2. Metabolic Enzyme/Protease Apoptosis
  3. HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53
  4. GEM-5

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.

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GEM-5 Chemical Structure

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

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GEM-5 Related Antibodies

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Description

GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth[1].

IC50 & Target

IC50: 30 nM (HIF-1α) in A2780[1]
Cellular Effect
Cell Line Type Value Description References
A2780 IC50
0.03 μM
Compound: GEM-5
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
[PMID: 33992863]
A2780 IC50
0.13 μM
Compound: GEM-5
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33992863]
A549 IC50
0.37 μM
Compound: GEM-5
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33992863]
A549 IC50
3.03 μM
Compound: GEM-5
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
[PMID: 33992863]
L02 IC50
3.04 μM
Compound: GEM-5
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs in hypoxic condition by MTT assay
[PMID: 33992863]
L02 IC50
4.43 μM
Compound: GEM-5
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33992863]
MCF7 IC50
2.6 μM
Compound: GEM-5
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33992863]
In Vitro

GEM-5 (0-80 μM; 12 hours) exhibits excellent antitumor activity toward A2780 cells under hypoxic condition with IC50 of 0.03 μM[1].
GEM-5 (0.5 μM; 72 hours) rises the apoptotic population to 52.67% under normoxic condition and 80.89% in A2780 cells under hypoxic condition[1].
GEM-5 (0.5 μM; 24 hours) arrests the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia)[1].
GEM-5 (0.1 and 1 μM; 24 hours) decreases the levels of HIF-1α and increases the levels of p53 in a dose dependent manner under hypoxic condition[1].

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

GEM-5 Related Antibodies

Apoptosis Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 72 hours
Result: Rose the apoptotic population to 52.67% under normoxic condition and 80.89% under hypoxic condition.

Cell Cycle Analysis

Cell Line: A2780 cells[1]
Concentration: 0.5 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle at the S phase (63.02% under normoxia and 72.64% under hypoxia).

Western Blot Analysis

Cell Line: A2780 cells[1]
Concentration: 0.1 and 1 μM
Incubation Time: 24 hours
Result: Decreased the levels of HIF-1α and increased the levels of p53 in a dose dependent manner
In Vivo

GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].

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

Animal Model: GEM-5 (125 or 271 mg/kg; tail vein injection, once a week for 4 weeks) effectively inhibits tumor growth in the A2780 xenograft mouse model and exhibited low toxicity[1].
Dosage: 125 or 271 mg/kg
Administration: Tail vein injection, once a week for 4 weeks
Result: Effectively inhibited tumor growth in the A2780 xenograft mouse model and exhibited low toxicity.
Molecular Weight

649.60

Formula

C32H29F2N5O8
CAS No.
SMILES

NC(C=CN1[C@@H]2O[C@@H]([C@H](C2(F)F)O)COC(CCC(OCC3=CC=C(O3)C4=NN(C5=C4C=CC=C5)CC6=CC=CC=C6)=O)=O)=NC1=O
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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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GEM-5 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:

GEM-52233543-49-0GEM5GEM 5HIF/HIF Prolyl-HydroxylaseApoptosisMDM-2/p53Hypoxia-inducible factorsHIFsHIF-PHGemcitabine conjugateHIF-1αp53Tumor hypoxiaCancerA2780 cellsBALB/c nude miceInhibitorinhibitorinhibit

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