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

RANKL-IN-2 is an orally active RANKL inhibitor with Kd values of 3.21 μM and 4.625 μM in the SPR and MST assays, respectively. RANKL-IN-2 binds to RANKL to interfere with RANKL-RANK interaction. RANKL-IN-2 suppresses osteoclastogenesis by inhibiting ROS, MAPK and NF-κB pathways. RANKL-IN-2 inhibits osteoclastogenesis via inhibition of RANKL-induced osteoclast formation, bone resorption, and osteoclast-specific gene and protein expressions in vitro.RANKL-IN-2 prevents bone loss in ovariectomized osteoporosis mice.RANKL-IN-2 can be used for the research of osteoporosis.

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RANKL-IN-2

RANKL-IN-2 Chemical Structure

CAS No. : 2667022-87-7

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RANKL-IN-2 Related Antibodies

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Description

RANKL-IN-2 is an orally active RANKL inhibitor with Kd values of 3.21 μM and 4.625 μM in the SPR and MST assays, respectively. RANKL-IN-2 binds to RANKL to interfere with RANKL-RANK interaction. RANKL-IN-2 suppresses osteoclastogenesis by inhibiting ROS, MAPK and NF-κB pathways. RANKL-IN-2 inhibits osteoclastogenesis via inhibition of RANKL-induced osteoclast formation, bone resorption, and osteoclast-specific gene and protein expressions in vitro.RANKL-IN-2 prevents bone loss in ovariectomized osteoporosis mice.RANKL-IN-2 can be used for the research of osteoporosis[1].

In Vitro

RANKL-IN-2 (compound 3w) (1 μM; 4 days) inhibits RANKL-induced osteoclastogenesis in RAW 264.7 cells with potent activity at 1 μM[1].
RANKL-IN-2 (0.0625-2 μM; 5 days) inhibits RANKL-induced osteoclastogenesis in BMMs dose-dependently with an IC50 of 0.577 μM[1].
RANKL-IN-2 (0.5-2 μM; 7 days) suppresses RANKL-induced F-actin ring formation and bone resorptionin by BMMs in a dose-dependent manner[1].
RANKL-IN-2 (0.5-2 μM; 5 days) inhibits RANKL-induced expression of osteoclast marker genes and proteins in BMMs dose-dependently[1].
RANKL-IN-2 (0.5-2 μM; 5 days) regulates ROS signaling in BMMs by inhibiting ROS production and promoting antioxidant enzyme expression[1].
RANKL-IN-2 (0.5-2 μM; 48 h) suppresses RANKL-induced intracellular and mitochondrial ROS production in BMMs dose-dependently[1].
RANKL-IN-2 (1 μM; 6 h pretreatment, 0-60 min RANKL stimulation) inhibits RANKL-induced MAPK and NF-κB signaling pathways in BMMs at 1 μM[1].
RANKL-IN-2 (0.5-2 μM; 7 or 21 days) does not affect osteoblast differentiation or mineralization in MC3T3-E1 cells[1].
RANKL-IN-2 is stable in PBS and rat plasma for at least 12 h[1].

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

RANKL-IN-2 Related Antibodies

Real Time qPCR[1]

Cell Line: Bone marrow macrophages (BMMs)
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 5 days
Result: Dose-dependently downregulated mRNA expression of C-Fos, MMP-9, TRAP, NFATc1, CTSK, and DC-STAMP compared to RANKL-induced controls.

Western Blot Analysis[1]

Cell Line: Bone marrow macrophages (BMMs)
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 5 days
Result: Dose-dependently decreased protein expression of NFATc1, MMP-9, c-Fos, and CTSK compared to RANKL-induced controls.\nDose-dependently inhibited RANKL-induced Nox1, TRAF6, and GTP-Rac1 (ROS-producing factors) and upregulated Catalase, GSR, and HO-1 (antioxidant enzymes).

Western Blot Analysis[1]

Cell Line: Bone marrow macrophages (BMMs)
Concentration: 1 μM
Incubation Time: 6 h (pretreatment); 0–60 min (RANKL stimulation)
Result: Reduced RANKL-induced phosphorylation of p38, ERK, JNK, and p65, inhibited IκBα degradation, and blocked p65 nuclear translocation.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t AUC0-24 F
Rat[1] 10 mg/kg p.o. >24 h 417 ng/mL / 8880 ng·h/mL 3.4 %
Rat[1] 1 mg/kg i.v. 4.901 h 8174.463 ng/mL 26617.245 ng·h/mL / /
In Vivo

RANKL-IN-2 (compound 3w) (10 mg/kg; p.o.; every other day; 8 weeks) prevents ovariectomy-induced bone loss in mice by increasing bone structural parameters and reducing osteoclast formation[1].

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

Animal Model: C57BL/6 (female, 7 weeks old, ovariectomy-induced)[1]
Dosage: 10 mg/kg
Administration: p.o.; every other day; 8 weeks
Result: Significantly increased bone volume/total bone volume (BV/TV), trabecular thickness (Tb.Th), and trabecular number (Tb.N) in OVX mice; reduced trabecular separation (Tb.Sp); reversed the decrease in bone surface (BS) caused by OVX; significantly decreased the number of TRAP-positive cells around the trabecula; suppressed osteoclast formation in vivo.
Molecular Weight

420.16

Formula

C17H13BrN2OSe
CAS No.
SMILES

CC(NC1=C2N=CC=CC2=C([Se]C3=CC=C(Br)C=C3)C=C1)=O
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-2 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-22667022-87-7RANKL/RANKReactive Oxygen Species (ROS)p38 MAPKNF-κBNuclear factor-κBNuclear factor-kappaBMAPKRAW 264.7 cellsRANKosteoclastogenesisMC3T3-E1 cellsovariectomized osteoporosis miceROSRANKLBMMsInhibitorinhibitorinhibit

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