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KU-32

カタログ番号GC31118

KU-32 は、神経細胞死を防ぐことができる新規のノボビオシンベースの Hsp90 阻害剤です。

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KU-32 化学構造

Cas No.: 956498-70-7

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Sample solution is provided at 25 µL, 10mM.

Description of KU-32

KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.

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].

Diabetic BKS-db/db mice, a model for type 2 diabetes, administered KU-32 for 10 weeks do not show any significant changes in blood glucose and insulin levels, despite having greater insulin staining/beta cell in the pancreas compared to untreated BKS db/db mice[1].

[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. [2]. Urban MJ, et al. Inhibiting heat-shock protein 90 reverses sensory hypoalgesia in diabetic mice. ASN Neuro. 2010 Aug 11;2(4):e00040.

Protocol of KU-32

Cell experiment:

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].

Animal experiment:

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].

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.
[2]. Urban MJ, et al. Inhibiting heat-shock protein 90 reverses sensory hypoalgesia in diabetic mice. ASN Neuro. 2010 Aug 11;2(4):e00040.

Chemical Properties of KU-32

Cas No. 956498-70-7 SDF
Canonical 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
Formula C20H25NO8 M.Wt 407.41
溶解度 Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of KU-32

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1 mg 5 mg 10 mg
1 mM 2.4545 mL 12.2726 mL 24.5453 mL
5 mM 0.4909 mL 2.4545 mL 4.9091 mL
10 mM 0.2455 mL 1.2273 mL 2.4545 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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