2. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation MAPK/ERK Pathway Stem Cell/Wnt
  3. RANKL/RANK Reactive Oxygen Species (ROS) NF-κB p38 MAPK ERK JNK MMP
  4. RANKL-IN-1

RANKL-IN-1 is a selective and orally active Receptor Activator of Nuclear Factor-κ B Ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 can be used for the research of metabolic disease, such as osteoporosis.

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

RANKL-IN-1

RANKL-IN-1 Chemical Structure

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RANKL-IN-1 Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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ERK ERK1 ERK2 ERK5 ERK8

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JNK1 JNK2 JNK3 JNK

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

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Description

RANKL-IN-1 is a selective and orally active Receptor Activator of Nuclear Factor-κ B Ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 can be used for the research of metabolic disease, such as osteoporosis[1].

IC50 & Target[1]

MMP-9

 

In Vitro

RANKL-IN-1 (Compound 19u) (50-400 nM, 4 days) shows no significant cytotoxicity in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) inhibits RANKL-induced osteoclastogenesis without affecting osteoblast differentiation in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) reduces RANKL-induced ROS levels and inhibits bone resorption in RAW264.7 cells[1].
RANKL-IN-1 (50-400 nM, 4 days) inhibits the expression of proteins associated with RANKL-induced osteoclast differentiation in RAW264.7 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RANKL-IN-1 Related Antibodies

Immunofluorescence[1]

Cell Line: RAW264.7 cells
Concentration: 50, 100, 200 and 400 nM
Incubation Time: 4 days
Result: Decreased the size of the F-actin ring.
Reduced ROS levels.

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 50, 100, 200 and 400 nM
Incubation Time: 4 days
Result: Downregulated the protein expression of TRAF6 and phosphorylation of p65, p38, ERK and JNK.
Downregulated the activity of the c-Fos/NFATc1 signaling and inhibited the expression of CTSK and MMP-9.
In Vivo

RANKL-IN-1 (Compound 19u) (0.313-1.25 μg/mL, 96 h) attenuated bone loss in zebrafish osteoporosis models[1].
RANKL-IN-1 (0.5-2 mg/kg, p.o., every 2 days for 11 weeks) prevents systemic bone loss in ovariectomy-induced osteoporosis mice models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Zebrafish osteoporosis models[1]
Dosage: 0.313, 0.625 and 1.25 μg/mL
Administration: 96 h
Result: Increased zebrafish skull bone mass.
Animal Model: Ovariectomy-induced osteoporosis mice models[1]
Dosage: 0.5, 1 and 2 mg/kg
Administration: Orally administration, every 2 days for 11 weeks
Result: Increased the bone mineral density, bone volume fraction, trabecular number and the trabecular thickness.
Reduced the trabecular separation and expanded the marrow cavity and trabecular spacing.
Reduced total cholesterol and triglyceride levels and increased high-density lipoprotein cholesterol levels.
Had no significant changes in ALT, AST and BUN levels.
Molecular Weight

621.90

Formula

C40H55N5O
SMILES

CC1=C(C2=CC3=NC=CN=C31)C=C[C@@]4(C2=CC[C@@]5([C@@]4(CC[C@@]6(C5C[C@](C(N7CCC(CC7)N8CCNCC8)=O)(CC6)C)C)C)C)C
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
References
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RANKL-IN-1 Related Classifications

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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:

RANKL-IN-1RANKL/RANKReactive Oxygen Species (ROS)NF-κBp38 MAPKERKJNKMMPNuclear factor-κBNuclear factor-kappaBExtracellular signal regulated kinasesc-Jun N-terminal kinaseMatrix metalloproteinasesRANKLMAPKOsteoporosisRAW264.7ROSInhibitorinhibitorinhibit

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