(-)-DHMEQ

小分子

(-)-脱氢表雄酮

(-)-DHMEQ

D648298-5mg

5mg

≥98%

-20°C储存,充氩

超低温冰袋运输

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity In Vitro (-)-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 AnalysisCell 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 AnalysisCell 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. In Vivo (-)-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cellsDosage: 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. Form:Solid IC50& Target:RelA RelB

(-)-DHMEQ（Dehydroxymethylepoxyquinomicin）是一种与半胱氨酸残基共价结合的强效、选择性和不可逆的 NF-κB 抑制剂。(-)-DHMEQ 可抑制 NF-κB 的核转位，并具有抗炎和抗癌活性。

287194-40-5

C13H11NO5

261.23 g/mol

9881652

C1=CC=C(C(=C1)C(=O)NC2=CC(=O)[C@@H]3[C@H]([C@H]2O)O3)O

C1=CC=C(C(=C1)C(=O)NC2=CC(=O)[C@@H]3[C@H]([C@H]2O)O3)O

9881652

DMSO : 50 mg/mL (191.40 mM; Need ultrasonic)

3

5

2

261.064 Da

261.064 Da

99.200 Ų

19

0

446.000

0

1

0.000