287194-40-5

中文名称:

287194-40-5

中文同义词:

(-)-DHMEQ;2-羟基-N-(((1S,2S,6S)-2-羟基-5-氧代-7-氧杂双环[4.1.0]庚-3-烯-3-基)苯甲酰胺;NF-ΚB抑制剂((+)-DHMEQ)

英文名称:

DEHYDROXYMETHYLEPOXYQUINOMICIN

英文同义词:

2-hydroxy-N-[(1S,2S,6S)-2-hydroxy-5-oxo-7-oxabicyclo[4.1.0]hept-3-en-3-yl]benzaMide;Dehydroxymethylepoxyquinomicin (DHMEQ);DEHYDROXYMETHYLEPOXYQUINOMICIN;DHM2EQ;DHMEQ;Benzamide, 2-hydroxy-N-[(1S,2S,6S)-2-hydroxy-5-oxo-7-oxabicyclo[4.1.0]hept-3-en-3-yl]-;(-)-DHMEQ?(dehydroxymethylepoxyquinomicin)

CAS号:

287194-40-5

分子式:

C13H11NO5

分子量:

261.23

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

287194-40-5.mol

生物活性

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) 是一种有效，选择性且不可逆的 NF-κB 抑制剂，与半胱氨酸残基共价结合。(-)-DHMEQ 抑制 NF-κB 的核易位，并显示抗炎和抗癌活性。

靶点

RelA RelB

RelA

RelB

体外研究

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 2-10 μg/mL; 12-48 hours) treatment significantly reduces the viability of all cell lines in a dose- and time-dependent manner, whereas the effect is not significant in a control cell line K562 without constitutive NF-κB activity. (-)-DHMEQ (10 μg/mL; 0-48 hours; TL-Om1, MT-1 and K562 cells) treatment significantly increases the Annexin V-positive cells in MT-1 and TL-Om1 cell lines. (-)-DHMEQ (10 μg/mL; 4-16 hours; MT-1 cells) treatment down-regulates Bcl-xL, Bcl-2, c-myc, cyclin D1, Rb, and p53, and up-regulates proapoptotic genes such as caspase-3, -8, and-9. (-)-DHMEQ treatment increases cells in G0 /G1 phase in a time-dependent manner, demonstrating antiproliferative effects of (-)-DHMEQ. (-)-DHMEQ binds to p65, cRel, RelB, and p50, but not to p52 at specific cysteine residues. (-)-DHMEQ inhibits not only DNA-binding of RelB, but also its interaction to importin. (-)-DHMEQ also induces instability of RelB. Cell Proliferation Assay Cell Line: TL-Om1, MT-1, KK-1, ST-1 and K562 cells Concentration: 2 μg/mL, 5 μg/mL, 10 μg/mL Incubation Time: 12 hours, 24 hours, 48 hours Result: Significantly reduced the viability of all cell lines in a dose- and time-dependent manner. Apoptosis Analysis Cell Line: TL-Om1, MT-1 and K562 cells Concentration: 10 μg/mL Incubation Time: 0 hours, 24 hours, 48 hours Result: Annexin V-positive cells were significantly increased after 24 to 48 hours. Western Blot Analysis Cell Line: MT-1 cells Concentration: 10 μg/mL Incubation Time: 4 hours, 8 hours, 16 hours Result: Annexin V-positive cells were significantly increased after 24 to 48 hours.

Cell Line:

TL-Om1, MT-1, KK-1, ST-1 and K562 cells

Concentration:

2 μg/mL, 5 μg/mL, 10 μg/mL

Incubation Time:

12 hours, 24 hours, 48 hours

Result:

Significantly reduced the viability of all cell lines in a dose- and time-dependent manner.

Cell Line:

TL-Om1, MT-1 and K562 cells

Concentration:

10 μg/mL

Incubation Time:

0 hours, 24 hours, 48 hours

Result:

Annexin V-positive cells were significantly increased after 24 to 48 hours.

Cell Line:

MT-1 cells

Concentration:

10 μg/mL

Incubation Time:

4 hours, 8 hours, 16 hours

Result:

Annexin V-positive cells were significantly increased after 24 to 48 hours.

体内研究

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 4 mg/kg or 12 mg/kg; intraperitoneal injection; on day 0 and 3 times a week; for one month; SCID mice) treatment shows a significant increase in the survival rate in mice. Animal Model: Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells Dosage: 4 mg/kg or 12 mg/kg Administration: Intraperitoneal injection; on day 0 and 3 times a week; for one month Result: Showed a significant increase in the survival rate in mice.

Animal Model:

Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells

Dosage:

4 mg/kg or 12 mg/kg

Administration:

Intraperitoneal injection; on day 0 and 3 times a week; for one month

Result:

Showed a significant increase in the survival rate in mice.