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HDAC6/HSP90-IN-2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HDAC6/HSP90-IN-2图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
HDAC6/HSP90-IN-2 (compound 6e) 是HDAC6Hsp90的双抑制剂,其IC50值分别为 106 nM 和 61 nM。HDAC6/HSP90-IN-2 可用于癌症的研究。
生物活性

HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor ofHDAC6andHsp90, withIC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research ofcancer[1].

IC50& Target

HDAC6

106 nM (IC50)

HDAC1

654.5 nM (IC50)

HDAC3

1539 nM (IC50)

HDAC7

1691 nM (IC50)

体外研究
(In Vitro)

HDAC6/HSP90-IN-2 (compound 6e) (0.05-2 μM; 24 h) effects HSP90, HDAC6 and signaling pathways regulated by Hsp90 dose-dependently[1].
HDAC6/HSP90-IN-2 (compound 6e) (2 μM; 24 h) promotes the acetylation of HSP90[1].
HDAC6/HSP90-IN-2 (compound 6e) (0-100 μM; 24-72 h) inhibits the growth of H1975 non-small cell lung cancer cells[1].
HDAC6/HSP90-IN-2 (compound 6e) (0-2 μM; 24 h) induces apoptosis of H1975 cells[1].

Western Blot Analysis[1]

Cell Line:H1975 cells
Concentration:0.05, 0.1, 0.5, 1 and 2 μM
Incubation Time:24 hours
Result:Showed inhibitory effect to Hsp90 and HDACs dose-dependently and increased the expression levels of Hsp70 and Hsp90 probably by activates HSF1.

Western Blot Analysis[1]

Cell Line:H1975 cells
Concentration:2 μM
Incubation Time:24 hours
Result:Promoted the acetylation of Hsp90 by inhibiting HDAC6, and increased the acetylation at K294 residue of Hsp90.

Apoptosis Analysis[1]

Cell Line:H1975 cells
Concentration:0, 0.5, 1 and 2 μM
Incubation Time:24 hours
Result:Induced early and late apoptosis of H1975 cells dose-dependently.

Cell Viability Assay[1]

Cell Line:H1975 cells
Concentration:0-100 μM
Incubation Time:24, 48 and 72 h
Result:Inhibited the growth of H1975 non-small cell lung cancer cells with a GI50value of 1.7 μM.
体内研究
(In Vivo)

HDAC6/HSP90-IN-2 (25-50 mg/kg; i.p. every weekdays for 6 weeks) exhibits antitumor activity of in NOD-scid IL2Rgammanull (NSG) mice with xenotransplantation of H1975 cells[1].

Animal Model:NOD-scid IL2Rgammanull (NSG) mouse with H1975 cells xenograft[1]
Dosage:25-50 mg/kg
Administration:Intraperitoneal injection; 25-50 mg/kg for every weekdays; for 6 weeks
Result:Delayed tumor growth after 2 weeks and reduced the growth rates of tumors in mice.
分子量

358.39

Formula

C19H22N2O5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.