Madindoline A
Madindoline A is an orally active gp130 antagonist with a KD of 288 μM. Madindoline A inhibits IL-6- and IL-11-induced osteoclastogenesis, suppresses IL-6-stimulated serum amyloid A protein production, inhibits bone resorption and bone loss, and also inhibits IL-6- and IL-11-dependent cell line growth, as well as IL-6-dependent Stat3 tyrosine phosphorylation. Madindoline A is applicable for the research of hormone-dependent postmenopausal osteoporosis.
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- CAS No.: 184877-64-3
- Formule: C22H27NO4
- Masse moléculaire:369.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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IL-6 |
Stat-3 |
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Cell Line
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Type | Value | Description | References |
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| HepG2 | CC50 |
>100 μM
Compound: (+)-Madindoline A
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 26810262] |
| HepG2 | IC50 |
21 μM
Compound: (+)-Madindoline A
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Inhibition of gp130-IL6/IL-Ralpha interaction in human HepG2 cells assessed as inhibition of IL-6-induced STAT3 activation by luciferase reporter gene assay
Inhibition of gp130-IL6/IL-Ralpha interaction in human HepG2 cells assessed as inhibition of IL-6-induced STAT3 activation by luciferase reporter gene assay
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[PMID: 26810262] |
| MH60 | IC50 |
8 μM
Compound: 1
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Cytotoxicity in mouse MH60 cells assessed as inhibition of recombinant human IL-6-induced growth incubated for 72 hrs by tetrazolium method
Cytotoxicity in mouse MH60 cells assessed as inhibition of recombinant human IL-6-induced growth incubated for 72 hrs by tetrazolium method
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[PMID: 36971365] |
Madindoline A (0.5-70 μM; 72 h) acts as a competitive and selective antagonist of IL-6 responses in IL-6-dependent MH-60 cells, with a pA2 value of 4.78. It does not affect cell growth mediated by IL-2, IL-3 or TNF, nor does it influence cell growth under non-IL-6-dependent conditions[1].
Madindoline A (70 μM; 72 h) significantly inhibits IL-6-induced differentiation of M1 cells into macrophage-like cells, but does not affect basal differentiation or LIF-induced differentiation[1].
Madindoline A (100 μM; 15 min) inhibits IL-6-induced tyrosine phosphorylation of STAT3 in HepG2 cells, but does not affect LIF-induced STAT3 phosphorylation[1].
Madindoline A (30 μM; 4 days) significantly inhibits osteoclast formation induced by IL-6 and IL-11 in a co-culture system of mouse calvarial osteoblasts and bone marrow cells, but exerts no effect on osteoclast formation induced by LIF, IL-1, or 1α,25 (OH) 2D3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:IL-6-dependent MH-60 cells; IL-2-dependent CTLL-2 cells; IL-3-dependent Baf3 cells; TNF-sensitive L929 cells; IL-6-independent MH-60 cells
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Concentration:0.5, 1.75, 3.5, 7, 17.5, 35, 70 μM
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Incubation Time:72 h
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Result:Did not alter growth of IL-2-dependent CTLL-2 cells, IL-3-dependent Baf3 cells, or TNF-sensitive L929 cells, nor inhibit growth of IL-6-independent MH-60 cells.
Dose-dependently suppressed IL-6-induced cell growth of IL-6-dependent MH-60 cells and caused parallel rightward shifts of IL-6 dose-response curves.
Yielded a pA2 value of 4.78 and a slope of 0.99 via Schild plot analysis, confirming competitive antagonism.
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Cell Line:M1 cells
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Concentration:70 μM (pre-incubation with IL-6)
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Incubation Time:72 h (pre-incubation with IL-6); 24 h (bead incubation)
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Result:Significantly decreased the population of differentiated macrophage-like cells induced by IL-6.
Did not alter differentiation status relative to untreated cells when used alone.
Madindoline A (60 mg/kg; p.o.; once every other day; for 4 weeks) significantly inhibits bone resorption and bone loss in ovariectomized mice without affecting their uterine weight or serum IL-6 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C3H/HeJ (6-week-old female; acute-phase response induced by intraperitoneal injection of 1 μg rhIL-6 per mouse)[1]
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Dosage:10 mg/kg; 60 mg/kg
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Administration:p.o.; single dose
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Result:Reduced IL-6-induced serum amyloid A (SAA) levels to 34.7 ng/mL.
Reduced IL-6-induced serum amyloid A (SAA) levels to 16.3 ng/mL.
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Animal Model:ddY (4-week-old female; postmenopausal osteoporosis induced by bilateral ovariectomy)[1]
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Dosage:10 mg/kg; 60 mg/kg
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Administration:p.o.; every other day; 4 weeks
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Result:Did not produce significant changes in measured parameters (bone mass, serum calcium, uterine weight, serum IL-6 levels).
Significantly suppressed ovariectomy-induced bone loss, resulting in a bone mass ratio of 1.92.
Reduced serum calcium levels to 11.3 mg/dL.
Did not alter uterine weight or serum IL-6 levels.
Chemical Information
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CAS No. 184877-64-3
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Masse moléculaire 369.45
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Formule C22H27NO4
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SMILES
O[C@@](C1=CC=CC=C12)(CCO3)[C@@]3([H])N2C[C@]4(C(C(CCCC)=C(C4=O)C)=O)C
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Hayashi M, et al. Suppression of bone resorption by madindoline A, a novel nonpeptide antagonist to gp130. Proc Natl Acad Sci U S A. 2002;99(23):14728-14733. [Content Brief]
[2]. Saleh AZ, et al. Binding of madindoline A to the extracellular domain of gp130. Biochemistry. 2005;44(32):10822-10827. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Madindoline A Related Classifications
HY-N14323 Related Classifications
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