iaIXtZY4hVUSDLXviNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iZ3z1Z49kd3K2aXPvbYQhemWlZYD0c5Iu\GWyZX7k[Y51KGy3Y3nm[ZJie2ViZYjwdoV{e2mxbjDh[pRmeiBzODDodpMh[nliZnny[YZtgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;MUCgcm0> MknmNlQ6QDR7M{[=
human SK-BR-3 cells MmPlVJJwdGmoZYLheIlwdiCjc4PhfS=> MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLVLSMVMh[2WubIOsJGlEPTB;MUWuPEBvVQ>? MYOxPVg6Pjh2OB?=
HUVEC cells NXTv[ZJSS3m2b4TvfIlkyqCjc4PhfS=> NV\re3JFPzJiaB?= MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBJXV[HQzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE6KG6P NVPZWmpCOjV{N{ewOlc>
human HCT116 cells NYCyTnhET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvDS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{NCCJSUWwQVIyKG6P M{n3WVE5OjR|N{Cz
K562 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4m4V2lvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKGyndXvlcYliKEt3NkKgZ4VtdCCuaX7ld{whUUN3ME2yNk4yKG6P NG\MTnEyPTZ3OEi3PS=>
HT-29 cell MnW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIL0OWtKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDoeY1idiClb3zvdoVkfGGuIHPhdoNqdm:vYTDIWE0zQSClZXzsJIxqdmW|LDDJR|UxRTJ2LkWgcm0> MVyxOVY2QDh5OR?=
HCT116 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBtfW2rbnXzZ4Vv[2ViYYPzZZktKEWFNUC9NE4xOyEQvF2= Ml64NlE3ODV7N{W=
NCI-H1975 cells NGjwN3FRem:uaX\ldoF1cW:wIHHzd4F6 MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INVk4PSClZXzsd{whUUN3ME2zOkBvVQ>? M2D6eVIyPzF3MU[1
human DLD1 cells MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH;zV5RIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBFVERzIHPlcIx{NCCJSUWwQVM4KG6P NI[xR28yQDJ2M{ewNy=>
human A431 cells M3vmRmN6fG:2b4jpZ:Kh[XO|YYm= NIfhTJE4OiCq NID6Rm5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFAhdk1? MnO0NlUzPzdyNke=
human HepG2 cells M2LDdGN6fG:2b4jpZ:Kh[XO|YYm= M3:zfVczKGh? M4rvfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OFAhdk1? NXzTbpdbOjV{N{ewOlc>
human BGC823 cells NIrYUHFEgXSxdH;4bYPDqGG|c3H5 MUK3NkBp M3\4NWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJISzh{MzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVQxKG6P M3fsOlI2Ojd5ME[3
human SKBR3 cells NHG4N3hEgXSxdH;4bYPDqGG|c3H5 MVS3NkBp NH;jeWdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0KUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubzDhd5NigSxiSVO1NF01OSCwTR?= M1jyeVE6PDB3NUK4
human MDA-MB-231 cells MofnR5l1d3SxeHnjxsBie3OjeR?= MXm3NkBp M4n3PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13MDDuUS=> MnfuNlUzPzdyNke=
human A549 cells MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1raPWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGE2PDliY3XscJMtKEeLNUC9OlQhdk1? NXzuOZZLOTh{NEO3NFM>
Sf9 cells Mo\6SpVv[3Srb36gZZN{[Xl? NIXmXWpFcXOybHHj[Y1mdnRib3[gS20uSk:GSWDZJIZzd21iaIXtZY4h\nWubDDs[Y5ofGhiSGPQPVAh[WyyaHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|LXnu[oVkfGWmIGPmPUBk\WyuczDh[pRmeiBzNjDodpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3ME23OEBvVQ>? NWfie|Q6OjR5NUG0OFE>
human U87MG cells M3nHUXBzd2yrZnXyZZRqd25iYYPzZZk> MmLSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXOEfNS{Bk\WyuczygTWM2OD16OTDuUS=> MViyNVcyPTF4NR?=
human A549 cells Mn3NR5l1d3SxeHnjxsBie3OjeR?= NGO3fWw4OiCq MlTXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUm3JI5O MnLENlUzPzdyNke=
mouse P19 cells MVPDfZRwfG:6aXRCpIF{e2G7 NEHvcZkyQCCq Mn3wR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgVFE6KGOnbHzzJIFnfGW{IEG4JIhzeyxiSVO1NF0xNjFizszN M{naflE4PDR{NU[1
human HL7702 cells NXSwVGp5S3m2b4TvfIlkyqCjc4PhfS=> MXG3NkBp MoO3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw4PzB{IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4yPDFizszN NEf0S3QzPTJ5N{C2Oy=>
human A549 cells MU\DfZRwfG:6aXRCpIF{e2G7 MYeyJIRigXN? Mn3IR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjCyJIRigXNiYomgRYxidWG{Qnz1[UBie3OjeTygTWM2OD1yLkG1JO69VQ>? NXLa[pEzOjN7NEe3PVQ>
human A431 cells NV7i[2lpWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1\XbVczKGh? NWT5fnJySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFMyKGOnbHzzJIFnfGW{IEeyJIhzeyxiSVO1NF0xNjJizszN NGCyN4szODZ3NUKzOy=>
human HepG2 cells MYDDfZRwfG:6aXRCpIF{e2G7 Mmm3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMzFOwG0> MmXVNlM3PTZ3NU[=
human SW480 cells MnjCR5l1d3SxeHnjxsBie3OjeR?= NULZcZYyPzJiaB?= MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTW|Q5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuN|Eh|ryP NEXES2szPTJ5N{C2Oy=>
human LNCAP cells M{e5bGN6fG:2b4jpZ:Kh[XO|YYm= NXfQWplJPzJiaB?= Mlz1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5ESVBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlQ{KM7:TR?= NFjGWIgzPTFyNUmyOC=>
human LS174T cells MXnDfZRwfG:6aXRCpIF{e2G7 NEjjNIxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNWzF5NGSgZ4VtdHNiYomgUXRUKGG|c3H5MEBKSzVyPUCuOFUh|ryP MYexO|A{PDF|NR?=
human HeLa cells MW\DfZRwfG:6aXRCpIF{e2G7 NF7KOVE4OiCq MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD63PVgh|ryP MXiyOVI4PzB4Nx?=
rat L6 cells MmHHR5l1d3SxeHnjxsBie3OjeR?= NEDHTnc4OiCq M4PEdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHKjdDDMOkBk\WyuczDh[pRmeiB5MjDodpMh[nliQXzhcYFzKEKudXWgZZN{[XluIFnDOVA:PSEQvF2= MXyyOFU5ODV|MR?=
human MCF7 cells M3zwfmN6fG:2b4jpZ:Kh[XO|YYm= MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiSVO1NF06NjZizszN MlzJNVk2PjB|NUO=
human MCF7 cells NY\tWndXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{DoZmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKg[IF6eyCkeTDTVmIh[XO|YYmsJGdKPTB;M{WuOkDPxE1? Ml;JNVc5PjlyOUi=
HEK293T cells M3TyWGZ2dmO2aX;uJIF{e2G7 M1PFRWlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiTl[tb4FxeGGEIHHjeIl3[XSrb36g[ZhxemW|c3XkJIlvKEiHS{K5N3Qh[2WubIOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 NHXXNIIyQDRyOEexNy=>
human Jurkat cells NYe4eYdsTnWwY4Tpc44h[XO|YYm= NHvnWWdKdmirYnn0bY9vKG:oIGTOSk1idHCqYT3pcoR2[2WmIF7GMYtieHCjQjDhZ5RqfmG2aX;uJIV5eHKnc4Pl[EBqdiCIQVTEJIRm\mmlaXXueEBpfW2jbjDKeZJs[XRiY3XscJMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NIjQe3oyQDRyOEexNy=>
human SKBR3 cells NYrMOXA{TnWwY4Tpc44h[XO|YYm= MYCyOEBp Mn;2TY5pcWKrdHnvckBw\iCKc4C5NE1u\WSrYYTl[EBJTVJ{IHTl[5Ji\GG2aX;uJIlvKGi3bXHuJHNMSlJ|IHPlcIx{KGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3R? NYPOXFRiOTh6MU[xNVE>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程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

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

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

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