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 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.

For research use only. We do not sell to patients.

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 Related Antibodies

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mTOR mTORC1 mTORC2

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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Description

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)

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].

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

HSP90/mTOR-IN-1 Related Antibodies

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.
In Vivo

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

MedChemExpress (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.
Molecular Weight

717.21

Formula

C36H34ClFN6O5S
CAS No.
SMILES

ClC1=CC(NC(NC2=CC=C(C=C2)C3=NC(N4CCOCC4)=C5C6=C(SC5=N3)CN(CC6)C(C7=CC(C(C)C)=C(C=C7O)O)=O)=O)=CC=C1F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HSP90/mTOR-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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