Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph(3,4OMe)
Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) is an anti-leukemic agent with potent ribosome-targeting protein synthesis inhibition. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) downregulates short-lived oncoproteins, including c-Myc and Mcl-1, by inhibiting protein synthesis. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) induces cell cycle arrest at the G0/G1 phase and triggers mitochondrial pathway-mediated apoptosis in acute myeloid leukemia (AML) cells. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) is applicable for research on leukemia.
For research use only. We do not sell to patients.
- Formula: C32H39NO9S
- Molecular Weight:613.72
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Mcl-1 |
In Vitro
Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph(3,4OMe) (P2) (48 h) potently inhibits proliferation of U937, MOLM-13, NB4, Kasumi-1, Jurkat, K562, Raji, and JeKo-1 cells with sub-nanomolar to low nanomolar potency[1].
Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph(3,4OMe) (1-3 nM; 24-72 h) suppresses proliferation of U937 and MOLM-13 cells in a dose- and time-dependent manner[1].
Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph(3,4OMe) (1-3 nM; 24 h) induces G0/G1 phase cell cycle arrest in U937 and MOLM-13 cells in a concentration-dependent manner[1].
Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph(3,4OMe) (48 h (Annexin V/PI staining); 24 h (JC-1 staining)) induces apoptosis in U937 and MOLM-13 cells via the mitochondrial pathway, and activation of caspase-9, caspase-3, and PARP cleavage[1].
Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph(3,4OMe) (1 h (Western blot for protein turnover); 24 h (flow cytometry); 6 h (microscopy)) inhibits protein synthesis in U937, MOLM-13, and A375 cells, preferentially depleting short-lived oncoproteins (c-Myc, Mcl-1) while sparing long-lived proteins (HSP90)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U937, MOLM-13
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Concentration:1 nM, 2 nM, 3 nM
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Incubation Time:24 h, 48 h, 72 h
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Result:Significantly suppressed proliferation of U937 and MOLM-13 cells in a dose- and time-dependent manner.
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Cell Line:U937 and MOLM-13
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Concentration:1.25 nM, 2.5 nM, 5 nM (U937); 5 nM, 7.5 nM, 10 nM (MOLM-13)
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Incubation Time:48 h
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Result:Induced apoptosis in both U937 and MOLM-13 cells in a concentration-dependent manner.
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Cell Line:U937 and MOLM-13
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Concentration:1 nM, 2 nM, 3 nM
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Incubation Time:24 h
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Result:Induced significant concentration-dependent G0/G1 phase arrest in
U937 and MOLM-13 cells.
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Cell Line:U937 and MOLM-13
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Concentration:1.25 nM, 2.5 nM, 5 nM (U937); 5 nM, 7.5 nM, 10 nM (MOLM-13)
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Incubation Time:48 h
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Result:Activated caspase-9 and caspase-3, and induced PARP cleavage, collectively confirming induction of the intrinsic mitochondrial apoptotic pathway.
Chemical Information
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Molecular Weight 613.72
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Formula C32H39NO9S
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SMILES
CCOC[C@@](CSC1=CC=C(C(OC)=C1)OC)(C(O[C@@H]2C(OC)=C[C@]34CCCN3CCC5=C([C@H]24)C=C6OCOC6=C5)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)