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BDM-2 

Cat. No. M28768
BDM-2  Structure
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Biological Activity

BDM-2 is an IN-LEDGF allosteric inhibitor (INLAI) of HIV-1 integrase (IN refers to integrase) (IC50=47 nM) with potent anti-Retroviral (ARV) activity. BDM-2 shows IN multimerization activation effect with an AC50 value of 20 nM. BDM-2 blocks the interaction between the catalytic core domain of IN (IN-CCD) and the Integrase binding domain of LEDGF/p75 (IBD), with an IC50 value of 0.15 μM. BDM-2 exhibits highly selective and favorable cytotoxicity.

Chemical Information
Molecular Weight 394.5
Formula C25H30O4
CAS Number 1643876-33-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Sofia Segal, et al. Cell Calcium. Eliminating contraction during culture maintains global and local Ca2+ dynamics in cultured rabbit pacemaker cells

[2] Arthur Forer, et al. Protoplasma. Does 2,3-butanedione monoxime inhibit nonmuscle myosin?

[3] Y Soeno, et al. Cell Tissue Res. BDM (2,3-butanedione monoxime), an inhibitor of myosin-actin interaction, suppresses myofibrillogenesis in skeletal muscle cells in culture

[4] N Khandoudi, et al. Cardiovasc Res. Skinned cardiac fibres of diabetic rats: contractile activation and effects of 2,3-butanedione monoxime (BDM) and caffeine

[5] G Kotsanas, et al. J Mol Cell Cardiol. Intracellular Ca2+, force and activation heat in rabbit papillary muscle: effects of 2,3-butanedione monoxime

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