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Mcl-1 inhibitor 16

Cat. No. M41318
Mcl-1 inhibitor 16 Structure
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Biological Activity

Mcl-1 inhibitor 16 is a mitochondrial targeting Platinum-based inhibitor of Mcl-1.

Chemical Information
Molecular Weight 637.51
Formula C25H29Cl2N3Pt
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Philipp J Heckmeier et al. J Chem Phys. MCL-1 promiscuity and the structural resilience of its binding partners

[2] Nooshin Ashofteh et al. Cell J. MiRNA-16-1 Suppresses Mcl-1 and Bcl-2 and Sensitizes Chronic Lymphocytic Leukemia Cells to BH3 Mimetic ABT-199

[3] Marius Winkler et al. Transl Oncol. Co-targeting MCL-1 and ERK1/2 kinase induces mitochondrial apoptosis in rhabdomyosarcoma cells

[4] Mohamed Elgendy et al. Cancer Cell. Combination of Hypoglycemia and Metformin Impairs Tumor Metabolic Plasticity and Growth by Modulating the PP2A-GSK3β-MCL-1 Axis

[5] Jingshan Tong et al. Cancer Res. Mcl-1 Phosphorylation without Degradation Mediates Sensitivity to HDAC Inhibitors by Liberating BH3-Only Proteins

Related Bcl-2 Products
BAD (103-127) (human)

BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL.

Bim BH3, Peptide IV

Bim BH3, Peptide IV is a 26-residue peptide from BH3-only protein Bim, which belongs to the pro-apoptotic group of the Bcl-2 family of proteins.

Bax inhibitor peptide, negative control

Bax inhibitor peptide, negative control is a inhibitor of Bax.

Bad BH3 (mouse)

Bad BH3 (mouse) is a biological active peptide.

Bid BH3 (80-99)

Bid BH3 (80-99) is a biological active peptide.

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