2. Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  3. VEGFR Autophagy Apoptosis
  4. Coibamide A

Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts.

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Coibamide A

Coibamide A Chemical Structure

CAS No. : 1029227-48-2

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Coibamide A Related Antibodies

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Description

Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts[1][2].

IC50 & Target[2]

VEGFR2

 

Cellular Effect
Cell Line Type Value Description References
A549 GI50
5.4 1
Compound: 1
Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
[PMID: 30247036]
A549 IC50
1.4 1
Compound: 1; CbA
Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
[PMID: 35059129]
A549 GI50
22800 1
Compound: 1a
Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
[PMID: 30247036]
PANC-1 GI50
3.1 1
Compound: 1
Growth inhibition of human PANC1 cells incubated for 72 hrs by MTT assay
Growth inhibition of human PANC1 cells incubated for 72 hrs by MTT assay
[PMID: 30247036]
MDA-MB-231 GI50
> 16000 1
Compound: 1a
Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTT assay
[PMID: 30247036]
A549 IC50
1.4 1
Compound: 1; CbA
Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay
[PMID: 35059129]
MDA-MB-231 IC50
66 1
Compound: Coibamide A
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 25488840]
MDA-MB-231 GI50
5 1
Compound: 1
Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTT assay
[PMID: 30247036]
MDA-MB-231 GI50
5 1
Compound: 1
Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells incubated for 72 hrs by MTT assay
[PMID: 30247036]
A549 GI50
5.4 1
Compound: 1
Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay
[PMID: 30247036]
NCI-H292 IC50
124 1
Compound: Coibamide A
Cytotoxicity against human NCI-H292 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human NCI-H292 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 25488840]
PANC-1 GI50
3.1 1
Compound: 1
Growth inhibition of human PANC1 cells incubated for 72 hrs by MTT assay
Growth inhibition of human PANC1 cells incubated for 72 hrs by MTT assay
[PMID: 30247036]
PC-3 IC50
80 1
Compound: Coibamide A
Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 25488840]
SF-295 IC50
219 1
Compound: Coibamide A
Cytotoxicity against human SF295 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human SF295 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 25488840]
In Vitro

Coibamide A (0.3-1 nM; 3-60 hours) inhibits proliferation of MDA-MB-231 breast cancer cells[1].
Coibamide A (2.3-230 nM; 3 days) produces concentration- and time-dependent cell death in human U87-MG and SF-295 glioblastoma cells[2].
Coibamide A (10-300 nM; 72 h) induces activation of caspase-3/7 and apoptosis in a cell type-specific manner[2].
Coibamide A (20 nM; 48 h) induces autophagosome accumulation in apoptotic-resistant U87-MG cells[2].

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

Coibamide A Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 0.3, 1 nM
Incubation Time: 3-60 hours
Result: Showed a steady concentration-dependent decrease in proliferative activity relative to vehicle-treated cells

Cell Cytotoxicity Assay[2]

Cell Line: U87-MG and SF-295 cells
Concentration: 2.3 to 230 nM
Incubation Time: 3 days
Result: Induced concentration-dependent cytotoxicity with EC50 values of 28.8 nM and 96.2 nM for U87-MG and SF-295 cells, respectively.

Apoptosis Analysis[2]

Cell Line: U87-MG and SF-295 cells
Concentration: 10-300 nM
Incubation Time: 72 h
Result: An 89 kDa band corresponding to the caspase 3-cleaved form of PARP1 was readily detected by 48 h indicative of apoptotic cell death in SF-295 cells, whereas only trace levels of this fragment were observed in late, detaching U87-MG cell lysates

Cell Autophagy Assay[2]

Cell Line: U87-MG cell
Concentration: 20 nM
Incubation Time: 48 h
Result: Caused a clear increase in LC3-II expression by 1 h, and this increase in LC3-II expression was generally sustained through 48 h.
In Vivo

Coibamide A (300 μg/kg; intratumoral injections; for the first two days, and then every 48 h afterward for 35 days) inhibits tumor growth in a subcutaneous mouse model of glioblastoma[1].

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

Animal Model: 8-week old female nude athymic mice with U87-MG cells[1]
Dosage: 300 μg/kg
Administration: Intratumoral injections; for the first two days, and then every 48 h afterward for 35 days
Result: Remained stable at 200-300 mm3 without significant growth over 4 weeks of treatmen, whereas the tumors of vehicle-treated animals continued to grow at a steady rate consistent with this aggressive cancer cell type
Molecular Weight

1287.63

Formula

C65H110N10O16
CAS No.
Sequence

{NMe-Val}-{Hiv}-{NMe-Ser}-{NMe-Leu}-{NMe-Thr}-{NMe-Ser}-{NMe-Ile}-{NMe-Ala}-{NMe-Leu}-{NMe-Tyr}-{NMe-Ala} lactone bridge:Thr5-Ala11
Sequence Shortening

{NMe-Val}-{Hiv}-{NMe-Ser}-{NMe-Leu}-{NMe-Thr}-{NMe-Ser}-{NMe-Ile}-{NMe-Ala}-{NMe-Leu}-{NMe-Tyr}-{NMe-Ala} lactone bridge:Thr5-Ala11
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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Coibamide A 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:

Coibamide A1029227-48-2VEGFRAutophagyApoptosisVascular endothelial growth factor receptorN-methyl-stabilizedcytotoxicdepsipeptideantiproliferativeautophagosomemTORVEGFA/VEGFR2glioblastoma xenograftInhibitorinhibitorinhibit

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