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

GEM-5 是一种基于吉西他滨、含有一个 HIF-1α 抑制剂 (YC-1) 的偶联物 (IC50 = 30 nM)。GEM-5 能显著下调 HIF-1α 的表达，上调肿瘤抑制因子 p53 的表达。GEM-5 诱导 A2780 细胞凋亡 (apoptosis)，抑制肿瘤生长。

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GEM-5 Chemical Structure

GEM-5 Chemical Structure

CAS No. : 2233543-49-0

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GEM-5 相关抗体

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查看 HIF/HIF Prolyl-Hydroxylase 亚型特异性产品:

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
细胞效力
(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]
体外研究
(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].

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

GEM-5 相关抗体:

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
体内研究
(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].

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.
分子量

649.60

Formula

C32H29F2N5O8
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

GEM-5 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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