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Dynarrestin

Cat. No. M14924
Dynarrestin Structure
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Biological Activity

Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells.

<span style='color:#ff0000;'><strong>*The compound is unstable in solutions, freshly prepared is recommended</strong></span>


Chemical Information
Molecular Weight 431.5
CAS Number 2222768-84-3
Solubility (25°C) DMSO 83.33 mg/mL
Storage 2-8°C, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kumiko Hayashi, et al. Effects of dynein inhibitor on the number of motor proteins transporting synaptic cargos

[2] Eric Dietel, et al. Crosstalks of the PTPIP51 interactome revealed in Her2 amplified breast cancer cells by the novel small molecule LDC3/Dynarrestin

[3] Susanne Hing, et al. Dynarrestin, a Novel Inhibitor of Cytoplasmic Dynein

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