(-)-DHMEQ (C007B-348441)

(-)-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 activityIn 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:SolidIC50& Target:RelA RelB. Specification: 0.98 Molecular Formula: C13H11NO5 Molecular Weight: 261.23 PubChem CID: 9881652 Isomeric SMILES: C1=CC=C(C(=C1)C(=O)NC2=CC(=O)[C@@H]3[C@H]([C@H]2O)O3)O

UPC:

51112704

Condition:

New

Weight:

1.06 Ounces

HazmatClass:

No;ManufacturerName=Aladdin Scientific"

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

D648298-10mg

CAS:

287194-40-5

Product Size:

10mg

Controlled Substances and Cyanide:

Yes