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Dynole 34-2 

Cat. No. M27824
Dynole 34-2  Structure
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Biological Activity

Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage. Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME).

Chemical Information
Molecular Weight 408.58
Formula C25H36N4O
CAS Number 1128165-88-7
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°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] Jennifer R Baker, et al. Methods Mol Biol. Dynole 34-2 and Acrylo-Dyn 2-30, Novel Dynamin GTPase Chemical Biology Probes

[2] Emily Wl Sun, et al. Mol Cell Endocrinol. Dynamin regulates L cell secretion in human gut

[3] Mark J Robertson, et al. Nat Protoc. Synthesis of Dynole 34-2, Dynole 2-24 and Dyngo 4a for investigating dynamin GTPase

[4] Megan Chircop, et al. Mol Cancer Ther. Inhibition of dynamin by dynole 34-2 induces cell death following cytokinesis failure in cancer cells

[5] Timothy A Hill, et al. J Med Chem. Inhibition of dynamin mediated endocytosis by the dynoles--synthesis and functional activity of a family of indoles

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Keywords: Dynole 34-2  supplier, Dynamin, inhibitors, activators


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