Madindoline A

Cat. No.: HY-N14323: Data Sheet Handling Instructions
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Madindoline A is an orally active gp130 antagonist with a K_D 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.

For research use only. We do not sell to patients.

Madindoline A Chemical Structure

CAS No. : 184877-64-3

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STAT3 STAT5 STAT6 STAT1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

IL-6

Stat-3

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	CC₅₀	> 100 μM Compound: (+)-Madindoline A	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 26810262]
HepG2	IC₅₀	21 μM Compound: (+)-Madindoline A	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	[PMID: 26810262]
MH60	IC₅₀	8 μM Compound: 1	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	[PMID: 36971365]

In Vitro

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.

Cell Proliferation Assay^[1]

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
Concentration:	0.5, 1.75, 3.5, 7, 17.5, 35, 70 μM
Incubation Time:	72 h
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.

Cell Differentiation Assay^[1]

Cell Line:	M1 cells
Concentration:	70 μM (pre-incubation with IL-6)
Incubation Time:	72 h (pre-incubation with IL-6); 24 h (bead incubation)
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.

In Vivo

Madindoline A (10-60 mg/kg; p.o.; single administration) dose-dependently inhibits IL-6-induced serum amyloid A (SAA) production in mice^[1].
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.

Animal Model:	C3H/HeJ (6-week-old female; acute-phase response induced by intraperitoneal injection of 1 μg rhIL-6 per mouse)^[1]
Dosage:	10 mg/kg; 60 mg/kg
Administration:	p.o.; single dose
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.

Animal Model:	ddY (4-week-old female; postmenopausal osteoporosis induced by bilateral ovariectomy)^[1]
Dosage:	10 mg/kg; 60 mg/kg
Administration:	p.o.; every other day; 4 weeks
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.

Molecular Weight

369.45

Formula

C₂₂H₂₇NO₄

CAS No.

184877-64-3

SMILES

O[C@@](C1=CC=CC=C12)(CCO3)[C@@]3([H])N2C[C@]4(C(C(CCCC)=C(C4=O)C)=O)C

Structure Classification

Others

Initial Source

Microorganisms

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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.

[2]. Saleh AZ, et al. Binding of madindoline A to the extracellular domain of gp130. Biochemistry. 2005;44(32):10822-10827.

Madindoline A Related Classifications

Metabolic Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Madindoline A184877-64-3Interleukin RelatedSTATILHepG2 cellsgp130 homodimerizationpostmenopausal osteoporosisMH-60 cellsosteoclastogenesisextracellular domainIL-11IL-6serum amyloid Agp130Inhibitorinhibitorinhibit

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