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KU-32

Names

[ CAS No. ]:
956498-70-7

[ Name ]:
KU-32

[Synonym ]:
ku 32

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> HSP
Signaling Pathways >> Metabolic Enzyme/Protease >> HSP
Research Areas >> Cardiovascular Disease
Research Areas >> Metabolic Disease
Research Areas >> Neurological Disease

[Target]

Hsp90[1]


[In Vitro]

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].

[In Vivo]

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].

[Cell Assay]

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 admin]

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.


[Related Small Molecules]

17-AAG | Ganetespib(STA-9090) | NVP-AUY922 | Geldanamycin | VER-155008 | AT13387 | 17-DMAG (Alvespimycin) HCl | BIIB021 | Apoptozole | IPI-504 | KNK437 | Teprenone | KRIBB11 | Debio-0932 | HSP-990

Chemical & Physical Properties

[ Density]:
1.37±0.1 g/cm3 (20 °C, 760 mmHg)

[ Boiling Point ]:
668.1±55.0 °C (760 mmHg)

[ Molecular Formula ]:
C20H25NO8

[ Molecular Weight ]:
407.41400

[ Exact Mass ]:
407.15800

[ PSA ]:
127.46000

[ LogP ]:
1.38330

Related Compounds