2. Metabolic Enzyme/Protease Others
  3. MetAP Drug Intermediate
  4. LAF389

LAF389, a prodrug of LAF153 (HY-183876), is a methionine aminopeptidase (MetAps) inhibitor with an IC50 of 800 nM against MetAp2, and exhibits a maximum inhibition rate of 20% against MetAp1 at 300 nM. LAF389 possesses antiproliferative, antiangiogenic and cytotoxic activities. LAF389 can be used in research related to cancers such as advanced solid tumors.

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LAF389

LAF389 Chemical Structure

CAS No. : 270902-51-7

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LAF389 Related Antibodies

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Description

LAF389, a prodrug of LAF153 (HY-183876), is a methionine aminopeptidase (MetAps) inhibitor with an IC50 of 800 nM against MetAp2, and exhibits a maximum inhibition rate of 20% against MetAp1 at 300 nM. LAF389 possesses antiproliferative, antiangiogenic and cytotoxic activities. LAF389 can be used in research related to cancers such as advanced solid tumors[1][2].

IC50 & Target[1]

MetAp2

800 nM (IC50)

MetAp1

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
13 nM
Compound: LAF389
Antiproliferative activity against human A549 cells after 96 hrs
Antiproliferative activity against human A549 cells after 96 hrs
[PMID: 28185457]
HCT-116 IC50
23 nM
Compound: LAF389
Antiproliferative activity against human HCT116 cells after 96 hrs
Antiproliferative activity against human HCT116 cells after 96 hrs
[PMID: 28185457]
MDA-MB-435 IC50
40 nM
Compound: LAF389
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability after 72 hrs by MTS assay
Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability after 72 hrs by MTS assay
[PMID: 28185457]
In Vitro

LAF389 potently inhibits monolayer proliferation of human cancer cell lines, including those unresponsive to standard cytotoxics or with drug resistance, and is more unaffected by P-glycoprotein overexpression than paclitaxel[1].
LAF389 (0.0001-10 μM; 72 h) inhibits proliferation of HUVEC (IC50 = 20 nM) and A549 human non-small cell lung carcinoma cells, with greater potency against endothelial cells and cytotoxic activity against A549 cells at micromolar concentrations[2].
LAF389 (3-300 nM; 8-48 h) induces a pH-shifted, unprocessed form of 14-3-3γ in H1299, U2OS, MDA-MB-435, and A549 cells, with detection starting at 3 nM after 24 h and accumulation over 48 h[2].
LAF389 (0.1-1000 nM; 18 h) inhibits processing of 14-3-3γ in HUVEC, inducing the unprocessed form with maximal response at 1 μM after 18 h of incubation[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LAF389 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: A549 human non-small cell lung carcinoma cells, human umbilical vein endothelial cells (HUVEC)
Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 h
Result: Potently inhibited HUVEC proliferation with an IC50 of 20 nM.
Inhibited A549 cell proliferation with roughly 10-fold lower potency.
Caused substantial cell death of A549 cells at micromolar concentrations.

Western Blot Analysis[2]

Cell Line: H1299 human small cell lung carcinoma cells, U2OS, MDA-MB-435, A549 human non-small cell lung carcinoma cells
Concentration: 3-300 nM (24 h incubation); 200 nM (8 h, 24 h, 48 h incubation)
Incubation Time: 8 h, 24 h, 48 h
Result: Shifted the isoelectric point of the 14-3-3γ isoform to a more basic pH in H1299 cells.
Caused the shifted band to be detectable after 8 h of incubation and accumulate up to 48 h.
Induced effects starting at 3 nM LAF389 at 24 h, increasing up to 300 nM.
Confirmed the shifted band as the unprocessed form of 14-3-3γ, retaining its N-terminal methionine.
Induced the same effect in U2OS, MDA-MB-435, and A549 cells.

Western Blot Analysis[2]

Cell Line: human umbilical vein endothelial cells (HUVEC)
Concentration: 0.1, 0.3, 1, 3, 10 and 30 nM (18 h incubation); 1, 10, 100 and 1000 nM (18 h incubation)
Incubation Time: 18 h
Result: Inhibited MetAp processing of 14-3-3γ, leading to detection of the unprocessed form via both isoform-specific polyclonal antibodies and the unprocessed-form-specific monoclonal antibody.
Caused maximal detection of the unprocessed form at 1 μM LAF389.
In Vivo

LAF389 exerts in vivo anti-tumor activity by inhibiting tumor cell proliferation and anti-angiogenesis, and induces transient cardiovascular effects and reversible myelosuppression in rats and dogs[1].
LAF389 (intravenous injection; repeated bolus administration; repeated cycle 3 times with a 7-day interval after 3 consecutive days of administration) exhibits significant, frequency-dependent tumor growth inhibition in a panel of human solid tumor xenograft models in immunocompromised mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

498.61

Formula

C25H42N2O8
CAS No.
SMILES

CC(C)(C)/C=C/[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC)C(N[C@H]1CC[C@H](CNC1=O)OC(C2CCCCC2)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LAF389 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LAF389270902-51-7LAF 389LAF-389MetAPDrug IntermediateMethionine AminopeptidaseDrug IintermediateMetAp1human methionine aminopeptidaseadvanced solid tumoursG0/G1 cell cycle arrestG2/M cell cycle arrestapoptosishuman small cell lung carcinomahuman non-small cell lung carcinomaMetAp2human breast cancerInhibitorinhibitorinhibit

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