2-Methoxystypandrone | CAS:85122-21-0 | Manufacturer ChemFaces

2-Methoxystypandrone

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Description:

2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitantly promotes neurodevelopmental protein expression and endogenous neurogenesis through inactivation of GSK3β to enhance β-catenin signaling for upexpression of neuroprotective genes and proteins.2-Methoxystypandrone has anti-osteoclastogenic effect, could reflect the block of RANKL-induced association of TRAF6-TAK1 complexes with consequent decrease of IkappaB-mediated NF-kappaB and mitogen-activated protein kinases-mediated c-Fos activation pathways and suppression of NFATc1 and other gene expression, essential for bone resorption.

Targets:

JAK | IkB | NF-kB | TNF-α | STAT | NOS | COX | p65 | GSK-3 | Bcl-2/Bax | Wnt/β-catenin | MMP(e.g.TIMP) | IKK

In vivo:

Biochem Pharmacol. 2014 Feb 1;87(3):502-14.

2-Methoxystypandrone ameliorates brain function through preserving BBB integrity and promoting neurogenesis in mice with acute ischemic stroke.[Pubmed: 24342702 ]

2-Methoxystypandrone (2-MS), a naphthoquinone, has been shown to display an immunomodulatory effect in a cellular model.
METHODS AND RESULTS:
To explore whether 2-Methoxystypandrone could protect mice against cerebral ischemic/reperfusion (I/R)-induced brain injury, we evaluated 2-Methoxystypandrone's protective effects on an acute ischemic stroke by inducing a middle cerebral artery occlusion/reperfusion (MCAO) injury in murine model. Treatment of mice that have undergone I/R injury with 2-Methoxystypandrone (10-100 μg/kg, i.v.) at 2 h after MCAO enhanced survival rate and ameliorated neurological deficits, brain infarction, neural dysfunction and massive oxidative stress, due to an enormous production of free radicals and breakdown of blood-brain barrier (BBB) by I/R injury; this primarily occurred with extensive infiltration of CD11b-positive inflammatory cells and upexpression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 and p65 nuclear factor-kappa B (NF-κB). All of these pathological changes were diminished by 2-Methoxystypandrone; 2-Methoxystypandrone also intensively limited cortical infarction and promoted upexpression of neurodevelopmental genes near peri-infarct cortex and endogenous neurogenesis near subgranular zone of hippocampal dentate gyrus and the subventricular zone, most possibly by inactivation of GSK3β which in turn upregulating β-catenin, Bcl-2 adam11 and adamts20.
CONCLUSIONS:
We conclude that 2-Methoxystypandrone blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity; 2-Methoxystypandrone also concomitantly promotes neurodevelopmental protein expression and endogenous neurogenesis through inactivation of GSK3β to enhance β-catenin signaling for upexpression of neuroprotective genes and proteins.

2-Methoxystypandrone Description

Source:	The roots of Polygonum cuspidatum
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Kinase Assay:

Cancer Sci. 2014 Apr;105(4):473-80.

2-Methoxystypandrone inhibits signal transducer and activator of transcription 3 and nuclear factor-κB signaling by inhibiting Janus kinase 2 and IκB kinase.[Pubmed: 24450414]

Constitutive activation of the signal transducer and activator of transcription 3 (STAT3) or the nuclear factor-κB (NF-κB) pathway occurs frequently in cancer cells and contributes to oncogenesis. The activation of Janus kinase 2 (JAK2) and IκB kinase (IKK) are key events in STAT3 and NF-κB signaling, respectively.
METHODS AND RESULTS:
We have identified 2-Methoxystypandrone (2-MS) from a traditional Chinese medicinal herb Polygonum cuspidatum as a novel dual inhibitor of JAK2 and IKK. 2-MS inhibits both interleukin-6-induced and constitutively-activated STAT3, as well as tumor necrosis factor-α-induced NF-κB activation. 2-MS specifically inhibits JAK and IKKβ kinase activities but has little effect on activities of other kinases tested. The inhibitory effects of 2-MS on STAT3 and NF-κB signaling can be eliminated by DTT or glutathione and can last for 4 h after a pulse treatment. Furthermore, 2-MS inhibits growth and induces death of tumor cells, particularly those with constitutively-activated STAT3 or NF-κB signaling.
CONCLUSIONS:
We propose that the natural compound 2-MS, as a potent dual inhibitor of STAT3 and NF-κB pathways, is a promising anticancer drug candidate.

Br J Pharmacol. 2010 Sep;161(2):321-35.

2-Methoxystypandrone represses RANKL-mediated osteoclastogenesis by down-regulating formation of TRAF6-TAK1 signalling complexes.[Pubmed: 20735418]

2-Methoxystypandrone (2-MS) is a naphthoquinone isolated from Polygonum cuspidatum, a Chinese herb used to treat bone diseases. Here we have determined whether 2-Methoxystypandrone antagonised osteoclast development and bone resorption.
METHODS AND RESULTS:
The number of multinuclear osteoclasts, actin rings and resorption pit formation were markedly inhibited by 2-Methoxystypandrone , targeting osteoclast differentiation at an early stage and without significant cytotoxicity. The anti-resorption effect of 2-Methoxystypandrone was accompanied by decreasing dendritic cell-specific transmembrane protein and matrix metalloproteinase-9 (MMP-9) mRNA expression. RANKL-increased MMP-9 gelatinolytic activity was also attenuated by concurrent, but not by subsequent addition of 2-Methoxystypandrone . 2-Methoxystypandrone markedly inhibited not only the RANKL-triggered nuclear translocations of NF-kappaB, c-Fos and nuclear factor of activated T cells c1 (NFATc1), but also the subsequent NFATc1 induction.Important for osteoclastogenesis and formation of such signalling complexes was prevented by 2-Methoxystypandrone.
CONCLUSIONS:
The anti-osteoclastogenic effects of 2-Methoxystypandrone could reflect the block of RANKL-induced association of TRAF6-TAK1 complexes with consequent decrease of IkappaB-mediated NF-kappaB and mitogen-activated protein kinases-mediated c-Fos activation pathways and suppression of NFATc1 and other gene expression, essential for bone resorption.

Structure Identification:

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3143-6.

Discovery, total synthesis, HRV 3C-protease inhibitory activity, and structure-activity relationships of 2-methoxystypandrone and its analogues.[Pubmed: 11720861]

METHODS AND RESULTS:
2-Methoxystypandrone, a naphthoquinone, was isolated from a Chinese herb Polygonum cuspidatum by bioassay guided fractionation using HRV 3C-protease assay. It showed an IC(50) value of 4.6 microM and is moderately selective. A new 10-step, total synthesis of 2-Methoxystypandrone was accomplished in 45% overall yield using a Diels-Alder approach.
CONCLUSIONS:
Several analogues of this compound were prepared. Isolation, synthesis and HRV 3C-protease structure-activity relationships of these compounds have been described.

Product Name	2-Methoxystypandrone
Price:	$318 / 5mg
CAS No.:	85122-21-0
Catalog No.:	CFN97412
Molecular Formula:	C₁₄H₁₂O₅
Molecular Weight:	260.2 g/mol
Purity:	>=98%
Type of Compound:	Quinones
Physical Desc.:	Red powder
Source:	The roots of Polygonum cuspidatum
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS SDF
Similar structural:	Comparison (Web) (SDF)
Guestbook:

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	3.8432 mL	19.216 mL	38.432 mL	76.864 mL	96.0799 mL
5 mM	0.7686 mL	3.8432 mL	7.6864 mL	15.3728 mL	19.216 mL
10 mM	0.3843 mL	1.9216 mL	3.8432 mL	7.6864 mL	9.608 mL
50 mM	0.0769 mL	0.3843 mL	0.7686 mL	1.5373 mL	1.9216 mL
100 mM	0.0384 mL	0.1922 mL	0.3843 mL	0.7686 mL	0.9608 mL

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CFN95269	2-Methoxy-1,4-naphthoquinone	2348-82-5	188.2	C₁₁H₈O₃
CFN90444	Plumbagin	481-42-5	188.17	C₁₁H₈O₃
CFN95676	Chimaphilin	482-70-2	186.2	C₁₂H₁₀O₂
CFN95672	7-(Hydroxymethyl)-2-methyl-1,4-naphthalenedione	145626-36-4	202.2	C₁₂H₁₀O₃
CFN95706	New compound 33	N/A	364.4	C₁₈H₂₀O₈
CFN91989	Droserone	478-40-0	204.18	C₁₁H₈O₄
CFN93018	Aristolindiquinone	86533-36-0	218.20	C₁₂H₁₀O₄
CFN97412	2-Methoxystypandrone	85122-21-0	260.2	C₁₄H₁₂O₅