Cemdomespib
Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response.
For research use only. We do not sell to patients.
- CAS No.: 1450642-92-8
- Formula: C24H30FNO6
- Molecular Weight:447.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HSP90 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
>500 μM
Compound: 3; KU-596
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Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay
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[PMID: 28844386] |
| SK-BR-3 | IC50 |
>500 μM
Compound: 3; KU-596
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Antiproliferative activity against human SKBR3 cells after 72 hrs by MTS assay
Antiproliferative activity against human SKBR3 cells after 72 hrs by MTS assay
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[PMID: 28844386] |
Cemdomespib (20 mg/kg; oral gavage once per week for 4 weeks) significantly reverses the sensory hypoalgesia in WT mice but not the Hsp70 KO mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diabetic Swiss Webster mice [1]
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Dosage:2, 10, or 20 mg/kg
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Administration:Administered after 8 weeks of diabetes via once per week intra-peritoneal injections.
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Result:Improved diabetes induced hypoalgesia and sensory neuron bioenergetic deficits in a dose-dependent manner.
Chemical Information
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CAS No. 1450642-92-8
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Molecular Weight 447.50
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Formula C24H30FNO6
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SMILES
CC(NCCC1=C(C2=CC(F)=CC=C2)C=C(C=C1)O[C@H]3[C@@H]([C@@H]([C@H](C(C)(O3)C)OC)O)O)=O
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Synonyms
KU-596
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
References
[1]. Jiacheng Ma, et al. Modulating Molecular Chaperones Improves Mitochondrial Bioenergetics and Decreases the Inflammatory Transcriptome in Diabetic Sensory Neurons. ACS Chem Neurosci. 2015 Sep 16;6(9):1637-48. [Content Brief]
[2]. Xinyue Zhang, et al. Targeting Heat Shock Protein 70 to Ameliorate c-Jun Expression and Improve Demyelinating Neuropathy. ACS Chem Neurosci. 2018 Feb 21;9(2):381-390. [Content Brief]
[3]. Zheng Zhang, et al. Synthesis and evaluation of a ring-constrained Hsp90 C-terminal inhibitor that exhibits neuroprotective activity. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2701-2704. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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