KU-32
KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.
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- CAS No.: 956498-70-7
- 화학식: C20H25NO8
- 분자량:407.41
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Hsp90[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | EC50 |
1.49 nM
Compound: KU32
|
Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release
Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release
|
[PMID: 19138859] |
| SK-BR-3 | EC50 |
10 nM
Compound: 2, KU-32
|
Antiproliferative activity against human SKBR3 cells
Antiproliferative activity against human SKBR3 cells
|
[PMID: 24953820] |
| SK-BR-3 | IC50 |
>900 μM
Compound: KU32
|
Antiproliferative activity against human SK-BR-3 cells
Antiproliferative activity against human SK-BR-3 cells
|
[PMID: 27563408] |
Treating human islets with KU-32 for 24 hours shows no toxicity. With a minimum of 2-day exposure, KU-32 improves cellular viability by blocking apoptosis. Functionally, isolated human islets release more glucose-stimulated insulin when preincubate in KU-32[1]. KU-32 protects against glucose-induced death of embryonic DRG (dorsal root ganglia) neurons cultured for 3 days in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 956498-70-7
-
분자량 407.41
-
화학식 C20H25NO8
-
SMILES
CC1=C(O2)C(C=C(NC(C)=O)C2=O)=CC=C1O[C@H]3[C@@H]([C@@H]([C@@H](OC)C(C)(C)O3)O)O
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
Islets are placed into 96-well plates and subjected to a 8-point dose of KU-32 in either low (5 mM) or high (17.5 mM) glucose in DMEM : F12 media and incubated overnight at 37°C and 5% CO2. Twenty-four hours later, alamarBlue is added directly to each well to achieve a final concentration of 10% alamarBlue. Readings on a microplate reader are collected 4, 24, and 48 hours later[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male and female lepr mice are used. At 10 weeks of age, animals are given once per week intraperitoneal injection of 5% Captisol or 20 mg/kg KU-32 in 5% Captisol. At termination of the study, blood from each animal is collected[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
References
[1]. Farmer K, et al. KU-32, a novel drug for diabetic neuropathy, is safe for human islets and improves in vitro insulin secretion and viability. Exp Diabetes Res. 2012;2012:671673. [Content Brief]
[2]. Urban MJ, et al. Inhibiting heat-shock protein 90 reverses sensory hypoalgesia in diabetic mice. ASN Neuro. 2010 Aug 11;2(4):e00040. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)