2. PI3K/Akt/mTOR Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis Autophagy
  3. mTOR HSP Apoptosis Autophagy
  4. HSP90/mTOR-IN-1

HSP90/mTOR-IN-1 是一种有效的 Hsp90 和 mTOR 抑制剂，IC50 分别为 69 nM 和 29 nM。HSP90/mTOR-IN-1 通过过度激活PI3K/AKT/mTOR 通路抑制 SW780 细胞增殖。HSP90/mTOR-IN-1 通过对 HSP90 和 mTOR 的选择性抑制来诱导细胞凋亡 (apoptosis) 和细胞自噬 (autophagy)。HSP90/mTOR-IN-1 在异种移植小鼠体内也表现出良好的抗肿瘤活性。HSP90/mTOR-IN-1 可用于膀胱癌的研究。

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HSP90/mTOR-IN-1 Chemical Structure

HSP90/mTOR-IN-1 Chemical Structure

CAS No. : 3033543-67-5

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HSP90/mTOR-IN-1 相关抗体

Top Publications Citing Use of Products

查看 mTOR 亚型特异性产品:

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mTOR mTORC1 mTORC2

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC50 values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the PI3K/AKT/mTOR pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer[1].

IC50 & Target[1]

mTOR

29 nM (IC50)

HSP90

69 nM (IC50)

体外研究
(In Vitro)

HSP90/mTOR-IN-1 (compound 17o) has antiproliferative activity against J82, T24 and SW780 cells[1].
HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) induces SW870 apoptosis in a dose-dependent manner, induces the formation of autophagosome[1].
HSP90/mTOR-IN-1 (0.2 and 0.5 μM; 24 h) decreases the expression of several Hsp90 client proteins in SW870[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HSP90/mTOR-IN-1 相关抗体:

Cell Proliferation Assay[1]

Cell Line: J82, T24 and SW780[1]
Concentration: 0-1 μM
Incubation Time: 48 h
Result: Exhibited antiproliferative activity against J82, T24 and SW780 with IC50s of 0.36 ± 0.03 μM, 0.41 ± 0.06 μM, 0.16 ± 0.03 μM.

Apoptosis Analysis[1]

Cell Line: SW870
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner (total apoptotic cell percentage was 12.4% and 16.5% at 0.2 and 0.5 μM, respectively).

Cell Autophagy Assay[1]

Cell Line: SW870 (transfected with GFP-LC3)
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: Induced the formation of autophagosome.
The green fluorescent spots were observed to increase in the number and gathered.

Western Blot Analysis[1]

Cell Line: SW870
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: Significantly decreased the expression of several Hsp90 client proteins, CDK4, C-Raf and CDC2.
体内研究
(In Vivo)

HSP90/mTOR-IN-1 (30 mg/kg; PO; for 17 days) exhibits significantly superior tumor growth inhibition in J82 xenograft mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balc/c nude mice (6-8 weeks; subcutaneously injected with 1×106 cells per 100 μL of J82 cells into the mice's dorsal skin)[1]
Dosage: 30 mg/kg
Administration: PO; for 17 days
Result: Exhibited significantly superior tumor growth inhibition, and did not showed remarkable weight decline.
Inhibited bladder cancer cell proliferation, induced cell apoptosis, degraded Hsp70, as well as decreased phosphorylation levels of mTOR and increased expression of LC3-II.
分子量

717.21

Formula

C36H34ClFN6O5S
CAS 号
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.
纯度 & 产品资料
参考文献

HSP90/mTOR-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

HSP90/mTOR-IN-13033543-67-5mTORHSPApoptosisAutophagyMammalian target of RapamycinHeat shock proteinsHsp90PI3K/AKT/mTOR pathwayanti-tumorbladder cancerJ82T24SW780orally activeInhibitorinhibitorinhibit

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