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General description
A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM142-161 for Mcl-1, but not Bcl-xL, binding (IC50 = 310 nM vs >40 µM; [Mcl-1] & [Bcl-xL] = 6.25 nM), displaying little inhibitory potency toward CYP450 isoforms 1A2/2D6/3A4/2C9 (IC50 = >10 µM). Antiproliferation potencies against 2 murine lymphoma cell lines (GI50 = 300 nM/ MCl1-1780 & 1.1 µM/Bcl2-1863) and 11 human cancer lines of various origins (GI50 from 1.6 to 25 µM) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment. Stability studies using murine and human liver microsome preparations reveal t1/2 values of 40 min and 55 min, respectively.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Mcl-1
Reversible: yes
Packaging
Packaged under inert gas
Other Notes
Richard, D.J., et al. 2013. Bioorg. Med. Chem.21, 6642.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥95% (HPLC) |
| Quality Segment | 100 |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white |
| solubility | DMSO: 25 mg/mL |
| web metadata keyword.default | 7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol chemical,7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol,Mcl-1 BH3-binding groove inhibitor,Mcl-1 Inhibitor II 315698-17-0,Mcl-1 Inhibitor II IC50 310 nM,Mcl-1 Inhibitor II for cellular assays,Mcl-1 Inhibitor II for drug discovery applications,Mcl-1 Inhibitor II for laboratory use,Mcl-1 Inhibitor II lab-grade product,Mcl-1 selective inhibitor 1.1 µM,Myeloid Cell Leukemia-1 Inhibitor II Mcl-1 inhibitor,Sigma-Aldrich Mcl-1 Inhibitor II for cancer research,antiproliferative Mcl-1 Inhibitor II for lymphoma cell lines,high purity Myeloid Cell Leukemia-1 Inhibitor II |
| storage temp. | 2-8°C |
| SMILES string | FC(F)(F)c1ccc(cc1)C(N4CCN(CC4)CC)c2c(c3ncccc3cc2)O |
| InChI key | NGAPBLRRJSKIRT-UHFFFAOYSA-N |
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¥ 805.47
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¥ 1376.90
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¥ 3593.05
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¥ 8152.33
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